-Five types of dopamine receptors are known:-Conversion of ATP to cAMP (as well as the left-over pyrophosphate) is catalyzed by adenylyl cyclase-Examples of biochemical purposes of protein kinases:
**Note that PKA's full name is cyclic adenosine monophosphate-dependent protein kinase meaning the enzyme's activity is dependent on which PKA and how much cAMP is present*
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F) Dopaminergic Areas of the Brain
Dopaminergic neurons are primarily concentrated in the ventral tegmental area and the substantia nigra pars compacta. However, this does not mean these are the only parts of the brain involved in dopaminergic processes. All known involved areas will now be briefly detailed:
1)
ventral tegmental area -- (VTA) -- involved in reward circuit, incentive/motivation, pleasure,
addiction
2)
substantia nigra -- unpredictable rewards, learning, addiction mimics reward/learn pattern
3)
frontal lobes -- pleasure, long-term memory, planning, drive/motivation
4)
nucleus accumbens -- reward, laughter, pleasure, addiction, and fear
5)
striatum -- planning, modulation of movement, executive function, reward feeling, motivation
6)
arcuate nucleus -- neuroendocrine neurons
7)
median eminence -- none; however, no blood brain barrier
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G) Dopaminergic Pathways
1)
mesocortical pathway -- One of the four major dopamine pathways in the human brain, the mesocortical pathway connects the ventral tegmentum with the frontal lobes of the cortex. In addition to its own purposes to run motivation and emotional response systems, the mescortical pathway is necessary to the proper function of the dorsolateral prefrontal cortex, which is the area most responsible for motor planning, organization, and regulation.
Neg.) Flaws in this pathway are often the cause of the negative aspects of schizophrenia, including avolition (extreme lack of motivation), speech poverty, and flat affect
2)
mesolimbic pathway -- Another of the four dopamine pathways in the brain. This major pathway links the ventral tegmentum with the nucleus accumbens, which is part of the striatum. The mesolimbic pathway is supposed to be essential in producing feelings of pleasure, as well as other feelings associated with reward and desire. Even though this pathway is highly connected with
drug addiction, research shows it is not the
euphoria that causes this here but rather incentive salience.
Neg.) The excess of dopamine associated with psychosis and schizophrenia is linked solely to this region. Since researchers know this quite well, anti-psychotics can be developed to specifically target the dopamine receptors in this specific path. The mesolimbic is also well known for losing many dopamine neurons in the progression of Parkinson's though the lost neurons are relatively asymptomatic and thus is not an issue until a large percentage of neurons have been lost.
3)
nigrostriatal pathway -- This is the third of the four dopamine pathways which happens to connect the substantia nigra with the striatum. Its key application is movement.
Neg.) This location is of most worry when it comes to Parkinson's victim's lose of neurons, primarily due to speed rather than effect (like the mesolimbic the neurons lost here are barely noticed). This area seems to be especially sensitive to antipsychotics which cause tardive dyskinesia due to the abundance of movement neurons here. Even some simple antipsychotics meant to reduce psychosis have be known to cause parkinsonian movement issues.
4)
tuberoinfundibular pathway -- The fourth dopamine pathway and the least neurotransmitter-based of them all. It seems most of the dopamine here is neuroendocrinal.
Neg.) It seems abnormal lactation, disrupted menstrual cycles, visual issues, sexual dysfunction, and headache are caused when antipsychotics block dopamine here as a
side effect, causing prolactin levels to increase in the blood.
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II. PHARMACEUTICALS AND THE DOPAMINERGIC SYSTEM*** *** *** *** *** *** ***NOTE: AUTHOR IS SIMPLY TRYING TO COMPILE INFO ON DRUGS RELATED TO THE DOPAMINERGIC SYSTEM. THIS IS NOT ALL-INCLUSIVE AND AUTHOR IS NOT RESPONSIBLE FOR INFORMATION NOT INCLUDED. INFORMATION PROVIDED IN "OTHER" SECTIONS SHOULD BE READ WITH CAUTION IN MIND. BE SAFE.*** *** *** *** *** *** ***ALSO, INFORMATION CONTAINED WITHIN THIS SECTION WAS DERIVED FROM THE FDA'S PROFESSIONAL MONOGRAPHS FOUND AT:
XXX no linking to another forum
*** *** *** *** *** *** ***ANY INFORMATION PERTAINING TO ILLICIT USE WAS FOUND AT : WWW.EROWID.ORG UNLESS OTHERWISE NOTED*** *** *** *** *** *** ***A) Quick Vocab
--
Ampakine -- new drug class of modified benzamide compounds designed to enhance attention span and alertness
--
Dopamine Reuptake Inhibitors -- drugs which bond to dopamine transports and prevent them from removing the DA from the synapse
--
Dopamine Agonists -- drugs which attach to dopamine receptors and simulate dopamine
--
Dopamine Antagonists -- drugs which attach to dopamine receptors and prevent dopamine from entering
--
GABA (gamma-amoniobutyric acid) -- the primary inhibitory neurotransmitter in the CNS as well as the retina
--
Prodrug -- a drug which is administered inactive and becomes an active compound in vivo
--
Racemate (racemic) -- a mixture which is made of two molecules of identical structure but different chirality; thus,
racemic - having equal amounts of left- and right-handed enantiomers
--
RC --
research chemical
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C) Over-The-Counter Medications, Grey Market Items, Etc.
CONTENTS:
1) PHENYLALANINE
2) TYROSINE
3) THEANINE (AKA L-THEANINE)
4) YOHIMBE
5) MUCUNA PRURIENS (TROPICAL VINE)
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-As we understand it, vastly more purposes....they are not fully understood yet
-PKA known to calcium channels linked to muscle contraction
-PKA tied to reward and motivation in nucleus accumbens
-PKA is used in metabolism
1) Phenylalanine
SYSTEMATIC NAME:
2-Amino-3-phenyl-propanoic acid
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2) Tyrosine
SYSTEMATIC NAME:
(S)-2-Amino-3-(4-hydroxyphenyl)-propanoic acid
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3) Theanine
SYSTEMATIC NAME:
2-Amino-4-(ethylcarbamoyl)butyric acid
Theanine is an amino acid which is believed to be found only in tea plants. The known neurochemical effects of theanine on the body are an increase of alpha brain waves as well as stimulating the production of the neurotransmitter GABA. Interestingly, theanine is actually an analogue of glutamate, the most common excitatory neurotransmitter as well as the precursor for GABA (the two neurotransmitters actually have counterbalancing effects), but despite being analogous to glutamate, it does not have quite the same affinity for glutamate receptors, rather simply stimulating release and/or production of GABA. This is the most likely cause of the relaxation and stress-relieving qualities of theanine. Theanine has shown potential medical uses for ADD/ADHD, PMS, and stress-relief.
*Dosing*-
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PERTAINING TO THEANINE; [Note: As of now, SWIM is going to disregard theanine's potential effects on other neurotransmitters because no studies seem to have been conclusive. SWIM would also like to note that theanine is a chiral compound, just like amphetamine, propanolol, and many others, and thus comes in D/L isomers (respectively this means dextrorotary and levorotary). Despite the minute difference between the isomers, the effects are profound. D-Theanine is not as efficiently absorbed and thus bioavailability is decreased. It is believed that some companies have used racemic D/L blends as L-Theanine to cut costs.]
4) Yohimbine
SYSTEMATIC NAME:
17α-hydroxy-yohimban-16α-carboxylic acid methyl ester
Yohimbine is the alkaloid which comes from the bark of the West-African evergreen Yohimbe. It is known to be an antagonist of the alpha2-adrenergic receptor causing an increase in epinephrine and norepinephrine. It also antagonizes 4 seperate serotonin receptors and use shows an increase of dopamine (some reports of up to 80%) as well as monoamine oxidase ihibiting properties.
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5) Mucuna pruriens
-tropical vine found in Central and South America shown to contain L-Dopa, Serotonin, 5-HTP, Nicotine, N,N-DMT, Bufotenine, and 5-MeO-DMT; despite L-Dopa being an excellent source of dopamine booster: A) too many other alkaloids in the plant and B) L-Dopa, as a dopamine agonist, runs a high risk of desensitization; likely little practice medical usage.
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D) Dopamine Reuptake Inhibitors
CONTENTS
1) AMINEPTINE
2) BENZATROPINE
3) BUPROPION
4) COCAINE
5) CFT
6) DEXMETHYLPHENIDATE
7) DEXTROMETHORPHAN
8) INDATRALINE
9) LOMETOPANE
10) MESOCARB
11) METHYLENEDIOXYPYROVALERONE
12) METHAMPHETAMINE
13) METHYLPHENIDATE
14) NOMISFENSINE
15) PHEN(-DI-)METRAZINE
16) PROCYCLIDINE HYDROCHLORIDE
17) RTI-121
18) TROPARIL
19) VANOXERINE
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1) Amineptine -- (atypical tricyclic antidepressant)
SYSTEMATIC NAME:
Due to demonstrating abuse potential while on market it was discontinued in 2005 and is currently off-patent.
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*Interactions*- monoamine inhibitors and drugs with monoamine inhibition properties
*Side Effects*- Common: acne; Rare/Very Rare: nervousness, irritability, insomnia, suicidal ideation, vasomotor episode, arterial hypotension, palpitations, hepatotoxicity (genetic predisposition likely in all cases)
*Contra-Indications*- chorea, MAOI's, infants less than one year of age, known hypersensitivity to amineptine
*Dosing*- Information unavailable.
*Prescription Medicines*- Survector (France, Spain, Italy, Phillipines); Maneon (Italy)
2) Benzatropine mesylate -- (anticholinergic)
SYSTEMATIC NAME:
In addition to reducing the effects of acetylcholine, as all anticholingergics do, benzatropine also acts as a dopamine reuptake inhibitor, primarily targeted at all forms of parkinsonism as well as for extrapyramidal disorders/symptoms (such as akinesia and akathisia), however, it is not to be prescribed for tardive dyskinesia). Given these extrapyramidal disorders/symptoms are often the result of anti-psychotics used for treatment of schizophrenia, benzatropine is often prescribed alongside the anti-psychotic treatment.
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*Other*-
*Interactions*- phenothiazines (largest class of anti-psychotics; includes aliphatic, piperidine, and piperazine groups), haloperidol, tricyclic anti-depressants
*Side Effects*- heat stroke, hyperthermia, fever, allergic reaction (skin rash), urinary retention, dysuria, blurred vision, dilated pupils, toxic psychosis, exacerbation of pre-existing psychotic symptoms, nervousness, depression, numbness of fingers, paralytic ileus, constipation, vomiting, nausea, dry mouth, tachycardia
*Contra-Indications*- patients under three years of age, hypersensitivity to benzatropine; has not been tested for use in pregnant women; aggravation and adverse effect in those with tardive dyskinesia and angle-closure glaucoma
*Dosing*- The drug is contained as a liquid for intramuscular injection. One mL of injection contains: 1mg benzatropine mesylate, 9mg sodium chloride, and 1mL. Usual daily dosage for parkinsonism treatment is 1-2mL, although the range of usage goes from .5mL to 6mL. For treatment and control of the effects of antipsychotic drugs, the recommended dosage is 1-4mL, either once or twice daily. In cases of acute dystonia, 1-2mL is the effective dose.
*Prescription Medicines*- Cogentin; generic
3) Bupropion (Amfebutamone) -- (atypical antidepressant/nicotine antagonist)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
*Prescription Medicines*- Wellbutrin, Zyban, generic (bupropion hydrochloride)
4) Cocaine -- (stimulant/appetite suppressant)
SYSTEMATIC NAME:
Cocaine's primary mechanism of action in the body is inhibition of monoamine uptake, which was demonstrated in rats at the ratio of 2:3 of serotonin to dopamine and 2:5 for serotonin to norepinephrine. The drug acts like all other MAOI's, by binding to transporters and preventing their function. Like many other dopaminergic drugs of abuse, cocaine is theorized to be highly linked to the ventral tegmental area, nucleus accumbens, and the frontal lobes of the cortex, since these areas are extremely rich in dopamine and receptors, as well as ties to the brain's "reward system."
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*Other*- LD50 of cocaine is 95.1mg/kg in mice.
*Interactions*- [too many to list currently]
*Side Effects*- Common (at medical doses): loss of sense of taste/smell; Other: abdominal pain, chills, confusion, dizziness/lightheadedness, excitement, nervousness, restlessness, fast/irregular heartbeat, general discomfort, hallucinations, headache, increased sweating, nausea
*Contra-Indications*- allergy to cocaine, pregnant, breast-feeding, children, older adults, cancer, history of chest pain, history of convulsions, fast/irregular heartbeat, heart disease, high blood pressure, liver disease, history of myocardial infarction, overactive thyroid, Tourette's syndrome, history of drug abuse
Illicit use:
Doses for illicit use vary widely due to factors such as tolerance. In addition, use is often measured by the illicit user by number of lines. Therefore, accurate doses are hard to determine. Other sources denote one line, which ranges from 35-100mg, as an average dose
*Dosing*- Use is rare/undocumented and so estimated:
Medical use:
Doses are administered by a doctor or nurse in the smallest effective dose. It should be noted that 400mg is never exceeded.
*Illicit Use*-
*Medical Use*- Still used as a local anesthetic in crystal or solution form.
5) CFT -- (stimulant/RC)
SYSTEMATIC NAME:
CFT is also sometimes known as beta-CFT or (-)-2[beta]-Carbomethoxy-3[beta]-(4-fluorophenyl)tropane. For the sake on being concise, it will only be referred to as CFT here. CFT is a dopamine reuptake inhibitor which is structurally an analogue of cocaine. In tests on animals, it has been shown to be 3-10 times more powerful than cocaine as well as lasting seven times longer. CFT's most common forms are a naphthalenedisulfonate salts, hydrochloride salts, and a free base. Despite thirty years of research, little is known about the compound and it has not history of human abuse.
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*Other*- Said to be a Schedule II by supplier Sigma-Aldrich, though it is not listed on the DEA's website as such. Regardless, it will fall under analogue laws.
*Interactions*- MAOI's, etc.
*Side Effects*- Said to be the same as cocaine although mere exposure is supposed to cause overdose-like effects.
*Contra-Indications*- Unknown. Likely similar to cocaine.
*Dosing*- Unknown. Rumored to be highly toxic, though thought to be a method of discouraging abuse.
6) Dexmethylphenidate -- (stimulant)
SYSTEMATIC NAME:
This is nothing more than the dextro-isomer-only version of methylphenidate (most commonly known as Ritalin). It is designed as a more practical form of methylphenidate since it is thought that levomethylphenidate cause many of metabolic and unwanted side effects. Further information that would apply here will be found at methylphenidate.
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*Other*- While it seems the removal of levomethylphenidate does little to help with side effects, it does result in a dosage of about half that of racemate methylphenidate.
*Interactions*- acid suppressants, antacids (can alter release of drug); anticonvulsants, anticoagulants, SSRIs, trycyclicantidepressants (effects possibly potentiated by dexmethylphenidate); antihypertensive agents, pressor agents (effects can be decreased by dexmethylphenidate); MAOIs; [SWIM would like to note here something that may be of little concern to anybody but given it could potentially help, he will continue. If you are on beta-blockers for any condition (i.e. tremors, glaucoma), do not forget that they were designed as antihypertensive agents, it just happens that they treat other conditions at lower doses.]
*Side Effects*- fever, pharyngolaryngeal pain, dry mouth, dyspepsia, abdominal pain, nausea, anorexia, headache, decreased appetite, feel jittery, anxiety, dizziness, anorexia
*Contra-Indications*- anxiety, tension, agitiation, glaucoma, motor tics, family history or diagnosis of Tourette's syndrome, MAOI use, hypersensitivity to methylphenidate
*Dosing*- Focalin comes in tablet form at the following doses: 2.5mg, 5mg, 10mg; Focalin XR comes in extended release capsules at the following doses: 5mg, 10mg, 15mg, 20mg
*Prescription Medicines*- Focalin, Focalin XR, generic (dexmethylphenidate hydrochloride)
7) Dextromethorphan (DXM) -- (antitussive)
SYSTEMATIC NAME:
[pharmacological information will be added soon]
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*Other*- High, usually recreational doses, cause DXM to act like dissociative hallucinogen.
*Interactions*- Amiodarone (Cordarone), Fluoexetine (Prozac), Quinidine, CNS depressants, MAOIs, avoid smoking tobacco
*Side Effects*- Uncommon/Rare: confusion, constipation, dizziness, drowsiness, headache, nausea, stomach pain; OD symptoms: blurred vision, confusion, difficulty with urination, extreme drowsiness/dizziness, severe nausea/vomiting, shakiness/unsteady walk, slowed breathing, unusual excitement, nervousness, restlessness, severe irritability
*Contra-Indications*- dextromethorphan allergy, pregnancy, breast feeding, children, older adults, asthma, diabetes, liver disease, chronic bronchitis, emphysema, mucus with cough, slowed breathing
*Dosing*- All dosages given will be those described as "Adults and children 12 years of age and older."Lozenge dosages: 5-15mg every 2-4 hrs; Syrup dosages: 30mg every six to 6-8 hrs; Extended-release oral suspension dosages: 60 mg every 12 hrs.
*OTC Drugs*- Benylin (Adult Formula Cough Syrup, Pediatric Cough Suppressant), Cough-X, Creo-Terpin, Delsym Cough Formula, Diabe-TUSS DM Syrup, Hold DM, Pertussin (CS, DM), Robitussin (Maximum, Pediatric), Sucrets 4 Hour Cough Suppressant, Trocal, Vicks 44 Cough Relief
8) Indatraline -- (monoamine reuptake inhibitor)
SYSTEMATIC NAME:
Also known as Lu 19-005, Indatraline, as a nonselective monoamine inhibitor, acts to block reuptake of norepinephrine, dopamine, and serotonin. It has also shown effects very similar to those of cocaine, however, less potent and may have potential as a treatment for cocaine addiction. [SWIM believes this is still a research chemical and this is all he has so far; look for updates]
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
9) Lometopane -- (stimulant)
SYSTEMATIC NAME:
Also known by the chemical name "(-)-2[beta]-Carbomethoxy-3[beta]-(4-iodophenyl)tropane," Lometopane is a stimulant that is primarily used in research. Its structure is pheyltropane based and thus it potentially a cocaine analogue under US law. It is considered to be extremely potent and thus has use in measuring dopamine neuron damage and loss in Parkinson's patients. [SWIM, it seems, must delve deeper if he wants info about this one; check back.]
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
10) Mesocarb -- (stimulant/antidepressant/anticonvulsive)
SYSTEMATIC NAME:
Due to it being a Soviet-developed drug, Mesocarb is still widely unknown and unsearched by the West. Acting as dopamine reuptake inhibitor it is said to be slower acting, longer lasting, and less neurotoxic than dextroamphetamine. [Beyond this SWIM doesn't want to detail much more because the only English-language source of info found was Wikipedia and due to the nature of the info and his inability to cross-reference with the Russian links he didn't want to put it on here yet; check back.]
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
11) Methylenedioxypyrovalerone -- (stimulant/NERI)
SYSTEMATIC NAME:
Also known as MDPV or MDPK, this drug is a designer drug with no history of medical use. It inhibits reuptake of norepinephrine and dopamine, apparently with the potency of four times that of methylphenidate. Although it does not hold illegal status in any country, it may possibly be fall under analogue illegal status (bears a semblance to ecstacy and other MDxx's) in countries with analogue laws.[Information here will clearly be rough and possibly inaccurate; SWIM will post for now but check back later.]
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*Other*- Despite being a methylenedioxyphenylalkylamine derivative, like ecstacy, it does not act anything like most of these MDxx substances. [SWIM predicts this will show up on a drug test as amphetamine like MDMA does; he will look into the nature of the test to make a better prediction.]
*Interactions*- [Check back.]
*Recreational Effects*- CNS stimulation, euphoric feeling, sexual urges, agitation, anxiety, insomnia; certain aphrodisiatic effects also noted
*Contra-Indications*- [Check back.]
*Dosing*- Erowid Experience Vaults showed doses ranging as follows: 10.5mg insufflated across 8 hours, 7.5 mg insufflated once, and 80mg insufflated across 6.5 hours. None of the experiences were negative or involved overdoses. The 80mg noted a strong stimulant "crash."
12) Methamphetamine -- (psychostimulant/sympathomimetic)
SYSTEMATIC NAME:
[Pharmacology will be up soon; SWIM wants to research a bit more and distinguish isomers.]
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*Other*- The methamphetamine used in Desoxyn is the dextromethamphetamine isomer. The left-handed levo- isomer is found in Vicks inhalers and has virtually no effect on the CNS.
*Interactions*- insulin requirements may be altered in diabetics, guanethidine, MAOIs, trycyclic antidepressants, other sympathomimetic amines, phenothiazines,
*Side Effects*- elevated blood pressure, tachycardia, palpitation, cardiac arrest (cases of abuse), psychosis, dizziness, dysphoria, overstimulation, euphoria, insomnia, tremor, restlessness, headache, tics, diarrhea, constipation, dry mouth, unpleasant tast, urticaria, impotence, changes in libido, growth suppression in youth with long-term stimulant use
*Contra-Indications*- pregnancy, breast feeding, children under the age of 12, older adults, glaucoma, advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, known hypersensitivity to sympathomimetic amines, history of drug abuse
*Dosing*- Desoxyn comes in tablet form at one dosage: 5mg. Initial dose is usually 5mg/daily. Dose is increased by 5mg/day each week until an effective dose is targeted. The usual effective dosage is reported as 20-25mg.
*Prescription Medicines*- Desoxyn, generic (methamphetamine hydrochloride)
b) levomethamphetamine -- aka levmetamfetamine --
a) dextromethamphetamine --
13) Methylphenidate -- (stimulant)
SYSTEMATIC NAME:
Though often deemed a dopamine reuptake inhibitor, not enough is known about the drug pharmacologically to make that declaration. The leading theory on its mechanism is that it activates the brain stem's arousal system as well as the cortex. As far as monoamines go, there have been some affinities noted. Studies show methylphenidate does have a affinity for bind to dopamine and norepinephrine transporters. Furthermore, the more active dextro- isomer of methylphenidate has a quite notable affinity for norepinephrine specifically. Both isomers also displayed an affinity for 5HT receptors but no acts of binding were recorded. Also noteworthy is a 2004 study which showed that methylphenidate does act as a reuptake inhibitor for dopamine and, like amphetamines, they cause a release of dopamine. However, methylphenidate seemed to release old stores of dopamine while amphetamines seemed to be using newly produced dopamine. Regardless, we still have no conclusive answers.
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In regards to the 2004 study mentioned above, methylphenidate's release of dopamine already stored in pre-synaptic vesicles in comparison with amphetamine's release of newly-created dopamine could explain why some patients who experience the effects of amphetamine treatments are unable to get the same effects from methylphenidate. The method used to determine these theories on where each drug releases dopamine from is also quite interesting. The antipsychotic drug reserpine (which is actually widely discontinued due to its irreversibility and side effects) actually depletes the pre-synaptic vesicles of their monoamines and furthermore irreversibly blocks them from storing monoamines. Knowing this, researchers realized that reserpine completely negates the effects of methylphenidate while leaving amphetamine completely unaffected. Which brings up a curious possibility to the author:
*Other*- The extended-release mechanism in Concerta is considerably different than that of many other extended-release ADD/ADHD medications, such as Ritalin-SR, Adderall XR, and Dexedrine. The pill, which looks no different than most other tablet medications, has a specially designed core which regulates the rate at which water enters, thus controlling the release of the drug. Concerta, via this release mechanism, is known to help control the hills (describing the rising and falling of methylphenidate levels in the plasma when displayed on a graph; this also correlates with moment by moment effectiveness of the drug) which are common with methylphenidate.
[Note: The following is nothing more than a rant by the author comprised entirely of opinion and theory developed from his own mind's logic flow.] Since reserpine can negate the effects of methylphenidate, due to the inavailability of dopamine in the vesicles, theoretically this explains the ineffectiveness of methylphenidate in some people. In the case of individuals who suffer from a disorder which is theoretically caused by dopamine deficiency (see Part IV) as well as recieve no or little effect from methylphenidate, could this lead to an explanation for previously cause-less symptoms or problems? Input, opinions, or down-right insults/shutdowns of this theory are certainly welcome.
*Interactions*- acid suppressants, antacids (can alter release of drug); anticonvulsants, anticoagulants, SSRIs, trycyclic antidepressants (effects possibly potentiated by dexmethylphenidate); antihypertensive agents, pressor agents (effects can be decreased by dexmethylphenidate); MAOIs; [SWIM would like to note here something that may be of little concern to anybody but given it could potentially help, he will continue. If you are on beta-blockers for any condition (i.e. tremors, glaucoma), do not forget that they were designed as antihypertensive agents, it just happens that they treat other conditions at lower doses.]
*Side Effects*- fever, pharyngolaryngeal pain, dry mouth, dyspepsia, abdominal pain, nausea, anorexia, headache, decreased appetite, feel jittery, anxiety, dizziness, anorexia
*Contra-Indications*- anxiety, tension, agitiation, glaucoma, motor tics, family history or diagnosis of Tourette's syndrome, MAOI use, hypersensitivity to methylphenidate
*Dosing*- Ritalin comes in tablet form at the following dosages: 5mg, 15mg, and 20mg. Ritalin-SR comes in tablet form and is only available at the dosage of 20mg. Concerta comes in extended-release tablet form at the following dosages: 18mg, 27mg, 36mg, and 54mg. Note: Only dosages for patients over six years of age will be listed. For all forms of methylphenidate the lowest possible dosage with effect should be taken. All instant-release tablets are taken either once or twice daily and extended-release forms are taken once daily.
*Prescription Medicines*- Ritalin, Concerta, generic
14) Nomifensine
SYSTEMATIC NAME:
Sometimes known as Merital, nomifensine was a fairly typical dopamine reuptake inhibitor researched and used primarily in the 1970's and 1980's for use as an antidepressant. The drug was also researched for use in ADHD and Parkinson's, however, despite successful animal testing, the drug seemed not to benefit human subjects. Despite being originally quite well recieved due to effectivness, few adverse effects, and little abuse potential, it is no longer used in medicine due to stimulant abuse potential, anemia, kidney and liver toxicity, overstimulation, and hyperthermia. Despite this, it is still used in research of links between dopamine and addiction due to one of its more unique effects on the brain.
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*Interactions*- [Likely MAOIs but need more research.]
*Side Effects*- dry mouth, headache, nausea
*Contra-Indications*- [Need more research; check back.]
*Dosing*- Common dosage was 50-225mg per day. Dosing as high as 400-600mg caused many of the side effects which led to itswithdrawal from the market.
15) Phen(-di-)metrazine -- (stimulant/anorectic)
SYSTEMATIC NAME:
Closely tied to older pharmaceutical methods of weight loss, phendimetrazine is chemically related to amphetamine. Little is actually known about the drug's mechanism though it is known that about 30% of it metabolizes into phenmetrazine once administered. Phenmetrazine is an ancestor pharmaceutical of phendimetrazine. Phenmetrazine, known as Preludin, was quite popular in the 1950's because it had less side effects and yet was more effective than amphetamine as a weight loss solution. However, the fact that it had less side effects, and also because the manufacturers claims that is was less euphoric was probably not true (it was considered more euphoric by some), led to it having quite an appeal among amphetamine addicts. The drug was pulled off the market by the late-fifties, though this was likely due to reports of psychosis similar to that which is amphetamine-induced. Regardless, the actual pharmacology of phendimetrazine is not well known and in recent years it is rarely prescribed in any case.
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*Other*- The anoretic, and so probably the weight loss, effect of the drug tends to wear off in as little as 14 days due to tolerance.
*Interactions*- all other CNS stimulants, MAOIs
*Side Effects*- palpitation, tachycardia, elevation of blood pressure, overstimulation, restlessness, dizziness, insomnia, tremor, headache, psychosis, agitation, flushing, sweating, blurring of vision
*Contra-Indications*- known hypersensitivity to sympathomimetics, advanced arteriosclerosis, cardiovascular disease, moderate to severe hypertension, hyperthyroidism, glaucoma, notably nervous/agitated patients, history of drug abuse
*Dosing*- 35mg once or twice daily
*Prescription Medicines*- Bontril, generic (phendimetrazine tartrate)
16) Procyclidine hydrochloride -- (anticholinergic)
SYSTEMATIC NAME:
This drug is commonly used for treatment of parkinsonism and drug-induced extrapyramidal symptoms. [As far as the pharmacology of the drug, not even the FDA clinical/professional fact sheet has much more than that. SWIM will hunt; check back later.]
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*Other*- LD50 (intravenously) is 60mg/kg.
*Interactions*- haloperidol, phenothiazines
*Side Effects*- tachycardia, palpitations, orthostatic hypotension, disorientation, confusion, memory loss, hallucinations, agitation, nervousness, depression, drowsiness, giddiness, lightheadedness, rash, urticaria, decreased sweating, mydriasis, blurred vision, dry mouth, nausea, vomiting, epigastric distress, constipation, paralytic ileus, urinary retention, urinary hesitancy, muscle weakness, acute suppurative parotitis, hyperthermia, heat stroke
*Contra-Indications*- angle-closure glaucoma, children, pregnancy,
*Dosing*- Kemadrin is only available in 5mg tablets. Common dose is between 15-20mg, gradually increased from a low starting dosage.
*Prescription Medicines*- Kemadrin
17) RTI-121 -- (highly selective DRI)
SYSTEMATIC NAME:
This phenyltropane (structurally similar to cocaine) based stimulant was developed in the 1990's and is reserved for research purposes. Its high potency and duration imply many risks for human abuse, however, due to its transporter binding process and speed it is theorized to have a lower abuse potential than cocaine. Due to its very specific binding with dopamine transporters it is most useful in mapping dopamine in research studies.
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*Other*- No recorded human abuse. [SWIM will hunt.]
18) Troparil -- (stimulant/RC)
SYSTEMATIC NAME:
This is yet another research chemical that acts as a dopamine reuptake inhibitor and is phenyltropane based. It has been shown to be equal in potency to cocaine although the duration is much longer, due to the absence of the link, which was easily and quickly metabolized, that connects the phenyl and tropane parts. It is used in research for dopamine mapping. Human abuse has not yet been documented, likely due to high cost (see note below about legality).
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E) Dopamine Agonists
CONTENTS
1) APOMORPHINE
2) BROMOCRIPTINE
3) DIHYDROERGOCRYPTINE
4) FENCAMFAMINE
5) LEVODOPA
6) LISURIDE
7) MESULERGINE
8) METERGOLINE
9) PERGOLIDE
10) PRAMIPEXOLE
11) ROPINIROLE
12) ROTIGOTINE
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*Other*- An interesting legality issue is raised with Troparil. Although Troparil is not currently a scheduled illegal substance in any country, it would theoretically fall under an analogue law at first glance since it is phenyltropane based. However, analogue laws only currently cover additions or substitutions to groups of illegal drug structures. Troparil, however, is a simplification of an illegal drug molecule, created by removing the link between the phenyl and the tropane rings. Therefore, this very instant it is not even illegal under analogue laws. Furthermore, in the case that someone decided to manufacture and sell this compound, as happened with methylone, they could likely get away with it, unlike the manufacturers of the methylone-containing Explosion, because even with the ability to set a precedence including simplification in analogue laws, it would have to be a broad change covering all simplifications of analogues. However, ethanol itself is an simplified version of GHB. Interesting.
1) Apomorphine -- (emetic)
SYSTEMATIC NAME:
This potent and non-ergoline dopamine agonist is primarily prescribed as a treatment for Parkinson's disease. The drug displays primary affinities for all dopamine receptors (from order of strongest to least: 4, 5, 3, 2, 1) as well as the 1D, 2B, and 2C adrenergic receptors. It is believed that the stimulation of the D2 receptors of the caudate-putamen is the drug's primary mechanism although that is just theoretical. The drug is also sometimes prescribed for erectile dysfunction.
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*Other*- Despite being derived from morphine, the drug has no binding affinity, nor effect whatsoever on opioid receptors.
*Interactions*- 5HT-3 antagonists, antihypertensive medications, vasoldilators, dopamine antagonists, any drug known to prolong the QT interval (such as haloperidol)
*Side Effects*- yawning, dyskinesias, nausea/vomiting, somnolence, dizziness, rhinorrhea, hallucinations, edema, chest pain, increased sweating, flushing, pallor
*Contra-Indications*- known hypersensitivity to apomorphine or sodium metabisulfite
*Dosing*- Dosages should begin at 0.2mL and may be increased if ineffective by 0.1mL every few days, not exceeding a dosage of 0.6mL. Administration is intended to be subcutaneous only. Any interruption of treatment lasting longer than a week requires starting again at a 0.2mL dosage.
*Prescription Medicines*- Apokyn, generic (apopmorphine hydrochloride)
2) Bromocriptine mesylate -- (ergoline-based)
SYSTEMATIC NAME:
Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2-methylpropyl)-
This dopamine agonist, derived from ergoline, is primarily used in the treatment of pituitary tumors and Parkinson's disease.
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
3) Dihydroergocryptine -- (ergoline-based)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
4) Fencamfamine -- (stimulant/appetite suppressant)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
5) Levodopa -- (prodrug)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
6) Lisuride -- (iso-ergoline)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
7) Mesulergine -- (ergoline-based)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
8) Metergoline -- (ergoline-based)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
9) Pergolide -- (ergoline-based)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*
10) Pramipexole -- (non-ergoline)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
11) Ropinirole -- (non-ergoline)
SYSTEMATIC NAME:
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
12) Rotigotine -- (non-ergotamine)
SYSTEMATIC NAME:
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F) Dopamine Antagonists
CONTENTS
1) AMOXAPINE
2) ARIPIPRAZOLE
3) CLOZAPINE
4) DROPERIDOL
5) DOMPERIDONE
6) METOCLOPRAMIDE
7) OLANZAPINE
8) QUETIAPINE
9) RISPERIDONE
10) ZIPRASIDONE
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1) Amoxapine -- (tricyclic anti-depressant)
SYSTEMATIC NAME:
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2) Aripiprazole -- (aypical anti-psychotic)
SYSTEMATIC NAME:
7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one
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3) Clozapine -- (atypical anti-psychotic)
SYSTEMATIC NAME:
8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine
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4) Droperidol
SYSTEMATIC NAME:
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5) Domperidone
SYSTEMATIC NAME:
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6) Metoclopramide
SYSTEMATIC NAME:
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7) Olanzopine
SYSTEMATIC NAME:
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8) Quetiapine
SYSTEMATIC NAME:
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9) Risperidone
SYSTEMATIC NAME:
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10) Ziprasidone
SYSTEMATIC NAME:
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G) Eugeroics
CONTENTS
1) ADRAFINIL
2) CX717
3) MODAFINIL
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*Other*-
*Interactions*-
*Side Effects*-
*Contra-Indications*-
*Dosing*-
1) Adrafinil -- (stimulant/prodrug)
SYSTEMATIC NAME:
Adrafinil is nothing more than the earlier and prodrug form of modafinil. Modafinil likely became preferred and thus manufactured due to quicker onset of effects.
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2) CX717 -- (ampakine)
SYSTEMATIC NAME:
Researched drug which stimulates glutamate and presumably AMPA receptors and shows possible use for ADHD and Alzheimer's. The drug has some problems with the FDA.
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3) Modafinil -- (stimulant)
SYSTEMATIC NAME:
[SWIM needs to really sift through this FDA report to get things straight. If you need the info it can all be found here: xxxx
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H) Other
CONTENTS
1) AMPHETAMINE (AKA SPEED, ADDERALL, DEXEDRINE, DEXTROAMPHETAMINE)
2) CATHINONE (INCL. METHCATHINONE, KHAT; AKA CAT, METHCAT)
3) 4-METHYL-AMINOREX (INCL. ALL AMINOREX ANALOGUES?)
4) PEMOLINE
5) LYSERGIC ACID DIETHYLAMIDE
6) BENZYLPIPERAZINE
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*Other*- The drug patent is presumably held by Cephalon under the name Olmifon although it has not been through FDA approval procedures.
1) Amphetamine -- (stimulant)
SYSTEMATIC NAME:
Amphetamine belongs in a seperate category from the other dopaminergics because it does not act like any of the either two main classes. Amphetamines only two mechanisms of action are a forced expulsion of dopamine contained in synaptic vesicles as well as amphetamines affinity for the DATs (dopamine active transporter), which takes control of it, denying it it's ability to clear the synapse of dopamine. Although this second act is technically reuptake inhibition, SWIM considers amphetamines to be certainly not dopamine reuptake inhibitors. [SWIM hopes that is the only time his personal opinion must be used.] Additional FDA material shows the drug to also act somewhat as an MAOI, preventing monoamine oxidases from breaking down dopamine to homovanillic acid, although methamphetamines, due to the additional methyl group, are much more effective as an MAOI.
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2) Cathinone/Methcathinone -- (stimulant)
SYSTEMATIC NAME:
Cathinone is an alkaloid present in the leaves of the shrub, Khat, and methcathinone is one of its analogues, which is synthetic. Methcathinone does not cross the blood-brain barrier as well as methamphetamines due to a slightly polar bond in its structure, but in other ways acts quite similar. The drug acts as both a serotonin and dopamine reuptake inhibitor. It is not known to have any effects on the norepinephrinergic system. The lack of these effects is the likely reason for its placement as a Schedule I substance, since it likely has no uses in treatment of ADD/ADHD.
DRUG INFO: xxxx
It should also be noted that weight, gender, build, and height have shown to have no effect on the metabolization and subsequently the plasma concentrations, and thus intensity, of d/l-amphetamines. However, even though equal doses are bioequivalent and are not effected by the above factors, this does not mean a dose safe for one "first-timer" is safe for another. Differing neurochemical systems can have huge effects on how the drug affects the body.
4) ANTACIDS ARE A QUICK, EASY WAY TO GET AN ALKALINE IN THE SYSTEM QUICKLY
3) KEEP OMEGA 6 TO OMEGA 3 INTAKE RATIO AT AROUND 2:1; IN ADDITION, ENSURE HEALTHY SOURCES
2) DEEP, HEALTHY BREATHING LEADS TO CELL SATURATION WITH OXYGEN AND A HIGHER pH
*Other*- Amphetamine absorbtion and expulsion is highly dependent on bodily pH levels. Presumably due to its high pKa level, even with average urine pH levels about half of the administered dose is found in urine as alpha-hydroxy-amphetamine with another 30-40% being found as pure amphetamine. Basic, or alkaline, body enviroments will cause a potentiated and more efficient metabolization of amphetamines. Possible methods of increasing bodily pH levels include:
*Interactions*- MAOI's, tricyclic antidepressants, SSRI's, SSNRI's, etc...
1) DIET--DRINK PLENTY OF WATER, NO CARBONATED BEVERAGES, BEER, ETC. AND PEEK AT THIS:
http://www.snyderhea.../alkalinity.htm
*Side Effects*- Common: loss of appetite, weight loss, insomnia, headache, dizziness; Other: nervousness, irritability, over-stimulation, restlessness, unpleasant taste, dry mouth, bruxism, nausea, stomach pain, euphoria, suspicion/paranoia, addiction, tolerance; Rare: tics, high blood pressure, rapid pulse, halluncinations, Tourette's syndrome, cardiomyopathy, amphetamine psychosis, death
*Contra-Indications*- arteriosclerosis, cardiovascular disease, hypertension, hyperthyroidism, hypersensitivity to sympathomimetic amines, glaucoma, history of drug abuse, MAOI use in the past 14 days
[Author suggests xxxx for further info, Dexedrine, etc.]
Adderall XR is available in the following doses: 5mg, 10mg, 15mg(blue pellets?); 20mg, 25mg, 30mg(red/yellow pellets)
Typical doses for treatment of narcolepsy range from 5-60mg daily, while 40mg is rarely exceeded in ADD/ADHD treatment.
XR capsules contain the following inactive ingredients:gelatin capsules (edible inks, kosher gelatin, and titanium dioxide), hydroxypropyl methylcellulose, opadry beige, methacrylic acid copolymer, sugar spheres, talc and triethyl citrate
*Dosing*- Adderall IR is available in the following doses: 5mg(white); 7.5mg, 10mg(blue); 12.5mg, 15mg, 20mg, 30mg(yellow)
*Illicit Use*- Known by the street name, "Speed," abusers and illicit users of amphetamines will either acquire prescription drugs via illegal means, synthesize amphetamine themselves, or purchase unprofessionally synthesized amphetamine. Most unprofessionally synthesized amphetamine is dextroamphetamine sulfate.
IR tablets contain the following fillers, binders, etc: lactitol, magnesium stearate, microcrystalline cellulose and colloidal silicon dioxide
*Prescription Medicines*- an amphetamine salt blend (using Shire Pharmaceuticals 72-28 d-/l-amp blend) is available as Adderall (instant-release), Adderall XR (extended-release; using the Microtrol delivery system), as well as by the generic name AMPHETAMINE SALTS (note: only instant-release currently; not extended-release version of amp. salt blends yet exists). Dexedrine, produced by GlaxoSmithKline, is the same essential drug, however it is 100% d-amphetamine sulfate. It also comes in instant-release tablets and sustained-release capsules (SPANSULE delivery system).
a) dextroamphetamine -- since amphetamines are chiral compounds they have left-handed and right-handed versions of the compound. Dextroamphetamine is the right-handed amphetamine isomer. D-amphetamine is recognized by many to be much more effective and potent than the levo-isomer of the same drug. While Shire Pharmaceuticals uses 72-28 blend of d-/l-amphetamines (the l-isomers help for a longer-lasting pill as well as a smoother pill), the generic extended release amphetamine is 100% dextroamphetamine.
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3) 4-Methyl-aminorex
SYSTEMATIC NAME:
4-methyl-5-phenyl-2-amino-oxazoline
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4) Pemoline
SYSTEMATIC NAME:
2-amino-5-phenyl-1,3-oxazol-4-one
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5) Lysergic acid diethylamide (LSD)
SYSTEMATIC NAME:
(6aR,9R)-N,N-diethyl-7-methyl-4,6,6a,7,8,9-hexahydroindolo-[4,3-fg]quinoline-9-carboxamide
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6) Benzylpiperazine (BZP)
SYSTEMATIC NAME:
1-benzylpiperazine
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I) OTHER VARIOUS PHENETHYLAMINES
CONTENTS
NEED TO RESEARCH - -
http://en.wikipedia.....henethylamines
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J) PASSIVELY-DOPAMINERGIC CHEMICALS
CONTENTS
1) ALCOHOL
2) CAFFEINE
3) IBOGAINE
4) THC
***ALSO AT LEAST SOME OPIOIDS---RESEARCH
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1) Alcohol
SYSTEMATIC NAME:
Ethanol
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2) Caffeine
SYSTEMATIC NAME:
1,3,7-trimethyl-1H-purine-2,6(3H,7H)-dione
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3) Ibogaine
SYSTEMATIC NAME:
12-Methoxyibogamine
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4) THC (Δ9-tetrahydrocannabinol)
SYSTEMATIC NAME:
(−)-(6aR,10aR)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydro-6H-benzo[c]chromen-1-ol
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K) CHEMICALS WITH UNIQUE DOPAMINERGIC EFFECTS
CONTENTS
1) GAMMA-BUTYROLACTONE
2) GAMMA-HYDROXYBUTYRIC ACID
3) NICOTINE
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1) Gamma-Butyrolactone (GBL)
SYSTEMATIC NAME:
Dihydrofuran-2(3H)-one
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2) Gamma-Hydroxybutyric Acid (GHB)
SYSTEMATIC NAME:
4-Hydroxybutanoic acid
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3) Nicotine
SYSTEMATIC NAME:
(S)-3-(1-Methyl-2-pyrroli-dinyl)pyridine
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POSSIBLE EFFECTS OF DRI/AGONIST USE:
*TOLERANCE: AS NOTED BEFORE IN PART I, NEUROTRANSMITTER TRANSPORTERS SERVE THE PURPOSE OF REUPTAKE THE NEUROTRANSMITTER FOR RECYCLING IN ORDER TO PROTECT THE RECEPTOR FOR CONSTANT STIMULATION. USE OF ANY DOPAMINE REUPTAKE INHIBITOR OR DOPAMINE AGONIST (AMPHETAMINE INCLUDED) OVER A PERIOD OF TIME OR IN AN ABUSIVE FASHION CAN RESULT IN DESENSITIZATION OF THE RECEPTOR RESULTING IN TOLERANCE. YES, THIS IS TOLERANCE BUILD-UP IN DOPAMINERGICS. IF YOU ABUSE YOU NEUROCHEMICAL SYSTEM IT MAY CHANGE ON YOU.*
*AMPHETAMINE PSYCHOSIS (STIMULANT PSYCHOSIS): WHEN USING STIMULANTS FOR EXTENDED PERIODS OF TIME (THIS RISK IS ESPECIALLY PRESENT WITH AMPHETAMINES AND METHAMPHETAMINES) IT IS POSSIBLE TO BECOME PSYCHOTIC. THOUGH THIS STATISICALLY ONLY OCCURS WITH CHRONIC USERS AND BINGE DOSES, IT IS POSSIBLE FOR IT TO HAPPEN OFF JUST ONE DOSE. WATCH WHEN COMBINING ANY DRUGS WHICH STIMULATE THE BODIES DOPAMINERGIC SYSTEM: THE CAUSE OF THIS IS LIKELY A FLOODING OF DOPAMINE INTO THE MESOLIMBIC PATHWAY (SLEEP DEPRIVATION ASSISTS THE PSYCHOSIS) AND SUBSEQUENTLY THE DOPAMINE CANNOT BE EXPELLED. THIS EXPERIENCE IS NEUROCHEMICALLY AND PHYSICALLY EQUIVALENT TO BEING TEMPORARILY SCHIZOPHRENIC.
BE CAREFUL!*
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III. MEDICAL CONDITIONS OF DOPAMINE UNDERSTIMULATION
Causes of Dopamine Deficiency
Although we understand very little about the causes or underlying reasons for the understimulation of dopamine receptors and the conditions which can derive from that, we know that, if dopamine understimulation is the case, then it must be a case of either excessively low dopamine levels in the brain or permanantly damaged or faulty receptors. At this point in history we understand very little about these conditions but know that they can result from the following:
1) Genetics -
2) Diet -
3) Drug Abuse -
Just as often as the cause of a dopaminergic is discovered, one is given up on, without a diagnosis.
Symptoms of Dopamine Deficiency
-Fatigue
-Inability to concentrate
-Difficulty with decision making and problem solving
-Cravings for meth, coffee, nicotine, or food
-Loss of interest in sex or inability to climax
-Lack of motivation, even for hobbies
-Depression (characterized by inability to feel joy and pleasure)
-Low energy levels
-Lethargy
-Tremor
-Attention deficits
-Trouble with memory
-Social anxiety
Disorders Believed To Be Caused By Insufficient Dopamine Stimulation
-Restless Legs Syndrome (RLS)
-Parkinson's Disease
-ADD/ADHD
-Depression
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IV. MEDICAL CONDITIONS OF DOPAMINE OVERSTIMULATION
Disorders Believed To Be Caused By Excess Dopamine Stimulation
-Schizophrenia
-Amphetmaine Psychosis
-Tourette's Syndrome
-Impulsive Behavior
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V. SOURCES AND REFERENCES
II-D-13:
http://findarticles....404/ai_n9356900
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VI. THINGS FOR FURTHER INVESTIGATION
neurotransmitters
http://www.benbest.c...d/anatmd10.html
serotonin syndrome
xxxx broken link
GABA
https://www.neurorel...e.php?issue=237
theanine
http://www.delano.co...ine-Sharpe.html
pharmacokinetics
http://www.boomer.org/c/p4/#topics
pKa
http://www.chemicalf...?page=pkavalues
receptor affinities!
http://pdsp.med.unc.edu/pdsp.php
*Other*- While the chemistry involved in methcathinone synthesis is quite simple, the resultant free base is very unstable and the reaction is reversed resulting in ephedrine from which it came.
*Effects*- Cathinone is described to have both stimulant and aphrodisiatic effects. Methcathinone has the following effects:
*Dosing*- No real great sources on the dosages needed here. Seems a considerable number of khat leaves must be chewed to get the effects of cathinone. Oral dosages for methcathinone ranged from 50-400mg and insufflated dosages supposedly are about 1/4 of that for equal effects or 15-100mg. Furthermore, intravenous dosages seem to run about 1/4 of the insufflated dosage or about the 10-20mg range. [Note: Due to the low number of experiences reported for this drug the dosages are estimated and may not be accurate. As with all drugs, start with lower dosages to err on the side of safety.]
-- euphoria, increased alertness, dilated pupils, rapid breathing, increased heart rate, inability to stop talking, increased emptathy, increased social ability, inability to understand the concept of priority and false understanding of importance, increased/decreased sexual function and desire, hypertension, tachycardia, decreased appetite
Might help you in researching.
Provided by: 
