189 replies to this topic

[Ampamet]

I tried it again a few days ago under different circumstances. I first had a moderate (40mg) dose of vyvanse, then took Pitolisant 3 hours in. The effects of the vyvanse almost completely disappeared. I felt none of the mild euphoria and quick thinking I usually experience. I take amphetamines very infrequently, so tolerance is unlikely to be the cause. If I remember correctly, there was a study showing H3 antagonism attenuated some of the effects of methamphetamine in lab mice.

[Multicultural Harmony]

I tried it again a few days ago under different circumstances. I first had a moderate (40mg) dose of vyvanse, then took Pitolisant 3 hours in. The effects of the vyvanse almost completely disappeared. I felt none of the mild euphoria and quick thinking I usually experience. I take amphetamines very infrequently, so tolerance is unlikely to be the cause. If I remember correctly, there was a study showing H3 antagonism attenuated some of the effects of methamphetamine in lab mice.

That sounds about right to me. Though I'm too lazy to dig through pubmed for it. Pitolisant itself also has no reinforcing effects. In my own travails 5-ht2c antagonists have shown to increase the reinforcing effects of hedonic subs like amphs (I won't take these, lol!), nicotine and even caffeine (imo). Maybe pitolisant reduces the hedonic effect of your stims by increasing the availability of 5-ht to agonize 5-ht2 receptors? Who knows.

I think pitolisant and similar H3 inverse agonists may prove beneficial for narcoleptics but that is probably about it. So far my trial with rubidium and taltirelin are proving somewhat lackluster, which at least rules out the TRH receptor as a possible beneficial target for me.

Intracellular Ca2+ seems somewhat interesting as to what regulates its homeostasis... as a potential target to reduce stress-induced cognitive decline. PLC pathway, yea!

Edited by Pitolisant, 18 December 2013 - 01:50 AM.

[Multicultural Harmony]

Well Rubidium definitely is worthless, still doing taltirelin, however.

[socialpiranha]

I'm interested to know if anyone who recieved this has paranoia or delusional thinking and if so what was the effect of pitolisant on this? It has been hypothesized to be a possible treatment based on the theory that the mentioned symptoms are caused by the brain being in a sort of mixed state of partial loss of consciousness and hyperadrenergic function.

[Multicultural Harmony]

You should check pubmed?
http://www.ncbi.nlm....pubmed/20437030

My guess is that pito probably has low potential for improving diseases that involve paranoia.

Perhaps D2 antagonists if you can tolerate them.

[socialpiranha]

You should check pubmed?
http://www.ncbi.nlm....pubmed/20437030

My guess is that pito probably has low potential for improving diseases that involve paranoia.

Perhaps D2 antagonists if you can tolerate them.

yeah i only get paranoid when i smoke weed (i don't smoke anymore) so it was more out of general interest. plus h3 ants/inverse ags are in clinical trails for schizophrenia http://www.ncbi.nlm....1?dopt=Abstract

[Multicultural Harmony]

You should check pubmed?
http://www.ncbi.nlm....pubmed/20437030

My guess is that pito probably has low potential for improving diseases that involve paranoia.

Perhaps D2 antagonists if you can tolerate them.

yeah i only get paranoid when i smoke weed (i don't smoke anymore) so it was more out of general interest. plus h3 ants/inverse ags are in clinical trails for schizophrenia http://www.ncbi.nlm....1?dopt=Abstract

Maybe for some of the negative symptoms/social aspects of shiz. However, based off of the user reports here I think its only real use will end up being as an alternative to modafinil for narcolepsy. I'm still hoping for some more positive reports to roll in from the volunteer guinea pigs here who have tried it, whom I guess represent a handful of healthy test subjects.

Glycine transporter inhibitors may be interesting too. Although sarcosine had no anxiolytic benefit in my own experiments. Currently my focus is on Ca2+ homeostasis, substances that modulate intracellular Ca2+ this seem to show benefit in my own guinea pig.

[JPC16]

So I finally got some time to extensively try out pitolisant.

Overall, I am pretty positive about pitolisant but for me it does have quite a few side effects. The most pronounced side effect for me was abdominal discomfort. This discomfort can best be described as the feeling (and sound ) of having an empty stomach (the feeling of being hungry).

Besides the abdominal discomfort I also experienced some sleeping problems but these only occured at dosages over 40 mg. I think my sleep was more superficial and my sleep onset latency increased from 20-30 minutes to about 50 minutes.
So for me I actually expierence more side effects with pitolisant than with modafinil since I don't experience any side effects from modafinil. But again this applies for me personally.

But I also have some good things to say about pitolisant. For me, dosages up to 40 mg are ideal since it provides me with a cleaner stimulant feeling compared to modafinil. Cleaner in the way that it doesn't tend to “overfocus” me which modafinil and amphetamines do. Pitolisant still allows you to “think freely” which is definitely diminished while using heavier stimulants. But this “advantage” drops away when bigger dosages are used (above 40 mg). I put advantage in quotation marks because that overfocusing effect for me can be normal focus for someone with ADHD. So I think it does have a potential as an ADHD drug. It would definitely be a good option if you experience a lot of side effects with modafinil since pitolisant overall presents with less side effects. I guess I am the exception.

I also have to note that the pitolisant was combined with caffeine (100 mg) which could have intensified certain side effects.

[Geoffrey1]

Does anyone know of a reliable source for Pitolisant powder?  Would like to obtain some---from individual or on-line source. 

A little late to the game i know

thanks

[Reformed-Redan]

Here is Pitolisant commercially available to you guys!

 

http://tht.co/pitolisant.html

[PWAIN]

Wow, thats a brilliant site. Thanks.

Here is Pitolisant commercially available to you guys!
 
http://tht.co/pitolisant.html

[MangekyōPeter]

Yeah, that site looks awesome, so many awesome compounds.

[Shorty]

why did yadayada get downvoted?

[chemicalambrosia]

why did yadayada get downvoted?

 

I didn't down vote him(quite possibly just someone with a general grudge), but he just posted a link to that store in three threads. He also hasn't said anything about it(the store). Whats the deal with the store, is he affiliated with it in some way or what? I've never heard of the store, but it seems to have quite a number of novel substances, including two that yadayada led group buys for. All in all, an interesting situation. Pretty cool though if everything is legit and its offering custom synthesis in such an open and easy manner as well.

[amara bin]

1:43
Well I'll just update this as long as it will work and just list my subjective experiences. As far as I can tell the single greatest benefit is having a feeling of lucidity and not daydreaming. I don't feel like daydreaming at all where I complete a task and just into this sleep mode until I have to jerk myself out of it by whatnot, anger or whatever. So far so good.

Oh, no. The greatest benefit to my in the internal chatter has died down. I just noticed this since I'm functioning very nicely. It's always that negativisitc internal chatter that gets me down in the dumps and its pretty much quieted out. Dunno.

 

This is interesting: are you still dealing with this internal chatting?

I'm asking you because this has been a very distinct tract of my thinking behavior for a long time, even with interesting paths.

 

My 2 cents is that is the result of LTP and the war against it ...aka...there are thoughts that are uncontrollable , some are negative, some are irrelevant (but maybe a little obsessive), and some are positive and are often a sort of defensive mechanism against our brain comes up against the firsts.

 

My cure is alternating nmda- (night, weekends) and nmda+ stacks (morning).

My secret weapon is definitely "emergency" Picamilon & occasional Seligiline MAOI-A dosage. 

 

I even gave names to my inner voices:

God  (the part of me that stays sane even when everything else goes bananas)

Beax (my defense system against human  idiocy)

[jerrybusey]

Anyone have any updates on this? It's been available on THT for awhile so I'm assuming some people have tried it. I'm looking for a modafinil replacement since I had an adverse reaction to modafinil but I loved its effects. I'm interested in experiences with it either alone or in conjunction with a conventional stimulant.

 

In this paper https://www.google.c...hYuZTYeuLZFnTYw  (if this doesn't link right it's Inocente et al from Clinical Neuropharmacology & Volume 35, Number 2, March/April 2012 and the full text is available with a google search)

 

it's mentioned near the end that there seemed to be synergy between pitolisant and conventional stimulants when treating narcolepsy. I'm wondering if pitolisant and a low dose stimulant may be a better option than either alone when treating other fatigue issues or adhd. Any thoughts or experiences?

[Infinityandbeyond]

I haven't heard alot of reviews not sure why?

[Area-1255]

OP - why Pitolisant out of curiosity? Wouldn't thioperamide  (which crosses the BBB easier and has more studies), has an anti-inflammatory effect as well be a better candidate? 

All Histamine H(3) antagonists will for sure boost alertness / wakefulness, probably = to or greater than modafanil. Depending on your histamine neuron genetics.

 

Also most Histamine H(3) antagonists should also boost GABA and would actually have anxiolytic effects....

They also would raise serotonin, dopamine etc -

As I always say

 

"The Histamine H3 Receptor is one of the most, if not the most nasty pieces of garbage in the human neuronal systems"

 

It is responsible for most of histamine's negative effects, including on anxiety and depression.

[jerrybusey]

OP - why Pitolisant out of curiosity? Wouldn't thioperamide  (which crosses the BBB easier and has more studies), has an anti-inflammatory effect as well be a better candidate? 

All Histamine H(3) antagonists will for sure boost alertness / wakefulness, probably = to or greater than modafanil. Depending on your histamine neuron genetics.

 

Also most Histamine H(3) antagonists should also boost GABA and would actually have anxiolytic effects....

They also would raise serotonin, dopamine etc -

As I always say

 

"The Histamine H3 Receptor is one of the most, if not the most nasty pieces of garbage in the human neuronal systems"

 

It is responsible for most of histamine's negative effects, including on anxiety and depression.

 

Why would you want something that also messes with H4? Pitolisant is at least in phase 3 human trials.

[Area-1255]

 

OP - why Pitolisant out of curiosity? Wouldn't thioperamide  (which crosses the BBB easier and has more studies), has an anti-inflammatory effect as well be a better candidate? 

All Histamine H(3) antagonists will for sure boost alertness / wakefulness, probably = to or greater than modafanil. Depending on your histamine neuron genetics.

 

Also most Histamine H(3) antagonists should also boost GABA and would actually have anxiolytic effects....

They also would raise serotonin, dopamine etc -

As I always say

 

"The Histamine H3 Receptor is one of the most, if not the most nasty pieces of garbage in the human neuronal systems"

 

It is responsible for most of histamine's negative effects, including on anxiety and depression.

 

Why would you want something that also messes with H4? Pitolisant is at least in phase 3 human trials.

 

H4's are pro-inflammatory and excess activation can cause immune disorders and chronic itching over time. 

 

Curious, did any of you experience allergic reactions or a worsening of ashtma that would be indicative of the increased histamine levels with Pitolisant?

 

Interesting, but I have had chronic allergies/asthma as a kid, not so much in the past few years.

But when taking pro-histamine ingredients/H3 antagonists....no symptoms re-emerge other than sneezing in bright sunlight and 

the occasional head itching.

 

I've tried; Betahistine, Clobenpropit, Conessine, and a very small sample of Thioperamide.

 

Have yet to try Pitolisant. Seems quite interesting though.

 

Betahistine was alright, but the dosing and poor oral bioavailability made it not worth the money.

Clobenpropit had more anti-anxiety effects, and Conessine was the most stimulating by far.

Thioperamide had the most balanced effect.

 

All of them nearly eradicated the "internal chatter" and had a euphoric sense - though I was using them with caffeine.

 

I used to think histamine was all stimulating, couldn't be farther from the truth.

Histamine allow's you to enjoy activities and to calm down the mental chatter - at least when H3's are blocked.....

 

 

[jerrybusey]

Reading more about H4 has me increasingly curious about it since I've always had energy and inflammatory issues and I now have Crohn's disease where H4 receptors may play a roll. Another study made mention of a possible role in H4 receptors in influencing the orexin system with this http://www.ncbi.nlm....pubmed/18345490 study as the reference. If anyone could get the full text for it I would greatly appreciate that.

[MrSliz1724]

 

 

OP - why Pitolisant out of curiosity? Wouldn't thioperamide  (which crosses the BBB easier and has more studies), has an anti-inflammatory effect as well be a better candidate? 

All Histamine H(3) antagonists will for sure boost alertness / wakefulness, probably = to or greater than modafanil. Depending on your histamine neuron genetics.

 

Also most Histamine H(3) antagonists should also boost GABA and would actually have anxiolytic effects....

They also would raise serotonin, dopamine etc -

As I always say

 

"The Histamine H3 Receptor is one of the most, if not the most nasty pieces of garbage in the human neuronal systems"

 

It is responsible for most of histamine's negative effects, including on anxiety and depression.

 

Why would you want something that also messes with H4? Pitolisant is at least in phase 3 human trials.

 

H4's are pro-inflammatory and excess activation can cause immune disorders and chronic itching over time. 

 

Curious, did any of you experience allergic reactions or a worsening of ashtma that would be indicative of the increased histamine levels with Pitolisant?

 

Interesting, but I have had chronic allergies/asthma as a kid, not so much in the past few years.

But when taking pro-histamine ingredients/H3 antagonists....no symptoms re-emerge other than sneezing in bright sunlight and 

the occasional head itching.

 

I've tried; Betahistine, Clobenpropit, Conessine, and a very small sample of Thioperamide.

 

Have yet to try Pitolisant. Seems quite interesting though.

 

Betahistine was alright, but the dosing and poor oral bioavailability made it not worth the money.

Clobenpropit had more anti-anxiety effects, and Conessine was the most stimulating by far.

Thioperamide had the most balanced effect.

 

All of them nearly eradicated the "internal chatter" and had a euphoric sense - though I was using them with caffeine.

 

I used to think histamine was all stimulating, couldn't be farther from the truth.

Histamine allow's you to enjoy activities and to calm down the mental chatter - at least when H3's are blocked.....

 

Wait you have personally tried Conessine? I have yet to find any real reviews of personal use before. Anyone mind chiming in here? How was the half-life, experience, etc?

[Area-1255]

 

 

 

OP - why Pitolisant out of curiosity? Wouldn't thioperamide  (which crosses the BBB easier and has more studies), has an anti-inflammatory effect as well be a better candidate? 

All Histamine H(3) antagonists will for sure boost alertness / wakefulness, probably = to or greater than modafanil. Depending on your histamine neuron genetics.

 

Also most Histamine H(3) antagonists should also boost GABA and would actually have anxiolytic effects....

They also would raise serotonin, dopamine etc -

As I always say

 

"The Histamine H3 Receptor is one of the most, if not the most nasty pieces of garbage in the human neuronal systems"

 

It is responsible for most of histamine's negative effects, including on anxiety and depression.

 

Why would you want something that also messes with H4? Pitolisant is at least in phase 3 human trials.

 

H4's are pro-inflammatory and excess activation can cause immune disorders and chronic itching over time. 

 

Curious, did any of you experience allergic reactions or a worsening of ashtma that would be indicative of the increased histamine levels with Pitolisant?

 

Interesting, but I have had chronic allergies/asthma as a kid, not so much in the past few years.

But when taking pro-histamine ingredients/H3 antagonists....no symptoms re-emerge other than sneezing in bright sunlight and 

the occasional head itching.

 

I've tried; Betahistine, Clobenpropit, Conessine, and a very small sample of Thioperamide.

 

Have yet to try Pitolisant. Seems quite interesting though.

 

Betahistine was alright, but the dosing and poor oral bioavailability made it not worth the money.

Clobenpropit had more anti-anxiety effects, and Conessine was the most stimulating by far.

Thioperamide had the most balanced effect.

 

All of them nearly eradicated the "internal chatter" and had a euphoric sense - though I was using them with caffeine.

 

I used to think histamine was all stimulating, couldn't be farther from the truth.

Histamine allow's you to enjoy activities and to calm down the mental chatter - at least when H3's are blocked.....

 

Wait you have personally tried Conessine? I have yet to find any real reviews of personal use before. Anyone mind chiming in here? How was the half-life, experience, etc?

 

It lasts a looong time, insomnia is an under statement..gives a euphoric feel, sort of like Meth.

[DagnyT]

I'd like in on a gram. Are you the Shawn who has the Pay it Square page? I sent an email to that address expressing interest.

I am a long time member here but don't post much - too sleepy and out of it most of the time.

Thanks

[Reformed-Redan]

I'd like in on a gram. Are you the Shawn who has the Pay it Square page? I sent an email to that address expressing interest.

I am a long time member here but don't post much - too sleepy and out of it most of the time.

Thanks

The group buy was closed a while ago. You can get Pitolisant from THT.co. I'm not interested in nootropics anymore; but, most of the compounds I created group buys for are at that website. Don't mean to promote the site, just saying that it is available there. 

[Area-1255]

1:43
Well I'll just update this as long as it will work and just list my subjective experiences. As far as I can tell the single greatest benefit is having a feeling of lucidity and not daydreaming. I don't feel like daydreaming at all where I complete a task and just into this sleep mode until I have to jerk myself out of it by whatnot, anger or whatever. So far so good.

Oh, no. The greatest benefit to my in the internal chatter has died down. I just noticed this since I'm functioning very nicely. It's always that negativisitc internal chatter that gets me down in the dumps and its pretty much quieted out. Dunno.

This sounds really nice, I'm not really surprised though - anything that blocks histamine H3's will both enhance histamine neuronal activity and will calm your ass down but yet give you a smooth stim - histamine's neg's tend to come from that one god awful H3 receptor - which is negative feedback on not just histamine, but a whole bunch of other neurotransmitters - including locally active GABA terminal to where histamine isn't even involved, what that means is essentially....EVEN IF you had no brain histamine, the H3 blockers would still give a positive effect because the paradox is that some of these receptors are also located on NON HISTAMINERGIC terminals - which is ironic because it's classified as a histamine receptor. ..... it might as well be considered a multi-transmitter receptor, part of it is coming from cation -gated channel regulation and negative feedback on calcium channels as well....which is also very interesting.....

 

Also, this receptor should also relieve paranoia when you block it, because it seems to be, other than opioid receptors, one of the main histamine receptors or any receptor - that negates or inhibits oxytocinergic neurons..so you should have anxiolytic effects on multiple levels with H3 antagonists - based on what I've read - the potential for these compounds is practically limitless.

 

Social anxiety, dopamine deficiencies, Dementia, ADHD, OCD, HPTA dysfunctions, epilepsy....this may very well be the "holy grail" of findings and the ultimate pathway in longevity , especially for the brain........also they are being investigated for obesity and compulsive eating....

 

These are miracle compounds for sure, and also would serve as the ultimate vehicle for unlocking a new degree of willpower, to an extent unprecedented - I will be adding it to my "dopaminergic pot of gold" article as I continue my pursuit to finishing the map of ultimate perfection. 

[hullcrush]

I have 950 mg of this shipped for $9.99 cross posted on eBay. It definitely improved wakefulness, but this type of application for me has absolutely no purpose. PM me, I accept a boatload of payment methods.

[Area-1255]

I have 950 mg of this shipped for $9.99 cross posted on eBay. It definitely improved wakefulness, but this type of application for me has absolutely no purpose. PM me, I accept a boatload of payment methods.

Oh, eBay's selling it now too? Tell me, what supplier is going to sell a potent research chemical for 9.99 $, and why would you want to sell it? Are you trying to scam members with bunk goods?

[BieraK]

Bad news for the nootropics future....
THT may stop selling noots soon
"We're currently reevaluating our sales/marketing position. We may introduce a new coupon code in the very near future. Alternatively, we may decide to focus on bulk distribution and custom synthesis for corporations and research institutions, and may therefore stop direct retail sales entirely. We expect to reach a decision very shortly."
http://www.reddit.co...e_thinkin_bout/

There are another source for pitolisant?

[Area-1255]

Bad news for the nootropics future....
THT may stop selling noots soon
"We're currently reevaluating our sales/marketing position. We may introduce a new coupon code in the very near future. Alternatively, we may decide to focus on bulk distribution and custom synthesis for corporations and research institutions, and may therefore stop direct retail sales entirely. We expect to reach a decision very shortly."
http://www.reddit.co...e_thinkin_bout/

There are another source for pitolisant?

That's not going to happen.