• Log in with Facebook Log in with Twitter Log In with Google      Sign In    
  • Create Account
  LongeCity
              Advocacy & Research for Unlimited Lifespans

Photo
* * * * * 5 votes

Deprenyl finally a nootropic that works!


  • Please log in to reply
124 replies to this topic

#61 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 05 December 2008 - 10:26 PM

At higher dosages you generally just get a more speedy effect that tends to leave you a scattered and not as focused.


You nailed it! That's exactly how I feel after using 5 mg for the first time. I'm aso feeling a bit euphoric and high! lol

I ordered Cyprenil from cytopharma in mexico. The order arrived pretty quick but I never received a confirmation email. This is pretty good stuff. Ofcourse, it might be a placebo effect, but what an effect! I'm cutting down the dose to 1 mg per day after today.

I have social anxiety. People with social anxiety were found to have decreased dopaminergic functions in the mesocortical pathway (link). So I started experimenting with Tyrosine to raise Dopamine levels. To my surprise, this worked effectively well. I felt more motivated, energized and less depressed. Also, many of the symptoms of SA vanished!

I figured Deprenyl could do the same for me. Any thoughts on this? Since I've been using Tyrosine regularly to increase dopamine, should I cut back on the dose or even stop using it at all?

Edited by Lufega, 05 December 2008 - 11:00 PM.


#62 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 06 December 2008 - 12:56 AM

Update.

It's been about 2 hours since my first dose. I no longer feel tired and unfocused, I actually feel the complete opposite. I am thinking with more clearness and clarity and I've really productive this last hour.

sponsored ad

  • Advert
Click HERE to rent this advertising spot for BRAIN HEALTH to support LongeCity (this will replace the google ad above).

#63 8tyduecevet

  • Guest
  • 9 posts
  • 0

Posted 10 December 2008 - 04:12 PM

Update.

It's been about 2 hours since my first dose. I no longer feel tired and unfocused, I actually feel the complete opposite. I am thinking with more clearness and clarity and I've really productive this last hour.


Friend, do you have anything new to report? I have to admit that I have experimented with many things in life to feel better from rits, to modafinil, & testosterone therapy, working out religiously etc. I've had deprenyl for a while but was concerned about using it until I've done a weeks of research on the net and finally here on this site. I tried 1mg this morning and have never felt this good in my life - I'm 40. I am hoping this is not a 1 time thing. Please update on your experiences if you care to.

#64 FunkOdyssey

  • Guest
  • 3,443 posts
  • 166
  • Location:Manchester, CT USA

Posted 10 December 2008 - 04:36 PM

Report in after a month of continuous use, tell us about your overall mood and mentality, and any entertaining stories you might have about your responses to minor, everyday irritations. :)

#65 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 10 December 2008 - 06:02 PM

I will report back after the first month. I wanted to comment though, be careful not to take it late in the day. I've been sleeping in lately and take it after Noon. This stuff keeps me up past 4 AM. Yesterday I decided not to use it to try and regulate my sleep pattern. I also did not use any Tyrosine either. What a mistake! I was moody...lashed out at my brother over something petty. I felt tired, down and had no motivation. I was up until the crack of dawn anyways. This morning, I felt horrible! I felt depressed, anxious, tired, moody, you get the idea. I took 2 drops and 1 gram tyrosine and I feel amazing again.

I normally feel the effect of reduced dopaminergic activity. This is something I have to continually tweak to be functional. I wonder if my experience was that, or maybe deprenyl has some kind of rebound effect. But I doubt it. I might stay on two drops for a while. I am 30 years old but I know I have problems with dopaminergic function (i.e. NO motivation, social anxiety, etc.) I hope that's ok.

#66 8tyduecevet

  • Guest
  • 9 posts
  • 0

Posted 10 December 2008 - 07:19 PM

I will report back after the first month. I wanted to comment though, be careful not to take it late in the day. I've been sleeping in lately and take it after Noon. This stuff keeps me up past 4 AM. Yesterday I decided not to use it to try and regulate my sleep pattern. I also did not use any Tyrosine either. What a mistake! I was moody...lashed out at my brother over something petty. I felt tired, down and had no motivation. I was up until the crack of dawn anyways. This morning, I felt horrible! I felt depressed, anxious, tired, moody, you get the idea. I took 2 drops and 1 gram tyrosine and I feel amazing again.


Thank you both, I can report on my first day that there was an initial "high" a smooth high energy feel, that seems to have worn off by now. this was about 8am to 2pm. From what I've read I was only going to use 1mg eod. But i am wondering if that is not enough.

#67 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 12 December 2008 - 04:34 PM

Just a heads up. After I ordered the deprenyl from cytopharmonline in Mexico, a fraudulent charge appeared on my card for $700+ for that same date. I did not make any other purchses a +/- 2 days from that date.

#68 8tyduecevet

  • Guest
  • 9 posts
  • 0

Posted 12 December 2008 - 04:49 PM

Just a heads up. After I ordered the deprenyl from cytopharmonline in Mexico, a fraudulent charge appeared on my card for $700+ for that same date. I did not make any other purchses a +/- 2 days from that date.


dam let us know how that turns out, I have not used them before but it does not surprise me.

#69 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 20 December 2008 - 07:33 AM

dam let us know how that turns out, I have not used them before but it does not surprise me.


I sent them an email and they replied with the expected answer...blabla, we had nothing to do with that, blabla.

It's just a coincidence that right after I purchased from them, another charge appeared from Germany! The only other place I've been using my card has been Iherb, luckyvitamin, LEF, etc. I also scrub my laptop clean from spyware and what not almost weekly. Anyways, I hope American Express will eat that charge. For future purchases, I'll use pre-paid gift cards. :-D

#70 Ghostrider

  • Guest
  • 1,996 posts
  • 56
  • Location:USA

Posted 20 December 2008 - 10:35 AM

dam let us know how that turns out, I have not used them before but it does not surprise me.


I sent them an email and they replied with the expected answer...blabla, we had nothing to do with that, blabla.

It's just a coincidence that right after I purchased from them, another charge appeared from Germany! The only other place I've been using my card has been Iherb, luckyvitamin, LEF, etc. I also scrub my laptop clean from spyware and what not almost weekly. Anyways, I hope American Express will eat that charge. For future purchases, I'll use pre-paid gift cards. :-D


AMEX is pretty good about those charges. I had something similar happen to me which they caught and called me about it. Totally painless, it's been my favorite credit card, wish they would have supported SENS though last August in their charity donation event.

#71 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 21 December 2008 - 03:04 AM

Can deprenyl lead to dopamine tolerance? I was using 500 mg -1000 mg of tyrosine for a couple of months and this did wonder for social anxiety, mood, anhedonia and motivation. Really, this was a godsend! The first night I tried deprenyl, I used 5 drops and these effects were multiplied x1000! Naturally, I was up all night!

The second day i used 3 drops and had a similiar effect but I lowered the dose to 1 drop a day after that. It's been about two weeks now and tyrosine seems to have lost it's effectiveness. I increased the dose to 5 grams and still felt nothing. I even tried to increase the dose of deprenyl gradually to 4 drops and still, nothing.

Now I'm wondering if you can develop tolerance to using tyrosine and if the deprenyl sped this process. I also switched brands to source natural powder and maybe this is the problem but now I am not sure. I was using NOW capsules previously.

Any ideas on this?

#72 8tyduecevet

  • Guest
  • 9 posts
  • 0

Posted 22 December 2008 - 03:31 AM

Can deprenyl lead to dopamine tolerance? I was using 500 mg -1000 mg of tyrosine for a couple of months and this did wonder for social anxiety, mood, anhedonia and motivation. Really, this was a godsend! The first night I tried deprenyl, I used 5 drops and these effects were multiplied x1000! Naturally, I was up all night!

The second day i used 3 drops and had a similiar effect but I lowered the dose to 1 drop a day after that. It's been about two weeks now and tyrosine seems to have lost it's effectiveness. I increased the dose to 5 grams and still felt nothing. I even tried to increase the dose of deprenyl gradually to 4 drops and still, nothing.

Now I'm wondering if you can develop tolerance to using tyrosine and if the deprenyl sped this process. I also switched brands to source natural powder and maybe this is the problem but now I am not sure. I was using NOW capsules previously.

Any ideas on this?


My brother this is an interesting topic, i have used both but i wonder about the quality of the deprenyl you are using?

#73 medicineman

  • Guest
  • 750 posts
  • 125
  • Location:Kuwait

Posted 22 December 2008 - 02:22 PM

First time I try deprenyl liquid, i dunno. I feel really tired.

maybe i didnt get enough sleep last nite. i dunno.....

Edited by medicineman, 22 December 2008 - 02:47 PM.


#74 medicineman

  • Guest
  • 750 posts
  • 125
  • Location:Kuwait

Posted 22 December 2008 - 05:21 PM

i retract my previous statement. deprenyl works alright, not like I hoped though. An hour after taking 4 drops, i decided that this was going no where, so ill have a cup of coffee. went got a strong americano, with an extra espresso, thinking 'eh, might as well potentiate whatever i put in myself'. than i started getting an uneasy feeling in my stomach, like i had double dropped ritalin. suddenly, appetite disappeared, but i can feel my stomach growling, but no, i cannot eat. i become irritable, and unable to focus on one thing. i flick through my notes hoping to get a good study session done, but no, i am impatient to get to the next page, to finish the chapter. i try to relax, but i can feel that my hearts contractility is stronger. i get this feeling of impending doom (i attribute that last one to the stigma behing maoi's you get in med school). i go home, take 5mg of valium, and things get better, as usual with valium....

i think i will stick to 1mg and see how that goes from now on..... i really did not enjoy one aspect of that experience..... i blame myself for taking three extra drops.

#75 Lufega

  • Guest
  • 1,814 posts
  • 274
  • Location:USA
  • NO

Posted 23 December 2008 - 04:19 AM

8tyduecevet,

I am using cyprenil from cytopharma.

#76 doctordog

  • Guest
  • 161 posts
  • 0

Posted 23 December 2008 - 04:23 AM

potentially silly question, but how do you administer liquid deprenyl, especially when it requires such exact (i.e. drop-by-drop) dosing? are you meant to just tilt your head back, position the dropper over your mouth and let rip? i've mail-ordered some - which has yet to arrive - but am trying to work out the best way to go about it, given that even when using eyedrops i end up flooding my eyes with way more than required.

#77 SteveF

  • Guest
  • 17 posts
  • 6

Posted 25 March 2009 - 04:21 AM

Very easy, I just look in mirror and drop drops under my tongue. I have followed the doses for my age as suggested by James Kimball. I'm at 4 drops a day at one time.

I'm 57 yr old male, have eaten raw vegan for up to 9 months at a time, several times, fasted once for 10 days and watch what I eat no white flour, sugar or rice but I do use organic raw milk products some. I have taken deprenyl 9yrs, but in the last 8 years it is Cyprenil. I have heavily partied on 151+rum, colt 45 and herb for over 25yr in the past but not now in the last 8 years, I just do regular rum occasionally. I feel physically like I'm 21 and can sleep soundly anytime and anywhere and have zero pain. I take no other supplements. I have cured my prostate which those butcher doctors wanted to ruin my sex life and repaired a seperated shoulder which the doctor gods said at my age wouldn't totally heal and be pain free. The secret was raw vegan and chinese herbs and accupucture for 30 days. My shoulder is pain free and I sleep or work over 8 hours without having to urinate.

I had 2 bottles of original deprenyl so last month I unfroze one and used it. The taste of the Cyprenil was 98% similar to the Deprenyl. My only personal lab analysis.

Two people I know in the last year, one took it for longevity and noticed right away that his depression had lifted and to this day he is depression free and had stopped the Cyprenil. He was never informed previously that it was an anti depressant. The 2nd person knew this when she got and it did the same thing and relieved her depression.

All I can assume it is working as deprenyl. No bad side effects in anyone.

The thing I have to encourage everyone don't expect body changing effects right away, make a commitment to take it one year by itself without other mind drugs too see the whole results.


My only objection to this forum is that there is nobody taking Deprenyl because it is not being produced anymore.

Lets give thanks to the Man that made all this possible, James Kimball who died August 8 2007 alone in prison as a FDA political prisoner, instead being out of jail living a long life with his family.
He was deprived of what he had developed.

#78 bgwithadd

  • Guest
  • 820 posts
  • 16

Posted 25 March 2009 - 07:36 AM

Can deprenyl lead to dopamine tolerance? I was using 500 mg -1000 mg of tyrosine for a couple of months and this did wonder for social anxiety, mood, anhedonia and motivation. Really, this was a godsend! The first night I tried deprenyl, I used 5 drops and these effects were multiplied x1000! Naturally, I was up all night!

The second day i used 3 drops and had a similiar effect but I lowered the dose to 1 drop a day after that. It's been about two weeks now and tyrosine seems to have lost it's effectiveness. I increased the dose to 5 grams and still felt nothing. I even tried to increase the dose of deprenyl gradually to 4 drops and still, nothing.

Now I'm wondering if you can develop tolerance to using tyrosine and if the deprenyl sped this process. I also switched brands to source natural powder and maybe this is the problem but now I am not sure. I was using NOW capsules previously.

Any ideas on this?


You get dopamine tolerance, period, over time. Your brain adjusts to adding more by making less. Only time away from stimulants or dopamine boosters will fix it.

#79 Phreak

  • Guest
  • 116 posts
  • 1
  • Location:London, UK

Posted 26 April 2009 - 10:11 AM

Okay. There's a lot of stuff to read through here (which I've done), but I'm getting so much information fired at me I'm struggling to process it all!

I've used the Search function and opened up ALL the threads with the keywords 'selegiline' and 'deprenyl' in them, but am yet to find a simple, concrete answer to the following question. That's probably because there isn't one (hence all this discussion), but if someone could answer this - whether it be from personal experience or just the recommended amount - then that would be great:

Used sporadically (i.e. not daily), how much Deprenyl [Selegiline HCl] should be used to help increase focus/motivation/boost dopamine levels in a healthy subject?

I will not be taking it everyday.
I understand "motivation and focus" will not necessarily come about, I'm just saying that's what I'm trying it for.
I just want to know what is both a safe dose, but still an effective dose.

Thanks :)

#80 f00bar

  • Guest
  • 19 posts
  • 8

Posted 27 April 2009 - 04:47 PM

Here is what you are looking for. Btw, deprenyl inhibits MAO-B (deals with dopamine) in low dosages (2.5mg a day I think), and it only inhibits MAO-A (deals with serotonin) in dosages over 10mg a day. You have to remember though, deprenyl will build up in your system over time. This means that even at 1mg a day for an extended period of time will eventually start to inhibit MAO-B. I believe this to be true when taking it at 5-10mg a day for it eventually inhibiting MAO-A.

Hey, this is very interesting. My knowledge on pharmacology is very limited, so I ruled selegiline out in the beginning of my research as I take an SSRI. So, is it safe to take it with a low dose of an SSRI? I'm still hesitant to take more potent medications, but it seems it might be worth a shot. I'm just considering how to change my lifestyle including meds/nootropics intake. Answers or hints to where I find more info about selegiline combined w/ SSRIs will be much appreciated.

#81 Thorsten3

  • Guest
  • 1,123 posts
  • 3
  • Location:Bristol UK
  • NO

Posted 27 April 2009 - 05:48 PM

test
  • dislike x 1

#82 yowza

  • Guest
  • 283 posts
  • 36
  • Location:Midwest

Posted 28 April 2009 - 03:33 AM

I just took 5 mg of Deprenyl for the first time.

I've noticed an effect. I feel kind of relaxed while on it. However, for some reason I feel tired and find it hard to concentrate? I'm reading something and I keep losing my place for some reason. It's like my spatial reasoning/organization feels a bit off...?



Does anyone have an idea on why this may be?

#83 yowza

  • Guest
  • 283 posts
  • 36
  • Location:Midwest

Posted 28 April 2009 - 04:46 AM

I just took 5 mg of Deprenyl for the first time.

I've noticed an effect. I feel kind of relaxed while on it. However, for some reason I feel tired and find it hard to concentrate? I'm reading something and I keep losing my place for some reason. It's like my spatial reasoning/organization feels a bit off...?



Does anyone have an idea on why this may be?


Well, I'm not too thrilled about the effects. I may try it at 1.75 mg next time and see if I experience the same issues.

I'll probably do it next week once the drug has tapered off some.

At the 5 mg dosage concentration is negatively impacted somehow.

Edited by yowza, 28 April 2009 - 04:46 AM.


#84 blazewind

  • Member
  • 77 posts
  • 7
  • Location:USA

Posted 28 April 2009 - 04:54 AM

I'm not sure on the scientific basis for some people feeling tired on selegiline but here is a guess: Dopamine has a wide range of actions (depending on receptor type and area of the brain) and one of them is social bonding, phenylethylamine (which mao-b acts on) which interacts with dopamine is increased in people in love, and people in love can't concentrate on things and feel relaxed. Maybe you have lots of phenylethylamine and that is overwhelming the concentration effect. When I first took selegiline, during sex it greatly canceled concentration and gave me euphoria, and I get the same effect combined with PEA. Basically I felt great but it was impossible to concentrate, maybe what you are experiencing. At the moment sex is still greatly enhanced but I don't feel as much euphoria and don't feel tired, in fact it makes me less tried after instead. I have never felt tired on selegiline without sex or PEA. For me it gives me greatly enhanced focus, and I prefer this effect to my baseline.

#85 Guacamolium

  • Guest
  • 747 posts
  • 30
  • Location:Tahoe

Posted 28 April 2009 - 04:54 AM

Fuck Deprenyl.

(my biochemistry made me type that)

Edited by somethingtoxic, 28 April 2009 - 04:55 AM.

  • Pointless, Timewasting x 1

#86 blazewind

  • Member
  • 77 posts
  • 7
  • Location:USA

Posted 28 April 2009 - 05:13 AM

I forgot about this, one more theory, dopamine is increased after sleep deprivation to keep you awake and partially functioning. On selegiline it is extremely easy to ignore any sleepiness, and inadvertently get less sleep which may make you tired. For instance I noticed on selegiline I would wake up after 6 or 7 hours of sleeping (I need 9) seemingly feeling like it is time to wake up, but if I would wake up at this time selegiline would not have its full effect. Instead I have ignored this fake signal and go back to sleep and go by the clock to make sure I sleep 9 hours no matter what, and I get the focus effect.

Edited by blazewind, 28 April 2009 - 05:13 AM.


#87 yowza

  • Guest
  • 283 posts
  • 36
  • Location:Midwest

Posted 28 April 2009 - 05:16 AM

The whole CAE thing > MAOB is what got me interested in this. Here's the link if anyone's interested:
http://www.eternitymedicine.com/english/04_eternity_medicine_products/Deprenyl/deprenyl_article.htm
http://www.imminst.o...showtopic=29506

Fuck Deprenyl.

(my biochemistry made me type that)


Yeah, that was my attitude beforehand. However, a recent article I read about Deprenyl's potential CAE (catecholemergic activity enhancer) is what made me order this . The whole CAE thing is extremely interesting, I wonder if Depreny's the only potential compound that does this?

I'm not sure on the scientific basis for some people feeling tired on selegiline but here is a guess: Dopamine has a wide range of actions (depending on receptor type and area of the brain) and one of them is social bonding, phenylethylamine (which mao-b acts on) which interacts with dopamine is increased in people in love, and people in love can't concentrate on things and feel relaxed. Maybe you have lots of phenylethylamine and that is overwhelming the concentration effect. When I first took selegiline, during sex it greatly canceled concentration and gave me euphoria, and I get the same effect combined with PEA. Basically I felt great but it was impossible to concentrate, maybe what you are experiencing. At the moment sex is still greatly enhanced but I don't feel as much euphoria and don't feel tired, in fact it makes me less tried after instead. I have never felt tired on selegiline without sex or PEA. For me it gives me greatly enhanced focus, and I prefer this effect to my baseline.


Thanks for the info.

The only thing that's changed for me compared to your experience is that after this first initial dosage, I feel like my sex drive is diminished in some way cause I feel kind of flat and out of it. I don't really feel greatly enhanced focus like you do, so maybe there's a correlation there...

I just feel tired, abit confused (off in some way), and that's about it...

Your explanation is still insightful though. But there may be something else at play here, I can't put my finger on what...

I think I'm gonna go to bed and see how long this sticks around.

Edited by yowza, 28 April 2009 - 05:30 AM.


#88 blazewind

  • Member
  • 77 posts
  • 7
  • Location:USA

Posted 28 April 2009 - 05:42 AM

I overlooked that.
Looks like we have a new drug to try yowza?

a quick look:


Major depression and the synthetic enhancer substances, (-)-deprenyl and R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane.
Gaszner P, Miklya I.

National Institute of Psychiatry and Neurology, H-1021 Huvösvölgyi út 116, Budapest, Hungary. h12890gas@ella.hu

Because of the high number of therapy-resistant depressions and the growing number of suicides, there is still a great need for the development of antidepressants with a new pharmacological spectrum. The finding that phenylethylamine and tryptamine are endogenous enhancers of the impulse propagation mediated release of catecholamines and serotonin in the brain, and the development of synthetic enhancer substances opened the possibility to stimulate catecholaminergic and serotonergic neurons in the brain stem via a previously unknown mechanism. (-)-Deprenyl, a prototype of the phenylethylamine-derived synthetic enhancer substances, stimulates the catecholaminergic neurons in the brain but is almost ineffective on the serotonergic neurons. R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane, (-)-BPAP, the recently developed tryptamine-derived selective synthetic enhancer substance, is a hundred times more potent enhancer of the catecholaminergic neuronal activity than (-)-deprenyl, and is also a highly potent stimulant of the serotonergic neurons. Evaluation of the peculiar pharmacological profile, the high potency and unusual safeness and tolerability of (-)-BPAP cherish the hope that this compound by itself and in combination with uptake inhibitors may improve the effectiveness of drug therapy in major depression and diminish the number of therapy resistant cases.





The novel catecholaminergic and serotoninergic activity enhancer R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane up-regulates neurotrophic factor synthesis in mouse astrocytes.
Ohta K, Ohta M, Mizuta I, Fujinami A, Shimazu S, Sato N, Yoneda F, Hayashi K, Kuno S.

Clinical Research Center, Utano National Hospital, Narutaki, Ukyo, 616-8255, Kyoto, Japan. kiyoeohta@mail.goo.ne.jp

We investigated the effects of the novel catecholaminergic and serotoninergic activity enhancer R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane ((-)-BPAP) on the synthesis and secretion of neurotrophins, nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), and glial cell line-derived neurotrophic factor (GDNF), in cultured mouse astrocytes. The protein and mRNA levels of the neurotrophic factors were measured using the enzyme-linked immunosorbent assay and reverse transcription-polymerase chain reaction methods, respectively. The amounts of NGF, BDNF, and GDNF secreted from astrocytes into the culture medium increased by up to 120, two, and seven times higher than those of the control, respectively, by treatment with 0.35 mM (-)-BPAP for 24 h. The increases in NGF and GDNF induced by the treatment with (-)-BPAP was inhibited by concomitant treatment with actinomycin D for transcriptional blockade. Furthermore, the treatment with (-)-BPAP for 6 h increased the mRNA expression of NGF, BDNF, and GDNF. These results suggest that (-)-BPAP up-regulated neurotrophic factor synthesis in cultured astrocytes.




Enhancer substances: selegiline and R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane [(-)-BPAP] enhance the neurotrophic factor synthesis on cultured mouse astrocytes.
Shimazu S, Tanigawa A, Sato N, Yoneda F, Hayashi K, Knoll J.

Research Institute, Fujimoto Pharmaceutical Corporation, 1-3-40 Nishiotsuka, Matsubara, 580-0011, Osaka, Japan. soyaku@fujimoto-pharm.co.jp <soyaku@fujimoto-pharm.co.jp>

R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane [(-)-BPAP] is a potent "catecholaminergic and serotonergic activity enhancer (CAE/SAE)", which enhances the impulse-evoked catecholamines and serotonin release, e.g. (-)-BPAP enhances in vitro norepinephrine efflux from the slices of locus coeruleus in a bipolar manner with the two effective ranges of low (fM-pM level) and high (nM-microM level) concentrations. Here, the effects of (-)-BPAP and selegiline on the cultured mouse astrocytes were studied. The protein levels of the neurotrophic factors (NGF, BDNF and GDNF) in the conditioned medium of cultured astrocytes were determined by using ELISA. In the cultured astrocytes incubated for 24 h with selegiline, the synthesis of NGF and BDNF was significantly enhanced in the concentration dependent manner, with minimum effective concentrations of 4 x 10(-4) and 5 x 10(-4) M, respectively. (-)-BPAP also enhanced the NGF, BDNF and GDNF synthesis, with minimum effective concentrations of 5 x 10(-5), 1 x 10(-5), and 1 x 10(-6) M, respectively. Although the effects of (-)-BPAP on the NGF synthesis was tested in the range of 1 x 10(-15)-5 x 10(-4) M, the concentration response curve of (-)-BPAP was a single bell shape with the peak effect at 1 x 10(-4) M, and did not show any effects in low concentrations such as fM-pM level. Each concentration response curve of (-)-BPAP on BDNF and GDNF synthesis was a single bell shape with peak effects at 1 x 10(-3) M and 1 x 10(-4) M, respectively.











5.2. ()-BPAP, the tryptamine-derived representative
synthetic enhancer substance
The discovery that tryptamine is also an endogenous
enhancer substance (Knoll, 1994) opened the way for the
synthesis of a new family of enhancer compounds unrelated
to PEA and the amphetamines. ()-BPAP was selected as
the reference compound for further studies (Knoll et al.,
1999). For details of its chemistry see: Oka et al., 2001;
Yoneda et al., 2001.
The in vivo dose-dependent enhancer effect of ()-BPAP
on noradrenergic, dopaminergic, and serotonergic neurons
proved that this compound showed a substantially higher
potency than ()-deprenyl. ()-BPAP, the highly selective
tryptamine-derived synthetic enhancer substance is for the
time being the best experimental tool for the analysis of the
enhancer regulation.
P. Gaszner, 10 I. Miklya / Progress in Neuro-Psychopharmacology & Biological Psychiatry 30 (2006) 5– 14
()-BPAP significantly enhanced in 0.18 nmol concentration
the impulse propagation mediated release of [3H]-
noradrenaline and [3H]-dopamine and in 36 pmol concentration
the release of [3H]-serotonin from the isolated brain
stem of rats. The amount of catecholamines and serotonin
released from isolated discrete rat brain regions (dopamine
from the striatum, substantia nigra, and tuberculum olfactorium;
noradrenaline from the locus coeruleus; and serotonin
from the raphe) enhanced significantly in the presence of
1012–1014 M ()-BPAP. Racemic BPAP protected
cultured hippocampal neurons from the neurotoxic effect
of h-amyloid25 – 35 fragment in 1014 M concentration. In
rats ()-BPAP significantly enhanced the activity of the
catecholaminergic and serotonergic neurons in the brain 30
min after acute injection of 0.1 Ag/kg s.c. In the shuttle box,
()-BPAP was in rats about 130 times more potent than
()-deprenyl in antagonizing tetrabenazine-induced inhibition
of performance (Knoll et al., 1999).
In a recent study the effect of ()-BPAP was compared
to that of the known stimulants of catecholaminergic and/or
serotonergic neurons (desmethylimipramine, fluoxetine,
clorgyline, lazabemide, pergolide, and bromocriptine) on
electrical stimulation induced release of the labelled transmitters
from the isolated brain stem of rats following the
incorporation of [3H]-noradrenaline or [3H]-dopamine or
[3H]-serotonin by preincubation into the transmitter stores.
50 ng/ml ()-BPAP was the most effective concentration in
enhancing the nerve stimulation-induced release of [3H]-
noradrenaline and [3H]-dopamine while 10 ng/ml ()-BPAP
was highly effective in enhancing the release of [3H]-
serotonin. In contrast, 250 ng/ml desmethylimipramine
(DMI), a selective inhibitor of the uptake of noradrenaline,
did not change significantly the nerve stimulation induced
release of [3H]-noradrenaline and 50 ng/ml fluoxetine, a
selective inhibitor of the uptake of serotonin, did not change
the release of [3H]-serotonin. Neither 250 ng/ml clorgyline,
a selective inhibitor of MAO-A, nor 250 ng/ml lazabemide,
a selective inhibitor MAO-B, was capable to significantly
increase the nerve stimulation induced release of either [3H]-
serotonin or [3H]-noradrenaline. The potent dopamine
receptor agonists, pergolide and bromocriptine, did not
change significantly the release of [3H]-dopamine in 50 ng/
ml concentration, which is sufficient to stimulate the
dopamine receptors. Thus the results proved that stimulation
of catecholaminergic and serotonergic neurons in the brain
via the enhancing mechanism is clearly different from
influencing uptake or MAO (Miklya and Knoll, 2003).
The subcutaneous administration of 1 mg/kg tetrabenazine,
once daily for 5 days, which depletes the catecholamine
stores in the brain, significantly inhibits in rats the
acquisition of a two-way conditioned avoidance reflex in
the shuttle box. Enhancer substances antagonize, in a
dose-dependent manner, the inhibition of learning caused
by tetrabenazine. The tryptamine-derived selective and
highly potent enhancer, ()-BPAP acted in dose range
from 0.05 to 10 mg/kg. The PEA-derived enhancer
substances, ()-deprenyl and ()-PPAP were much less
active (1–5 mg/kg). 1-(Benzofuran-2-yl)-2-(3,3,3-trifluoropropyl)-
aminopentane HCl [3-F-BPAP], a newly synthetized
analogue of ()-BPAP with low specific activity,
significantly antagonized the enhancer effect of ()-BPAP
but left the effect of ()-deprenyl and ()-PPAP
unchanged. This was the first proof for a difference in
the mechanism of action between a PEA-derived enhancer
substance and its tryptamine-derived peer (Knoll et al.,
2002a).
()-BPAP enhanced the performance of midbrain neurons,
both in vivo and ex vivo, in a characteristic bi-modal
manner, presenting one bell shape dose/concentration effect
curve in the low nanomolar range and another at higher
micromolar range. For example, 4.7 T0.10 nmol/g wet
weight noradrenaline was released within 20 min from the
quickly removed locus coeruleus of saline treated rats. This
amount was increased 30 min after the subcutaneous
administration of 0.0005 mg/kg ()-BPAP to 15.4 T0.55
nmol/g (P <0.001). However, following the injection of a
hundred times higher, 0.05 mg/kg dose of ()-BPAP, the
amount of noradrenaline (4.3T0.25 nmol/g) released from
the locus coeruleus did not differ from the control value. In
ex vivo experiments, when the isolated locus coeruleus was
soaked in an organ bath containing ()-BPAP, the release of
noradrenaline was significantly enhanced from 1016 M
concentration, reached a peak effect at 1013 M concentration,
but 1010 M ()-BPAP was ineffective. A
significant enhancer effect was detected also in the high
concentration range from 108 M, the peak effect was
reached at 106 M concentration and 105 M ()-BPAP
was ineffective. ()-BPAP enhanced in the low concentration
range the performance of dopaminergic and serotonergic
neurons with a peak effect at 1013 and 1012 M
concentration, respectively (Knoll et al., 2002b). The
authors concluded that (i) high and low affinity Fenhancer_
receptors exist in the brain, and (ii) that they may be
identified with the recently cloned family of the Ftrace
amine_ receptors, activated by PEA and tryptamine, the
prototypes of the endogenous enhancer substances (Borowsky
et al., 2001).

#89 psy333che

  • Guest
  • 55 posts
  • 1
  • Location:North East

Posted 28 April 2009 - 01:42 PM

Everything I know of this drug is that it is helpful with Parkinson's disease and most research is about that.. I would be interested in trying it myself if you have found such good results
I am wondering if anyone else has............. I am also interested in where you order it... or if you have gotten it as a RX

http://www.sciencema...ct/245/4917/519

"The effect of deprenyl (selegiline) on the natural history of Parkinson's disease"
JW Tetrud and JW Langston

California Parkinson's Foundation, San Jose 95128.

The effects of MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine), a neurotoxin that produces the symptoms of Parkinson's disease, can be fully prevented in experimental animals by inhibiting monoamine oxidase B. On the basis of this observation, a double-blind, placebo-controlled study in patients with early Parkinson's disease was initiated to determine whether deprenyl (a selective monoamine oxidase B inhibitor) would delay the need for L-dopa therapy by slowing the progression of the disease. Fifty-four patients were randomly assigned to deprenyl (10 mg/day) or placebo treatment groups and followed until L-dopa therapy was indicated or until the patient had been in the study for 3 years. Analysis of Kaplan-Meier survival curves for each group showed that deprenyl delayed the need for L-dopa therapy; the average time until L-dopa was needed was 312.1 days for patients in the placebo group and 548.9 days for patients in the deprenyl group. Disease progression, as monitored by five different assessment scales, was slowed (by 40 to 83% per year) in the deprenyl group compared to placebo. Therefore, early deprenyl therapy delays the requirement for antiparkinsonian medication, possibly by slowing progression of the disease.
and.............................
http://www3.intersci...l...=1&SRETRY=0
"Brief Communication
"Deprenyl suppresses the oxidant stress associated with increased dopamine turnover"
Dr Gerald Cohen, PhD *, Mary Beth Spina, PhD
Department of Neurology and Graduate School in Biomedical Sciences, Mount Sinai School of Medicine of the City University of New York, New York, NY

*Correspondence to Gerald Cohen, Department of Neurology (Box 1137), Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029

Abstract
Tissue glutathione disulfide (GSSG) was studied as an index of changes in redox state in the striatum. When increased turnover of dopamine was provoked in mice by injection of haloperidol (1 mg/kg), the concentration of GSSG in the striatum tripled. Deprenyl (2.5 mg/kg) suppressed the rise in GSSG by 71.9%. These results indicate that deprenyl suppresses an oxidant stress associated with increased dopamine turnover.

This was an interesting artiv=cle I found you may want to check out............
Deprenyl is metabolized to methamphetamine and amphetamine in man.
G P Reynolds, J D Elsworth, K Blau, M Sandler, A J Lees, and G M Stern

http://www.pubmedcen...i?artid=1429688



I recently picked up some deprenyl and I am very happy with it. I have tried various nootropics before including piracetam, aniracetam, ortho mind, and vinpocetin. I never had any luck with these nootropics but with deprenyl I finally get positive results. I am more focused and sharper. I am not affected by brain fog and it is easier to motivate me. Are there any bad consequences of supplementing with this daily? If so what can I do to minimize the negative effects?



sponsored ad

  • Advert
Click HERE to rent this advertising spot for BRAIN HEALTH to support LongeCity (this will replace the google ad above).

#90 blazewind

  • Member
  • 77 posts
  • 7
  • Location:USA

Posted 28 April 2009 - 03:53 PM

Another thing yowza, this report is why I think selegiline is important for the drug combination holy grail







http://www.bluelight...hic#post3983391

"I'll chip in my 2c. I've taken several courses of selegiline. You do get a mild amphetamine effect in the first few days / week, but that tends to wear off. When I say mild, I do mean mild.

After about 2.5 weeks of selgiline (and NOT drinking -- this is important), something truly hectic happens to my memory. My memory slowly improve for 2.5 weeks or so, but overnight my memory becomes essentially eidetic/photographic.

Now when I say this, I mean I can memorise enormous quantities of information with essentially zero trouble.

For example: I memorised 212 pages of statistical physics notes in two days, and got 97% on the exam. I memorised 180 pages of notes on theoretical quantum mechanics in two and a bit days and got 98% on the exam.

The effect ceases within a few days of stopping the selegiline, and is (interestingly) destroyed by drinking. I went out and had half a bottle of wine one night, and the effect vanished for 3 days, then returned.

I have a good memory normally, and am intelligent, but this sort of feat is not within my grasp.

Perhaps even more interestingly I have the memory without the perception of having learned the material. I don't have the feeling that I know any of it, but when I go to write it down it's all there, with 100% accuracy.

I don't take it for any depression/other psychoaffective disorder.

My girlfriend has also found the same thing, though it takes her just over 3 weeks for the effects to appear.

I realise that this could be some sort of placebo effect, but if it is, it's stronger than anything else I've ever encountered. I never expected it the first time it happened either.

I've never encountered such a memory effect from any other nootropic drug either. "



http://www.bluelight...tam#post2065071


"I'm coming up to my exams now and I have to say I think my nootropic splurge has been worth it...

in the last two days I've managed to learn and memorise the best part of 160 pages of statistical physics... admittedly i'm not memorising anything word for word, but there's a lot of derivations with a lot of finicky steps that are quite confusing.. Two days before that I revised a similar amount of quantum mechanics, and I appear to have retained *most* of it.

I should have learnt this subject right from the start, but the lecturer was pretty poor and I hate anything involving statistics...

re Selegiline
It's rather weird. You know the feeling when you know something? When someone asks you a question and you know you know the answer to it? You feel confident in your knowledge? I don't have that feeling. To be honest I feel like I know very little, but then when i actually go to do it I remember huge slabs of it... it's rather odd.

I've been taking 5mg/day of selegiline about 15 mins after breakfast (two pieces of toast, milk, vita brits).... I spread promite on my toast (high in tyramine) and have experienced nothing remotely resembling a hypertensive crisis... no headaches, sweating, dizziness etc.

500mg l-phenylalanine seems to work, 1g seems to work better.... I don't really feel that selegiline gives a "clear-headed" feeling so much... I've still been using caffeine tablets where appropriate etc.

I have noticed that in darker rooms my pupils are larger than they normally would be. Not completely dilated, but still quite large. At night I get substantial halos (white-blue) around street lights, and around other lights. Looking at bright nights in the street at night I get a mild version of the "overexposed" look that you get from pills, where there's this pure white in the centre.

I had hoped that selegiline might do something for my tiredness, but alas it has not. The first day I took it I noticed a stimulant effect, but it declined thereafter (even with phenylalanine).

Summary: I found selegiline to be a useful adjunct to piracetam + choline supplementation. It's not some miracle drug that bestows an infinite learning capacity, but it does seem to work.

Comments re Hydergine
I'm not sure what hydergine has done in this mix... I've only take it some days, and I noticed that on some of those days I felt somewhat tired... I was awake, but my brain felt sluggish. I cannot say whether this is the Hydergine or merely some uncorrelated effect from my sleeping hours or caffeine withdrawl etc, but I do have to say its odd. I used it today and felt more clearheaded... used it yesterday and felt somewhat dull.

I may try this again in future, though I can't say when.

Now its over?
My main concern now that I'm about to stop the selegiline is when I can next do pills, to be honest... The best studies I can find put the mean time to plasma MAO-B return at around 240ish hours, up to 300 in people who have been taking it for multiple months... I'll keep taking phenylalanine for the next week or two and observe what happens to my eyes. I intend to leave at least 8 or 9 days between now and taking pills, and will see how I go in the meantime."



http://www.bluelight...tam#post3167044

"Vinpocetine is a well-researched, safe, cerebral vasodilator and antioxidant. It's derived from vincamine. I've tried it before, and there appears to be *some* result, but to be honest I think piracetam is superior. Everyone gets different results, though...

I've found fantastic results for exams with the following:
4g piracetam per day (2g morning, 2g evening)
4g choline (2g morning, 2g evening)
5mg selegiline
1000mg phenylalanine (500mg morning, 500mg evening)
10 fish oil tablets (~3g omega-6)

After about a week or two my memory starts becomng almost photographic. I can memorise enormous volumes of information with relative ease.... For example, I didn't really go to statistical physics for most of the semester, and in 3 days managed to learn around 130 pages of notes... Ended up getting 91 in the subject.

My thoughts were much clearer too"


also:
http://www.bluelight...earchid=3868015




============================================================


I actually tried doing that same combination listed above 6 months ago for 1 month, and then switched to 8g piracetam, 2g aniracetam, 2g oxiracetam, 500mg alpha gpc, 500mg cdp choline for a month and still didn't get this effect combined with selegiline.

Maybe a stronger racetam like noopept or nefiracetam could enhance the effect more than piracetam.
And then maybe the CAE is the key instead of MAO-B, in which BPAP would be more effective.




32 user(s) are reading this topic

0 members, 32 guests, 0 anonymous users