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basis for new types of stimulants?

It's funny you should mention epibatidine analogs Vecktor, as I am at Abbott right now being a guineapig for such a compound(not sure ABT-272 i believe). However what do you refer to as having abuse potential? These compounds were created because epibatidine is 1000x the analgesic potency of morphine without being an anesthetic(no nodding, no euphoria at all)and obviosly no WDs. Poison dart frog venom, while it may have "intoxicating effects", is VERY unpleasant. I don't see nicotonic agonists or antagonists as pleasant drugs, unless there's a specific medical need, leave those receptors alone.
 
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glenjih said:
Also, this has me confused:

"Tobacco smoke contains the monoamine oxidase inhibitors harman, norharman,[20] anabasine, anatabine, and nornicotine. These compounds significantly decrease MAO activity in smokers.[20][21] MAO enzymes break down monoaminergic neurotransmitters such as dopamine, norepinephrine, and serotonin."

Does this mean that inhibiting MAO enzymes causes those neurotransmitters to hang around for longer? Potentially increasing euphoria?
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Nicotine, in itself, is not as addictive as smoking cigarettes are.
 
If you're asking why he says that, it's documented in several studies. As to why it happens...

The nicotinic acetylcholine receptor appears to be related to the process of addiction, not just to nicotine but to other substances as well. The combination of cocaine and nicotine is more addictive than cocaine alone.

So, the combination of nicotine and harman may be causing an addiction to harman, weird as it sounds.

http://www.nature.com/nm/journal/v8/n5/full/nm0502-447.html
 
The nootropic effects of tobacco are due to nicotine's primary metabolite, cotinine (2-oxo-nicotine), a racetam [and anagram of 'nicotine.'] Cotinine has a much longer half life in vivo than nicotine.

Also, there are a handful of drugs in the pipeline (or there were a year or two ago, when I read the article here) which target nicotine receptors and are being developed for the treatment of schizophrenia. This novel class of antipsychotics was looked into by big pharma because nicotine is known to alleviate certain symptoms of schizophrenia at the clinical level.

Also, the type of tobacco in use today has been bred to have much, much lower levels of nicotine than what the native americans were smoking when the white settlers arrived. That type of tobacco smoking regularly induced strong CNS effects such as hallucinations.
 
I have had doses of nicotine far higher than in a cigarette in the form of a tobacco tea, and while there was certainly a much more pronounced effect the negative effects seemed far more amplified, while positive effects, while lasting longer were no different, so i am curious as to what causes CNS effects like hallucinations at high doses?
 
According to the history book that I read, there were alkaloids other than nicotine which were responsible for the hallucinations, but since this happened a couple of hundred years ago there is no way to be certain. GC/MS, NMR, FTIR and HPLC technology came along much later.

I think it's a shame we don't have any of the hallucinogenic tobacco cultivars left to sample, test, and assay. So, basically, who knows?

(The name of the book btw is Seeds of Wealth: Five Plants That Made Men Rich by Henry Hobhouse.)
 
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I've had doses of nicotine high enough to make me sweat and vomit uncontrollably... and it doesn't make you hallucinate; there was a sort of trance-ish state that lasted maybe twenty minutes.

I imagine nicotine's nootropic effect might make ayahuasca more interesting?
 
(zonk) said:
What I meant when I said waste of time is that the ridiculous amount of time, work, and $ put into trying to discover a stimulant with a nicotine molecule as a base(which may not even b possible)seems totally pointless when there r so many other easier more logical bases for stims out there.
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Even a remote chance of discovering something cool ought to be enough to justify exploring a particular avenue of research. The opposite attitude leads to stagnancy, which has been shown over and over in the historic pursuit of scientific knowledge. Don't you think most of the low hanging fruit in classical stims has probably already been picked?
 
I just can't see any benefit/payoff. What if one were to discover a nicotine based stimulant, then what? What uses would it have? But perhaps I am being short sited and there's something i'm not seeing as a benefit but my gut tells me that trying to make something which seems utterly toxic/useless to me except in myabe treating schizofrenia, is not the best way to spend alot of time. I could b wrong tho
 
Is this thread about nicotine analogues or nicotinic receptor ligands? And are you sure you want full agonists? A lot of these are poisons.

<pyridinyl_30> said:
Also, there are a handful of drugs in the pipeline (or there were a year or two ago, when I read the article here) which target nicotine receptors and are being developed for the treatment of schizophrenia. This novel class of antipsychotics was looked into by big pharma because nicotine is known to alleviate certain symptoms of schizophrenia at the clinical level.
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There still are. Ispronicline for example (not a nicotine analogue), a partial agonist selective for the a4b2 subtype. I haven't read the literature but I suspect the efficacy has more to do with counteracting the anticholinergic side effects of typical/atypical antipsychotics than with any particular aspect of the schizophrenic disease process. Ever been around schizophrenics? They smoke like chiefs when they're on their meds.
 
The benefit is, at the least, an enhanced understanding of pharmacology. You learn something important regardless of the results, and you might even see immediate, tangible benefits.
 
acetylcholine plays a vital role in schizophrenia, and indeed at high doses many anticholergens induce temporary schizophrenia. So likely nicotines cholergen effect is what is makes it useful in battling mental illness. Yes, the original idea of the thread was to see if nicotine could be altered to make more recreationally valuable drugs, i am curious (Zonk) as to what platforms you think are more viable for the basis of stimulants, I think amphetamines and most other current platforms have been fairly well documented already, and I have not yet come across any novel bases for a new class of stimulants
 
there are hundreds of possibilities, wiki of course has quite a few. But this area doesn't particularly interest me much and i haven't looked into it all that much either. If they can be made into empathogens/entactogen well then... now yer speaking my language. But so far only arylalkylamines seem to fit that criteria AFAIK.
 
(zonk) said:
If they can be made into empathogens/entactogen well then... now yer speaking my language. But so far only arylalkylamines seem to fit that criteria AFAIK.
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http://en.wikipedia.org/wiki/WAY-267,464
http://en.wikipedia.org/wiki/Eltoprazine
http://en.wikipedia.org/wiki/Indeloxazine

I have to wonder if the phenethylamines are the right place to look for new entactogens. MDMA appears to be the best thing that the phens have to offer, with only methylone coming close. MDA is a fun drug but really a rather different thing. Perhaps beta-methoxy MDMA will do something interesting.

The tryptamines might work a little better. AET seems like a good place to start. The reports on erowid seem to say it suffers some of the same issues as the MDEA/MDA/etc, but AET analogs are an entirely unexplored area pharmacologically.
 
when I say arylalkylamines I was also refering to tryptamines as well:). There's the 5-indol analog of amt that is a stimulant so what about a 3,5-di-indol. There's alot that can be played around with there. I think tryptamines are a very under studied type of class
 
ya i have to agree that empathogens are a lot more interesting than run of the mill stimulants, i was just looking up nicotine one day, and noticed that it effected receptors which could result in a much more interesting drug then the base and I was wondering if anybody had done this, or thought it was feasible. Is it just oxytocin release which is responsible for empathogen effects or are other neurotransmitters/hormones involved?
 
[quote\Quote:
Originally Posted by seep View Post
Ever been around schizophrenics? They smoke like chiefs when they're on their meds.
yes mental institutions often have people who smoke huge amounts, seems to add up [/quote\

Well it might just be boredom.. got nothing to do in there for however long.

I'd love to try phenmetrazine, or some analog of that, i hear its like amphetamine but way cleaner.. too bad its hard to find. Analogs would probably not fall under analog acts and such.
 
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