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Synthetic Cannabinoid Drugs

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Slaughterhousefive42

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Mar 31, 2003
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This is going towards the neuroscience gurus in here. Anyone have an idea what kind of cognitive effect these drugs have: the endocannabinoid reuptake inhibitors like AM404, CB antagonist rimonabant, and/or agonists such as WIN 55,212-2. And how they work.

Basically I'm asking if these drugs produce noticeable changes in consciousness if taken alone, not if they cause chemical changes in rats. Long term, short term effects...any information about their effect on consciousness.
Come on Bilz0r...
 
Uptake inhibitors definatly cause effects... the antagonists don't seem to have much an effect when given acutely..

In Rang Dale and Ritter: Pharmacology, he claime that SR141716 INCREASED short term memory... Perhaps there is a animal study backing this up, I don't know..

Meanwhile, if you get access the the SR141716 (Acomplia) Phase I-III trial information, you're the only person outside of Sanofia-Aventis to see it.

I don't quite get why your discounting rat info here... so there's not much I can tell you.
 
I'm not discounting rat info. I work with ratties in a neuroscience lab (and around the dumpster behind my house). I was curious if any of the synthetic cannabinoids had abuse potential like THC. Would the uptake inhibitors induce a high like THC? Cocaine roughly induces a shorter version of the amphetamine high, by inhibiting the reuptake of catecholamines (esp dopamine). Since Am404 inhibits the reuptake of endocannabinoids, does it induce a shorter THC-like high?

So no one has taken accomplia or AM404? I assumed so but I was hoping someone had stumbled into a bit.
 
The slightly more water soluble cannabinoids, with shorter half-lives, should be more abusable... perhaps even addictive.

I don't know if it would be fair to compare the different between a dopamine reuptake inhibitor and a dopamine agonist to the difference between a cannabinoid reuptake inhibitor and a cannabinoids agonist... even if amphetamine was a dopamine agonist.
 
I've no fucking idea.
It's an indirect agonist though.
 
It is indirect but isn't it also a direct agonist... look at how similar the chemical structure of amphetamine and dopamine are...dopamine just has those two alcohol groups which ensure quick enzymatic degradation
 
Not to my knowledge, not at any relavent physiological concentrations at least. Not according to the only reference I can find on the subject-
BURT, D.R., CREESE, I., and SNYDER, S.H.
Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes.
Mol. Pharmacol. 12: 800-812 (1976).
 
In my lab and in the literature I have read they have used amphetamine to produce psychosis through hyperdopaminergic activity. Using this model of psychosis they test various dopamine antagonists/partial agonists for their ability to reduce psychosis.
 
Well it does produce hyperdopaminergic activity. Nothing to do with it being an agonist though.
 
hmm...we must have different definitions for agonist then. Would it be fair to say amphetamine agonizes the dopaminergic systems, esp the mesolimbic and nigrostriatal pathways?
 
^ Might as well...

An agonist is something that binds to and stimulates a receptor (or only binds to it in its active conformation)... I wouldn't saying amphetamine agonizes the dopaminergic system, because you can't bind to and activate a system, I might say it stimulates that system, but I don't really like talking about systems either, what I'd prefer to say is that it is an indirect dopaminergic agonist.
 
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Does anybody either have a pic of the structure or the IUPAC name of a synthetic cannabioid that contains nitrogen in the same position asd the structure given below (I don't think it's correct, I just used it to illustrate where the nitrogen is substituted into the molecoue - where the double bond occurs)

59655nitrogen_THC_analogue.JPG



I think it was a product of McNeil labs (McN xxxxx), and was an agonist that formed water soluble salts. I've tried finding it with google; it lists papers concerning research with THC nitrogen analogues, but none actually give the structure or IUPAC name)

Thanks
 
Its neither of those... I can't actually find what the chem is, but the IUPAC name of that compound, by my figuring is:
3,10,10-Trimethyl-7-pentyl-2,3,4,4a,10,10a-hexahydro-1H-9-oxa-3-aza-phenanthren-5-ol, which doesn't turn up any hits on google...
 
Blowmonkey

Thanks, but it's not either of them as CP 55,490 doesn't contain a nitrogen and O-1057 has the morpholine group attached to the end of butyric acid, which is esterified with the free OH group on the benzene ring


BilZ0r

I can't remember what the alkyl chain is that's attached to the benzene ring. I just put up the structure to show where abouts the nitrogen is substituted into the THC molecule (the 9 position). Thanks for trying

I'll try using a metasearch engine to see if I can track it down. I know that it's a CB1 agonist, but other than that, my memory is a bit sketchy about the rest of the structure. Also the medline abstracts aren't very forthcoming on the IUPAC names of the compounds used, just that they are "nitrogen containing THC derivatives".
 
that was a good question actually. you guys got sidetracked on the DA / amphetamine mechanism stuff though. anyone know what difference there is in potency etc.?
i heard THC is a partial agonist or has some more complex mechanism than just agonist. is that right?
 
Well from my modest understanding of the situation, it depends.

If you get in vitro, things get simple, and 9 time outa 10, THC is a full agonist... But, anandamide is more efficacious than D9-THC in producing catalepsy, but it was only a partial agonist for reducing body temperature in comparison to D9-THC...

More agonist directed trafficking me thinks.

Smith PB, Compton DR, Welch SP, Razdan RK, Mechoulam R and Martin BR (1994) The pharmacological activity of anandamide, a putative endogenous cannabinoid, in mice. J Pharmacol Exp Ther 270: 219-227
 
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