Rimonabant, cannabinoid inverse agonist / active antagonist.

[Nagelfar]

Has anybody tried this or any similar type drug? I'm sure a non-fan of the cannabinoid class of drugs I always thought I'd actually *like* a potential inverse-agonist. Wonder if it increases your short term memory at all like a nootropic.

 

[sekio]

Has anybody tried this

It was marketed as a weight loss/smoking cessation aid, until the FDA realized that it had the small problem of making people miserable, depressed, and suicidal.

Mr. Morris took some and wrote his experiences.

 

[Nagelfar]

It was marketed as a weight loss/smoking cessation aid, until the FDA realized that it had the small problem of making people miserable, depressed, and suicidal.

Mr. Morris took some and wrote his experiences.

Somehow, I still think I'd *like* it. ;-j

 

[Nagelfar]

if you want to experiment in a more natural route you could try CBD, that also is an inverse agonist for CB1, it is also an antagonist at the putative new cannabinoid receptor, GPR55.
As far as Rimonabant goes I think it has the most potential as a medicine in ER setting when patients have OD's on synth cans.

Interesting, I just looked up "Abnormal cannabidiol (abn-cbd)" from that novel receptor link at WP. Therein the structure given reminds me of (cross-over yet again! [cf. other recent threads]) fitting in close quarters with various kinds of MAT stimulant type drugs.

 

[sekio]

GC/MS tested to be free of bacterias and heavy metals

GCMS can't test for either of these.

CBD/THC are antibacterials so I wouldn't be concerned about it, but you'd need to have something like atomic absorption spectroscopy to test for metals.

 

[endotropic]

Rimonabant also acts as a fairly potent mu-opioid antagonist: http://www.ncbi.nlm.nih.gov/pubmed/22771770

I wonder how much that action contributes to the negative psychological side effects? A more selective CB1 antagonist might not be as bad.

 

[Nagelfar]

Rimonabant also acts as a fairly potent mu-opioid antagonist: http://www.ncbi.nlm.nih.gov/pubmed/22771770

There you have it..!! *That's* the culprit..!! ;-j

An opioid antagonist (a la Narcan/Naloxone & Naltrexone; which are used in a similar way to disulfiram for alcoholics, even; so the popular myth that they do not have an effect on non-opioid users is misdirected) surely must be what causes (and is a known cause of) the dysphoria alluded to. Now one that isn't an opioid antagonist, but simply a selective CB1 antagonist, as endotropic noted just prior to me here, would be indeed the true litmus test for the drug-type.

 

[sekio]

So is rimonabant then a promising lead compound for debelopment of a dual mu-CB1 agonist ? Sounds like a fun class to explore to me!

 

[Dresden]

Sure, if you want to suffer extreme irritability and depression, take a THC antagonist such as rimonabant.

 

[serotonin2A]

I don't think rimonabant is a THC antagonist, really nothing to my knowledge is, THC is a naturally occurring cannabinoid that has no such receptors to be antagonized, while the brain has CB1 and CB2 receptors that can be affected by antagonist and inverse agonist.

THC binds to CB1 and so does rimonabant, so they compete for the same receptor. People who take rimonabant do not experience any effects from THC. That makes rimonabant a THC antagonist.

 

[Nexus_Tripper]

Maybe it would help reverse marihuana overdoses.

 

[Nagelfar]

Maybe it would help reverse marihuana overdoses.

Paranoia issues, yes exactly, that's it.