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Rimonabant-Cannabinoid receptor antagonist?

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Dr. McBudstoke

Ex-Bluelighter
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Mar 5, 2004
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Rimonabant

This is merely a theoretical question, seeing as the drug is still pending FDA approval. Rimonabant blocks cannabinoid receptors in the brain, thus eliminating hunger(Weight-loss is the main purpose of the drug). Would using this drug also make it impossible to get high? Could it be the first developed cannabinoid antagonist?

If so, this could become the suboxone/noloxone of marijuana.

Here is an exerpt from the article:

Its planned brand name -- pending FDA approval -- is Acomplia. For now, it's still going by its generic name rimonabant. But it already has a nickname: the munchies drug. That's because it works like marijuana in reverse. It blocks cannabinoid receptors in the brain.
 
http://www.ncbi.nlm.nih.gov/entrez/...ve&db=pubmed&dopt=Abstract&list_uids=15134279
Cannabinoid receptor antagonists and obesity.

Black SC.

Cardiovascular and Metabolic Diseases, MS 8220-3119, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA.

The cannabinoid-1 (CB1) receptor plays a role in the regulation of appetitive behavior. Exogenously administered cannabinoid receptor agonists stimulate food consumption in animals and humans. Endogenous cannabinoid receptor agonists are present in the brain, and the brain level of these agonists increases with greater demand of food by rodents. Specific CB1 receptor antagonist compounds have been discovered that display high affinity and selectivity for the CB1 receptor. CB1 receptor antagonists inhibit both acute and long-term food intake in rodents. Chronic treatment with CB1 antagonists results in a sustained reduction in body weight in rodents (5 weeks), and weight loss in humans (16 weeks). Patent literature indicates CB1 receptor antagonist discovery efforts at a number of pharmaceutical companies. The CB1 receptor antagonist, rimonabant (SR-141716), discovered by Sanofi-Synthelabo, is in phase III clinical trials for the treatment of obesity and has been found to decrease appetite and body weight in humans.


Seems like it isn't the first, just the first to go through clinical trials. I have no idea if it will reduce the high, probably will, but who am I to tell..
 
^ do you know if it's anandamide that stimulates hunger through the endocannabinoid system when no exogenous cannabinoids are administered?
 
As far as I know, anandamide is the main endogenous analogue of THC, that is, it's the neurotranmitter that THC mimics in the brain. I've even heard the cannabinoid receptors referred to as anandamide receptors.
 
Surely, the feeling of hunger has more to do with just the endogenous anandamide/cannabinoid receptrs in the brain..
 
Dr. McBudstoke said:
^ do you know if it's anandamide that stimulates hunger through the endocannabinoid system when no exogenous cannabinoids are administered?
Click to expand...

Oh and yes, it does. That article really exaplains it all. :)
 
Rimonabant (SR 141716a) wouldn't STOP you getting high, it would just mean you'd need fuck loads more weed.
 
A while I'd geuss.. though Phase III clinical trials were going on late 2003... maybe the end of this year... I don't know.
 
Sampling the panoply of PubMed abstracts leads me to predict this is only the tip of the iceberg when it comes to synthetic cannabinoid drugs being commercially pushed by big pharma. Hopefully rimonabant (SR141716a) proves to be the wonder drug it seemed in clinical trials: reduction in reward-motivated behavior (food, drug- esp nicotine and THC), increased "good" HDL, and weight loss. Finally the pharm companies spending billions on R&D wise up to a mechanism known to marijuana smokers for millenia- the munchies (caused by THC- a naturally available cannabinoid agonist). There are many other potential avenues and molecules, AM404- a sort of Prozac for cannabinoids-inhibiting the reuptake, cannabinoid receptor agonist WIN55212-2, artial agonist without inverse agonistic activity, O-1184 ... etc etc. Once cannabinoid research becomes even more accepted in the popular scientific press, it will eventually spill over to the public and fuel interest in the endocannabinoid system. I see the rise of cannabinoid drugs mirroring the end of the ridiculous prohibition of cannabis.
I'm a first time poster, long time reader by the way, this topic happens to be in the area of my so-called expertise (neurobio).
 
I strongly doubt that Rimonbant will be that useful clinically, but thats just my opinion at the moment. Also, cannabinoid research is highly palatable to the scientific press, infact, I can hardly think of things they like to publish more, as far as simple receptor-action pharmacology goes.
 
What is your basis for your unenthusiastic opinion concerning rimonabant? Cannabinoid research is also being focused on ligand-independent effects, esp. manipulating non-CB receptors. As far as simple receptor-action pharmacology, research has shown would say cannabinoids rely greatly on retrograde signaling for other NT systems more than actual allosteric or direct antagonistic effects. Simplifying the complex endocannabinoid systems into simple receptor-action pharmacology has little actual biological importance other than determining pharmacological data for specific ligands. Cannabinoid research might be highly palatable to the international scientific press, as a majority of the abstracts published on PubMed on this topic are international. However, I guess I was alluding to the limited US arena in which the political drug war overshadows and limits research into even non-recreational cannabinoids.
 
It is important to examine the possible negative effects of long term admin of CB antagonists such as SR141716. Yet the preliminary clinical results thus far seem more promising than any other obesity drug in testing, and appear to lack any serious side effects. There is no question Rimonabant (if it passes the FDA's red tape without safety concerns) has the potential to be a life-saving drug, particularly its potential role in tobacco cessation or improving cardiovascular health. Smoking and obesity are number one and two killers in the US, as the media constantly asserts. Doctors around the country will jump at this novel pharmacological challenge to these two societal ills.
 
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