The development of cannabinoid antagonists.


Current medicinal chemistry, 6(8), 745-55 (1999) .


The discovery of two distinct cannabinoid receptors (CB1 and CB2) in the early 1990’s has revived the research on cannabinoid antagonists. While the search for antagonists based on the structure of agonists (classical cannabinoids or aminoalkylindoles) appeared rather disappointing, the first potent cannabinoid antagonists were developed in a new chemical series: the diarylpyrazoles. Since its discovery in 1994, the selective CB1 antagonist SR 141716 has became a major pharmacological tool to elucidate the physiological role of the CB1 cannabinoid receptor and its endogenous ligand. The selective CB2 antagonist SR 144528 is expected to play the same role for the CB2 receptors, while the recent development of cannabinoid antagonists belonging to other chemical series illustrates the interest of these compounds which are now considered as interesting therapeutic targets by many pharmaceutical companies.

Add your rating and review

If all scientific publications that you have read were ranked according to their scientific quality and importance from 0% (worst) to 100% (best), where would you place this publication? Please rate by selecting a range.

0% - 100%

This publication ranks between % and % of publications that I have read in terms of scientific quality and importance.

Keep my rating and review anonymous
Show publicly that I gave the rating and I wrote the review