Article
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction.
Journal of medicinal chemistry - 5 Oct 2006
Hurst Dow, Umejiego Uju, Lynch Diane, Seltzman Herbert, Hyatt Steven, Roche Michael, McAllister Sean, Fleischer Daniel, Kapur Ankur, Abood Mary, Shi Shanping, Jones Jannie, Lewis Deborah, Reggio Patricia
Abstract excerpt
The biarylpyrazole, N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716; 1) has been shown to act as an inverse agonist/antagonist at the cannabinoid CB1 receptor. Our previous mutant cycle study suggested that K3.28(192) is involved in a direct interaction with the C-3 substituent of 1 in wild-type (WT) CB1.(1) However, these results did not establish what...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.