Article
Position 5.46 of the serotonin 5-HT2A receptor contributes to a species-dependent variation for the 5-HT2C agonist (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one: impact on selectivity and toxicological evaluation.
Molecular pharmacology - 1 Dec 2009
Miller Keith J, Wu Ginger Y, Varnes Jeffrey G, Levesque Paul, Li Julia, Li Danshi, Robl Jeffrey A, Rossi Karen A, Wacker Dean A
Abstract excerpt
Successful development of 5-HT(2C) agonists requires selectivity versus the highly homologous 5-HT(2A) receptor, because agonism at this receptor can result in significant adverse events. (R)-9-Ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one (compound 1) is a potent 5-HT(2C) agonist exhibiting selectivity over the human 5-HT(2A) receptor. Evaluation of the compound at the rat...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.