Title of article :
5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist
Author/Authors :
John E. Macor، نويسنده , , David H. Blank، نويسنده , , Kishor Desai، نويسنده , , Carol B. Fox، نويسنده , , B. Kenneth Koe، نويسنده , , Lorraine A. Lebel، نويسنده , , Ronald J. Post، نويسنده , , Anne W. Schmidt، نويسنده , , David W. Schulz، نويسنده , , Patricia A. Seymour، نويسنده ,
Abstract :
The discovery of CP-161,242 (5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl]benzimidazole), a potent, selective, orally active central serotonin (5-HT1D) agonist [IC50 (binding) = 1.3 nM, EC50 (inhibition of adenylate cyclase) = 42 pM] and benzodiazepine ligand [IC50 (binding) = 3.3 nM], is presented.
