O-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

Authors
MACOR JE BLANK DH DESAI K FOX CB KOE BK LEBEL LA POST RJ SCHMIDT AW SCHULZ DW SEYMOUR PA
Citation
Je. Macor et al., O-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, Bioorganic & medicinal chemistry letters, 5(20), 1995, pp. 2391-2396
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
20
Year of publication
1995
Pages
2391 - 2396
Database
ISI
SICI code
0960-894X(1995)5:20<2391:OB(>2.0.ZU;2-X
Abstract
The discovery of CP-161,242 pyrrolidin-2R-ylmethyl)indol-5-yl]benz-imi dazole), a potent, selective, orally active central serotonin (5-HT1D) agonist [IC50 (binding) = 1.3 nM, EC(50) (inhibition of adenylate cyc lase) = 42 pM] and benzodiazepine ligand [IC50 (binding) = 3.3 nM], is presented.