title: Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists.
abstract: A novel series of indolyl and dihydroindolyl glycinamides were identified as potent NPY5 antagonists with in vivo activity from screen hit 1. The dihydroindolyl glycinamide 10a significantly inhibits NPY5 agonist induced feeding at a dose of 0.1 mg/kg. The indolyl glycinamide 12c also inhibits NPY5 agonist induced feeding at a dose of 1 mg/kg. Both compounds 10a and 12c represent potential tools for further investigation into the biology of the NPY5 receptor.
authors.affiliation: Chemical & Pharmacokinetic Sciences, Paramus, NJ 07652, USA. wuly2000@yahoo.com
authors.forename: Lingyun
authors.initials: L
authors.lastname: Wu
authors.forename: Kai
authors.initials: K
authors.lastname: Lu
authors.forename: Mathivanan
authors.initials: M
authors.lastname: Packiarajan
authors.forename: Vrej
authors.initials: V
authors.lastname: Jubian
authors.forename: Gamini
authors.initials: G
authors.lastname: Chandrasena
authors.forename: Toni C
authors.initials: TC
authors.lastname: Wolinsky
authors.forename: Mary W
authors.initials: MW
authors.lastname: Walker
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D019167:Appetite Stimulants / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D001921:Brain / Q000187:drug effects; D002460:Cell Line; D004435:Eating / Q000187:drug effects; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D015394:Molecular Structure; D010539:Permeability; D051381:Rats; D017207:Rats, Sprague-Dawley; D017476:Receptors, Neuropeptide Y / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D019167:Appetite Stimulants; D007211:Indoles; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; D005998:Glycine