title: N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists.
abstract: A series of benzamides was synthesized as selective agonists for the 5-HT1A receptor. It was found that (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarb oxamide(7-(S)) has potent and selective agonistic activity for the 5-HT1A receptor (5-HT1A; Ki 0.49 nmol/L, D2; IC50 = >1000 nmol/L, 5-HT2; Ki = 240 nmol/L).
authors.affiliation: Exploratory Research 1, Drug Discovery Laboratories, Pharmaceutical Research Division, Yoshitomi Pharmaceutical Industries, Ltd., Iruma, Saitama, Japan. fujo@yoshitomi.co.jp
authors.forename: M
authors.initials: M
authors.lastname: Fujio
authors.forename: Y
authors.initials: Y
authors.lastname: Togo
authors.forename: H
authors.initials: H
authors.lastname: Tomozane
authors.forename: T
authors.initials: T
authors.lastname: Kuroita
authors.forename: Y
authors.initials: Y
authors.lastname: Morio
authors.forename: J
authors.initials: J
authors.lastname: Katayama
authors.forename: Y
authors.initials: Y
authors.lastname: Matsumoto
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D066298:In Vitro Techniques; D009474:Neurons / Q000187:drug effects / Q000378:metabolism; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011903:Raphe Nuclei / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2 / Q000187:drug effects / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000577:Amides; D011759:Pyrrolidines; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists