title: Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.
abstract: The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses.
authors.affiliation: Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
authors.forename: T J
authors.initials: TJ
authors.lastname: Rosen
authors.forename: K J
authors.initials: KJ
authors.lastname: Coffman
authors.forename: S
authors.initials: S
authors.lastname: McLean
authors.forename: R T
authors.initials: RT
authors.lastname: Crawford
authors.forename: D K
authors.initials: DK
authors.lastname: Bryce
authors.forename: Y
authors.initials: Y
authors.lastname: Gohda
authors.forename: M
authors.initials: M
authors.lastname: Tsuchiya
authors.forename: A
authors.initials: A
authors.lastname: Nagahisa
authors.forename: M
authors.initials: M
authors.lastname: Nakane
authors.forename: J A
authors.initials: JA
authors.lastname: Lowe
mesh_terms: D000818:Animals; D002211:Capsaicin / Q000037:antagonists & inhibitors; D002460:Cell Line; D006168:Guinea Pigs; D006801:Humans; D009043:Motor Activity / Q000187:drug effects; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; C099414:(2S,3S)-2-phenyl-3-((5-trifluoromethoxy-2-methoxy)benzylamino)piperidine; D002211:Capsaicin