title: Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.
abstract: The synthesis of a highly potent and selective NK1 receptor antagonist radioligand, [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine (6a) is described. The in vitro binding pharmacology and autoradiographic distribution of 6a in guinea pig brain following peripheral administration are also reported.
authors.affiliation: Pfizer Central Research, Department of Medicinal Chemistry, Groton, Connecticut 06340.
authors.forename: T
authors.initials: T
authors.lastname: Rosen
authors.forename: T F
authors.initials: TF
authors.lastname: Seeger
authors.forename: S
authors.initials: S
authors.lastname: McLean
authors.forename: M C
authors.initials: MC
authors.lastname: Desai
authors.forename: K J
authors.initials: KJ
authors.lastname: Guarino
authors.forename: D
authors.initials: D
authors.lastname: Bryce
authors.forename: K
authors.initials: K
authors.lastname: Pratt
authors.forename: J
authors.initials: J
authors.lastname: Heym
authors.forename: P M
authors.initials: PM
authors.lastname: Chalabi
authors.forename: J H
authors.initials: JH
authors.lastname: Windels
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000378:metabolism; D006168:Guinea Pigs; D008297:Male; D008969:Molecular Sequence Data; D015288:Neurokinin A / Q000037:antagonists & inhibitors*; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D013237:Stereoisomerism; D013373:Substance P / Q000737:chemistry
chemical_list: D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; C080755:3-(2-methoxybenzylamino)-2-phenylpiperidine; D013373:Substance P; D015288:Neurokinin A