SYNTHESIS, IN-VITRO BINDING PROFILE, AND AUTORADIOGRAPHIC ANALYSIS OF[H-3] CIS-3-[(2-METHOXYBENZYL)AMINO]-2-PHENYLPIPERIDINE, A HIGHLY POTENT AND SELECTIVE NONPEPTIDE SUBSTANCE-P RECEPTOR ANTAGONIST RADIOLIGAND

Authors
ROSEN T SEEGER TF MCLEAN S DESAI MC GUARINO KJ BRYCE D PRATT K HEYM J CHALABI PM WINDELS JH ROTH RW
Citation
T. Rosen et al., SYNTHESIS, IN-VITRO BINDING PROFILE, AND AUTORADIOGRAPHIC ANALYSIS OF[H-3] CIS-3-[(2-METHOXYBENZYL)AMINO]-2-PHENYLPIPERIDINE, A HIGHLY POTENT AND SELECTIVE NONPEPTIDE SUBSTANCE-P RECEPTOR ANTAGONIST RADIOLIGAND, Journal of medicinal chemistry, 36(21), 1993, pp. 3197-3201
Citations number
16
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
36
Issue
21
Year of publication
1993
Pages
3197 - 3201
Database
ISI
SICI code
0022-2623(1993)36:21<3197:SIBPAA>2.0.ZU;2-C
Abstract
The synthesis of a highly potent and selective NK1 receptor antagonist radioligand, ]cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine (6a) is described. The in vitro binding pharmacology and autoradiographic d istribution of 6a in guinea pig brain following peripheral administrat ion are also reported.