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

被引：43

作者：

ROSEN, T

SEEGER, TF

MCLEAN, S

DESAI, MC

GUARINO, KJ

BRYCE, D

PRATT, K

HEYM, J

CHALABI, PM

WINDELS, JH

ROTH, RW

机构：

[1] PFIZER INC,CENT RES,DEPT NEUROSCI,GROTON,CT 06340

[2] CHEMSYN SCI LABS,LENEXA,KS 66215

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 21期

关键词：

D O I：

10.1021/jm00073a022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a highly potent and selective NK1 receptor antagonist radioligand, [H-3]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.

引用

页码：3197 / 3201

页数：5

共 16 条

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BHAGWATHEESWARAN H, 1976, SYNTHESIS-STUTTGART, P615

[2]

CHANG MM, 1970, J BIOL CHEM, V245, P4784

[3] 1,3,5-TRISUBSTITUTED BENZENES .1. SYNTHESIS AND REACTIONS OF 3,5-DIBROMOPHENYLLITHIUM [J].