SYNTHESIS AND METABOLIC PROFILE OF CI-966 - A POTENT, ORALLY-ACTIVE INHIBITOR OF GABA UPTAKE

被引：19

作者：

BJORGE, S

BLACK, A

BOCKBRADER, H

CHANG, T

GREGOR, VE

LOBBESTAEL, SJ

NUGIEL, D

PAVIA, MR

RADULOVIC, L

WOOLF, T

机构：

[1] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT CHEM,ANN ARBOR,MI 48105

[2] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS RES DIV,DEPT PHARMACOKINET & DRUG METAB,ANN ARBOR,MI 48105

来源：

DRUG DEVELOPMENT RESEARCH | 1990年 / 21卷 / 03期

关键词：

anticonvulsant; guvacine; pyridinium; rats;

D O I：

10.1002/ddr.430210305

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A lipophilic derivative of the known GABA uptake inhibitor guvacine has been prepared. The synthesis of this compound, [1‐]2‐bis 4‐(trifluoromethyl)]phenyl[‐methoxy]ethyl[‐ 1,2,5,6‐tet‐rahydro‐3‐pyridine carboxylic acid, monohydrochloride, Cl‐966, is described. Studies were carried out to determine the metabolic profile of Cl‐966, in rats. Two metabolites, one less polar and the other more polar than Cl‐966, were identified and their structures assigned by spectroscopic methods and confirmed by comparison to synthetic material. Copyright © 1990 Wiley‐Liss, Inc.

引用

页码：189 / 193

页数：5

共 23 条

[1] ORALLY ACTIVE AND POTENT INHIBITORS OF GAMMA-AMINOBUTYRIC ACID UPTAKE [J].