RP-70676 - A POTENT SYSTEMICALLY AVAILABLE INHIBITOR OF ACYL-COA-CHOLESTEROL O-ACYL TRANSFERASE (ACAT)

被引：31

作者：

ASHTON, MJ

BRIDGE, AW

BUSH, RC

DRON, DI

HARRIS, NV

JONES, GD

LYTHGOE, DJ

RIDDELL, D

SMITH, C

机构：

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(00)80149-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

RP 70676 (3d) is a potent inhibitor of ACAT. It is an effective hypocholesterolaemic agent in the cholesterol-fed rabbit, and reduces the accumulation of both cholesterol and cholesterol ester in rabbit aorta and thoracic artery. The compound is readily bioavailable in rabbits with significant levels of parent compound present in plasma up to 6 hours after an oral dose.

引用

页码：375 / 380

页数：6

共 8 条

[1]

BELL FP, 1986, PHARM CONTROL HYPERL, P409

[2]

BILLHEIMER JT, 1990, Patent No. 327445

[3]

BILLHEIMER JT, 1991, 9TH INT S ATH CHIC

[4]

COFFEE ECJ, 1990, Patent No. 391796

[5]

DENNIS MJ, 1990, COMPREHENSIVE MED CH, P7

[6]

LICHTENSTEIN AH, 1980, J BIOL CHEM, V255, P9098

[7] THERAPEUTIC POTENTIAL OF ACAT INHIBITORS AS LIPID LOWERING AND ANTIATHEROSCLEROTIC AGENTS [J].

SLISKOVIC, DR ;

WHITE, AD .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1991, 12 (05) :194-199

[8]

SUCKLING KE, 1985, J LIPID RES, V26, P647

← 1 →