Hyperalphalipoproteinaemic activity of BRL 26314--I. Enhanced cholesterol turnover in rats |
| |
Authors: | R Fears W R Rush P Walker H Ferres |
| |
Affiliation: | Beecham Pharmaceuticals Research Division, Great Burgh, Epsom, Surrey KT18 5XQ, U.K. |
| |
Abstract: | Administration of BRL 26314 [N-(4-chlorobenzyl)-L-phenylalanine] raises circulating high-density lipoprotein (HDL) cholesterol and lowers total triglyceride levels in rats whether maintained on stock or semi-synthetic diets. HDL is also elevated by BRL 26314 in hypothyroid rats and in rats with pre-existing hyperlipidaemia where aortic total cholesterol concentration is decreased. BRL 26314 promotes the excretion of a dose of radiolabelled cholesterol as faecal sterols and bile acids, and decreases the extent of cholesterol-radiolabelling in tissue pools, particularly the aorta and adipose tissue. The increase in cholesterol and bile acid (cholic acid) turnover distinguishes BRL 26314 from a cholestatic agent such as 1-naphthyl isothiocyanate where a superficially similar change in HDL concentration disguises an impaired cholesterol transport. BRL 26314 is not a general protein inducer but part of the mechanism of action may involve enhancement of white adipose tissue lipoprotein lipase activity. |
| |
Keywords: | To whom correspondence should be addressed. |
本文献已被 ScienceDirect 等数据库收录! |