苯乙醇胺LY79771及其立体异构体对正常和肥胖Avy/a小鼠脂肪组织中环磷酸腺苷（cAMP）和脂肪分解的刺激作用。

Stimulation of cyclic AMP and lipolysis in adipose tissue of normal and obese Avy/a mice by LY79771, a phenethanolamine, and stereoisomers.

作者信息

Yen T T, McKee M M, Stamm N B, Bemis K G

出版信息

Life Sci. 1983 Mar 28;32(13):1515-22. doi: 10.1016/0024-3205(83)90918-9.

Abstract

The stimulation of cyclic AMP and lipolysis by LY79771, a phenethanolamine antiobesity compound, and its 3 stereoisomers in adipose tissue of obese viable yellow mice and normal mice were studied. Both activities were stereo-specific with LY79771, the R,S isomer, and LY79730, the R,R isomer, being more potent than LY103085, the S,S isomer, and LY103672, the S,R isomer. Propranolol, a nonspecific beta-antagonist, completely inhibited the elevation of cyclic AMP and lipolysis whereas atenolol, a specific beta 1 antagonist, inhibited the elevation of cyclic AMP but did not completely inhibit lipolysis. These findings indicate that the elevation of cyclic AMP was mediated by the beta 1-receptor whereas the stimulation of lipolysis was mediated by both the beta 1 and beta 2 receptors. The adipose tissue of the obese viable yellow mice responded to these compounds less than that of the normal mice.

摘要

研究了苯乙醇胺抗肥胖化合物LY79771及其3种立体异构体对肥胖可存活黄色小鼠和正常小鼠脂肪组织中环磷酸腺苷（cAMP）和脂肪分解的刺激作用。两种活性对LY79771（R,S异构体）和LY79730（R,R异构体）具有立体特异性，它们比LY103085（S,S异构体）和LY103672（S,R异构体）更有效。非特异性β拮抗剂普萘洛尔完全抑制cAMP升高和脂肪分解，而特异性β1拮抗剂阿替洛尔抑制cAMP升高，但未完全抑制脂肪分解。这些发现表明，cAMP升高由β1受体介导，而脂肪分解刺激由β1和β2受体共同介导。肥胖可存活黄色小鼠的脂肪组织对这些化合物的反应比正常小鼠小。