克伦特罗对大鼠子宫β-肾上腺素能受体的脱敏作用

Beta-adrenoceptor desensitization by/clenbuterol in rat uterus.

作者信息

Bramuglia G F, Kazanietz M G, Pezman E, Enero M A

机构信息

Catedra de Farmacología, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Instituto de Investigaciones Farmacológicas--CONICET, Argentina.

出版信息

Gen Pharmacol. 1993 May;24(3):769-73. doi: 10.1016/0306-3623(93)90244-r.

DOI:10.1016/0306-3623(93)90244-r

PMID:8103497

Abstract

The relaxant response and cAMP production mediated by stimulation of isoproterenol is reduced in uterine rings from clenbuterol treated rats (0.25 mg kg-1 s.c. 24 hr before experiments) precontracted with 50 mM KCl. 2. Forskolin, in contrast, showed similar relaxant responses in untreated or clenbuterol treated rats. 3. Isoproterenol produces a biphasic response that is composed of a rapid relaxation followed by a slower regaining of tension, which is considered as desensitization. 4. The kinetic study demonstrates marked changes in the desensitization process of beta-adrenoceptors after clenbuterol administration.

摘要

用50 mM氯化钾预收缩的克伦特罗处理大鼠（实验前24小时皮下注射0.25 mg/kg）的子宫环中，异丙肾上腺素刺激介导的舒张反应和环磷酸腺苷（cAMP）生成减少。2. 相比之下，福斯高林在未处理或克伦特罗处理的大鼠中显示出相似的舒张反应。3. 异丙肾上腺素产生双相反应，包括快速舒张，随后是较慢的张力恢复，这被认为是脱敏。4. 动力学研究表明，给予克伦特罗后β-肾上腺素能受体脱敏过程发生显著变化。