Andersson R G, Johansson S R, Salomonsson I
Department of Pharmacology, University Hospital, University of Linköping, Sweden.
Pharmacol Toxicol. 1988 Jan;62(1):29-31. doi: 10.1111/j.1600-0773.1988.tb01839.x.
The time course of resensitization of the down-regulated beta-adrenoceptor system of rat myometrium was studied. The isoprenaline-induced decrease of myometrial cAMP reversed rather rapidly and after 4 and 8 days no significant change of the cAMP level was demonstrated, however, the cAMP level was higher than in the control myometrium after 12 days. The elevated phosphodiesterase activity decreased to 80% of control activity after 4 days, but returned to control activity after 8 days. The decreased number of beta-adrenoceptors increased gradually after discontinuing the treatment and reached the number of the controls after 12 days. Our results suggest that the resensitization of the beta-adrenoceptor-cAMP-system is rather complex, the normalization of the cAMP content and the phosphodiesterase activity is more rapid than the normalization of the beta-adrenoceptor number which is a rather slow process in myometrial tissue.
研究了大鼠子宫肌层下调的β-肾上腺素能受体系统再敏化的时间进程。异丙肾上腺素诱导的子宫肌层环磷酸腺苷(cAMP)水平降低逆转相当迅速,4天和8天后cAMP水平无显著变化,然而,12天后cAMP水平高于对照子宫肌层。升高的磷酸二酯酶活性在4天后降至对照活性的80%,但8天后恢复到对照活性。停止治疗后,β-肾上腺素能受体数量的减少逐渐增加,12天后达到对照数量。我们的结果表明,β-肾上腺素能受体-cAMP系统的再敏化相当复杂,cAMP含量和磷酸二酯酶活性的正常化比β-肾上腺素能受体数量的正常化更快,而β-肾上腺素能受体数量的正常化在子宫肌层组织中是一个相当缓慢的过程。