Kano T
Jpn J Pharmacol. 1982 Jun;32(3):535-49. doi: 10.1254/jjp.32.535.
The effects of estrogen and progesterone on adrenoceptors and cyclic nucleotides were studied in ovariectomized rat uterus. The effects on adrenoceptors were examined by measuring mechanical responses to noradrenaline and by binding site determinations with [3H]-dihydroergocryptine and [3H]-dihydroalprenolol. After acute administration of estradiol-17 beta, uterine cyclic GMP was progressively and significantly elevated, but cyclic AMP declined through it was not significant. Phentolamine suppressed this cyclic GMP elevation. Both acute and chronic treatments with estrogen increased the number of alpha-receptors. The increase in uterine cyclic GMP was related to the increase in alpha-stimulation as a result of increased alpha-receptors. Chronic treatment with estrogen increased the number of alpha-receptors. The alpha-effect induced by noradrenaline was bidirectional in the uterus treated with estrogen chronically; there was contraction in normal Tyrode's solution and relaxation in high K+ Tyrode's solution. In other hormonal group, either alpha- or beta-effects produced relaxation. Enhancement of the alpha- and beta-effects by estrogen is attributed to an increased number of the receptors. Acute treatment with estrogen decreased the responses of cyclic AMP to isoproterenol and mechanical reactivity. Progesterone also enhanced the beta-effect as a result of an increase in the number of beta-receptors.
在去卵巢大鼠子宫中研究了雌激素和孕酮对肾上腺素能受体及环核苷酸的影响。通过测量对去甲肾上腺素的机械反应以及用[3H]-二氢麦角隐亭和[3H]-二氢心得静进行结合位点测定来检测对肾上腺素能受体的影响。急性给予17β-雌二醇后，子宫环鸟苷酸（cGMP）逐渐且显著升高，但环腺苷酸（cAMP）虽有下降但不显著。酚妥拉明可抑制这种环鸟苷酸的升高。雌激素的急性和慢性处理均增加了α-受体的数量。子宫环鸟苷酸的升高与因α-受体增加导致的α-刺激增加有关。雌激素的慢性处理增加了α-受体的数量。在长期用雌激素处理的子宫中，去甲肾上腺素诱导的α-效应是双向的；在正常台氏液中出现收缩，而在高钾台氏液中出现舒张。在其他激素组中，α-或β-效应均产生舒张作用。雌激素增强α-和β-效应归因于受体数量的增加。雌激素的急性处理降低了环腺苷酸对异丙肾上腺素的反应及机械反应性。孕酮也因β-受体数量增加而增强了β-效应。
