Takayanagi I, Maeda O, Koike K
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
J Pharm Pharmacol. 1987 Sep;39(9):754-7. doi: 10.1111/j.2042-7158.1987.tb06987.x.
Postsynaptic alpha 1-adrenoceptor mechanisms in vasa deferentia isolated from 3, 6, 18 and 40 week-old rats were studied by analysis of the concentration-response curve of noradrenaline and the Scatchard plot of specific binding of [3H]prazosin to microsomal fractions. The maximum tension developed by noradrenaline also increased with age from 3 to 18 weeks. The efficacy of noradrenaline and capacity of the maximum binding sites of [3H]prazosin increased with increasing age, while the dissociation constants of noradrenaline (KA) and prazosin (Kd) were not changed with age. The increase of the maximum tension was proportional to the increase in efficacy. The increase of efficacy for noradrenaline in the vasa deferentia from rats of different ages is due to the increase in the total concentration of postsynaptic alpha 1-adrenoceptors.
通过分析去甲肾上腺素的浓度-反应曲线以及[³H]哌唑嗪与微粒体部分特异性结合的Scatchard图,研究了从3周龄、6周龄、18周龄和40周龄大鼠分离出的输精管中的突触后α1-肾上腺素能受体机制。去甲肾上腺素产生的最大张力也随年龄从3周增加到18周而增加。去甲肾上腺素的效能以及[³H]哌唑嗪最大结合位点的容量随年龄增加而增加,而去甲肾上腺素(KA)和哌唑嗪(Kd)的解离常数不随年龄变化。最大张力的增加与效能的增加成正比。不同年龄大鼠输精管中去甲肾上腺素效能的增加是由于突触后α1-肾上腺素能受体总浓度的增加。