Honda K, Miyata-Osawa A, Takenaka T
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jul;330(1):16-21. doi: 10.1007/BF00586704.
The alpha-adrenoceptor subtype mediating contraction of the smooth muscle in the urinary bladder base (trigone), proximal urethra and prostate isolated from male rabbits was investigated by comparing the responsiveness to alpha-adrenoceptor agonists and antagonists under condition where beta-adrenoceptors and neuronal and extraneuronal uptakes were inhibited. Noradrenaline (non-selective), phenylephrine (alpha 1-selective) and clonidine (alpha 2-selective) caused a dose-dependent contraction in the trigone, urethra and prostate. Phenylephrine acted as a full agonist whereas clonidine was a partial agonist. YM-12617 and prazosin (alpha 1-selective), phentolamine (non-selective) and yohimbine (alpha 2-selective) produced dose-dependent shifts to the right of the dose-response curves for noradrenaline, phenylephrine and clonidine in the all three tissues. YM-12617 (pA2 = 9.77, 9.67 and 9.73 for trigone, urethra and prostate, respectively), prazosin (pA2 = 8.26, 8.20 and 8.08), phentolamine (pA2 = 7.67, 7.62 and 7.45) and yohimbine (pA2 = 6.30, 6.30 and 5.94) showed constant pA2 values irrespective of the agonists and tissues used, suggesting that only a single subclass of alpha-adrenoceptors is present. The actual pA2 values for these antagonists are comparable to those reported previously in tissues said to contain mainly alpha 1-adrenoceptors. Thus, we concluded that the postsynaptic alpha-adrenoceptors of the rabbit trigone, urethra and prostate mediating contraction belong to the alpha 1-subtype.
通过比较在β-肾上腺素能受体、神经元和非神经元摄取被抑制的条件下对α-肾上腺素能受体激动剂和拮抗剂的反应性,研究了介导雄性兔离体膀胱底部(三角区)、近端尿道和前列腺平滑肌收缩的α-肾上腺素能受体亚型。去甲肾上腺素(非选择性)、苯肾上腺素(α1选择性)和可乐定(α2选择性)在三角区、尿道和前列腺引起剂量依赖性收缩。苯肾上腺素起完全激动剂作用,而可乐定是部分激动剂。YM-12617和哌唑嗪(α1选择性)、酚妥拉明(非选择性)和育亨宾(α2选择性)使去甲肾上腺素、苯肾上腺素和可乐定在所有三个组织中的剂量-反应曲线向右发生剂量依赖性位移。YM-12617(三角区、尿道和前列腺的pA2分别为9.77、9.67和9.73)、哌唑嗪(pA2分别为8.26、8.20和8.08)、酚妥拉明(pA2分别为7.67、7.62和7.45)和育亨宾(pA2分别为6.30、6.30和5.94)显示出恒定的pA2值,与所使用的激动剂和组织无关,表明仅存在单一亚类的α-肾上腺素能受体。这些拮抗剂的实际pA2值与先前在据说主要含有α1-肾上腺素能受体的组织中报道的值相当。因此,我们得出结论,介导兔三角区、尿道和前列腺收缩的突触后α-肾上腺素能受体属于α1亚型。