Larsen J J
Br J Pharmacol. 1979 Feb;65(2):215-22. doi: 10.1111/j.1476-5381.1979.tb07821.x.
1 The presence and type of adrenoceptors in the smooth muscle of the pig and human urinary bladder was assessed on the basis of the relative potency of alpha- and beta-adrenoceptor agonists and antagonists.2 In isolated, carbachol-contracted bladder strips from the pig detrusor muscle the relaxing potency of isoprenaline was four times that of salbutamol and ritodrine and thirty times that of noradrenaline.3 Propranolol caused a parallel shift to the right of the noradrenaline dose-response curve which was not changed by phentolamine.4 Propranolol and butoxamine showed, in contrast to practolol, a dose-dependent antagonism of the response to isoprenaline. A pA(2) value of 9.2 +/- 0.2 and 6.8 +/- 0.2 (mean +/- s.e. mean) for the first two antagonists was calculated.5 In the bladder base of the pig, propranolol caused a parallel shift to the right and phentolamine a shift to the left of the dose-response curve to noradrenaline.6 In the human detrusor muscle the potency and maximum effect of isoprenaline and salbutamol were less than those in the pig detrusor muscle. The potency of isoprenaline was sixty times that of salbutamol.7 Whereas a parallel shift to the right of the dose-response curve to isoprenaline was obtained with propranolol, no antagonism was obtained with butoxamine or practolol.8 The results are interpreted as indicating the presence of beta(2)-adrenoceptors in the detrusor muscle of the pig and beta-adrenoceptors with neither beta(1)- nor beta(2)-characteristics in the detrusor muscle of man. An indication of the presence of alpha-adrenoceptors in the bladder base but not in the detrusor muscle of the pig was obtained.
根据α和β肾上腺素能受体激动剂及拮抗剂的相对效价,评估猪和人膀胱平滑肌中肾上腺素能受体的存在情况及类型。
在猪逼尿肌分离的、由卡巴胆碱收缩的膀胱条上,异丙肾上腺素的舒张效价是沙丁胺醇和利托君的四倍,是去甲肾上腺素的三十倍。
普萘洛尔使去甲肾上腺素剂量 - 反应曲线平行右移,酚妥拉明对此无影响。
与普拉洛尔相反,普萘洛尔和布托沙明对异丙肾上腺素的反应呈剂量依赖性拮抗。计算出前两种拮抗剂的pA(2)值分别为9.2±0.2和6.8±0.2(均值±标准误均值)。
在猪膀胱底部,普萘洛尔使去甲肾上腺素剂量 - 反应曲线平行右移,酚妥拉明使其左移。
在人逼尿肌中,异丙肾上腺素和沙丁胺醇的效价及最大效应低于猪逼尿肌。异丙肾上腺素的效价是沙丁胺醇的六十倍。
普萘洛尔使异丙肾上腺素剂量 - 反应曲线平行右移,而布托沙明或普拉洛尔未产生拮抗作用。
结果表明,猪逼尿肌中存在β(2)肾上腺素能受体,人逼尿肌中存在既无β(1)也无β(2)特性的β肾上腺素能受体。有迹象表明猪膀胱底部存在α肾上腺素能受体,但逼尿肌中不存在。