Gray Katherine T, Ventura Sabatino
Prostate Research Co-operative, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia.
Eur J Pharmacol. 2006 Jul 1;540(1-3):155-61. doi: 10.1016/j.ejphar.2006.04.016. Epub 2006 Apr 28.
The subtype of alpha1-adrenoceptor mediating noradrenaline-induced contractile responses in isolated mouse prostate glands was investigated. Adrenoceptor agonists were able to produce concentration-dependent contractions with the following rank order of potency: adrenaline > or = noradrenaline > or = clonidine = phenylephrine > dopamine > or = isoprenaline. Concentration-response curves to noradrenaline of the prostatic smooth muscle were antagonised by prazosin, N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha, alpha-dimethyl-1H-indole-3-ethanamine (RS-17053), 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB 4101), tamsulosin and yohimbine with mean antagonist affinity estimates (pA2 or apparent pKB) of 8.12+/-0.10, 6.56+/-0.11, 8.38+/-0.06, 10.14+/-0.19 and 7.38+/-1.36 respectively. Propranolol (1 microM) had no antagonist activity (P = 0.994, n = 6). Yohimbine (0.01, 0.1, 1 microM) had no antagonist activity in the presence of prazosin (0.1 microM) (P > or = 0.059). The results obtained indicate that alpha1-adrenoceptors mediate the contractile response in isolated preparations of the mouse prostate. Furthermore, the particular subtype of alpha1-adrenoceptor mediating the response to exogenously administered noradrenaline corresponds to the alpha1L-subtype, the same subtype as that which has been shown to mediate noradrenaline-induced contractile activity in the human prostate.
研究了介导去甲肾上腺素诱导的离体小鼠前列腺收缩反应的α1-肾上腺素能受体亚型。肾上腺素能受体激动剂能够产生浓度依赖性收缩，其效力顺序如下：肾上腺素≥去甲肾上腺素≥可乐定 = 去氧肾上腺素＞多巴胺≥异丙肾上腺素。哌唑嗪、N-[2-(2-环丙基甲氧基苯氧基)乙基]-5-氯-α,α-二甲基-1H-吲哚-3-乙胺（RS-17053）、2-(2,6-二甲氧基苯氧基乙基)氨基甲基-1,4-苯并二恶烷（WB 4101）、坦索罗辛和育亨宾可拮抗前列腺平滑肌对去甲肾上腺素的浓度-反应曲线，平均拮抗剂亲和力估计值（pA2或表观pKB）分别为8.12±0.10、6.56±0.11、8.38±0.06、10.14±0.19和7.38±1.36。普萘洛尔（1μM）无拮抗活性（P = 0.994，n = 6）。在存在哌唑嗪（0.1μM）的情况下，育亨宾（0.01、0.1、1μM）无拮抗活性（P≥0.059）。所得结果表明，α1-肾上腺素能受体介导小鼠前列腺离体标本中的收缩反应。此外，介导对外源性给予去甲肾上腺素反应的α1-肾上腺素能受体的特定亚型对应于α1L-亚型，与已证明介导人前列腺中去甲肾上腺素诱导的收缩活性的亚型相同。
