Lepor H, Zhang W, Kobayashi S, Tang R, Wang B, Shapiro E
Department of Urology, Medical College of Wisconsin, Milwaukee.
J Pharmacol Exp Ther. 1994 Aug;270(2):722-7.
The present study was designed to compare the binding and functional properties of alpha-1 adrenoceptors and the area density of smooth muscle in the human, canine and rat prostates. Chloroethylclonidine (CEC)-sensitive and -insensitive alpha-1 adrenoceptors were characterized on slide-mounted prostatic tissue sections using the ligand [3H]prazosin. The mean equilibrium dissociation constants (Kd) for [3H]prazosin binding sites were not significantly different among the three different species. The densities (Bmax) of CEC insensitive [3H]prazosin binding sites in the human, canine and rat prostates were 1.71 +/- 0.32, 0.35 +/- 0.04 and 0.84 +/- 0.11 fmol/mg of wet weight, respectively. The Bmax of CEC-sensitive [3H]prazosin binding sites in the human, canine and rat prostates were 1.32 +/- 0.83, 0.44 +/- 0.11 and 0.25 +/- 0.10 fmol/mg of wet weight, respectively. The contractile response elicited by the rat prostate in the presence of phenylephrine was consistently negligible. The mean maximal force after phenylephrine challenge (phenylephrine Emax) in the human and canine prostates were 0.125 +/- 0.025 g of force/mm2 cross-sectional area and 0.096 +/- 0.014 g of force/mm2 cross-sectional area, respectively. CEC inactivated 80 and 53% of the phenylephrine contractile response in man and dog, respectively. The mean percentage of area densities of smooth muscle in the human, canine and rat prostates were 38.8, 12.9 and < 1%, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
本研究旨在比较人、犬和大鼠前列腺中α-1肾上腺素能受体的结合和功能特性以及平滑肌的面积密度。使用配体[3H]哌唑嗪对载玻片上的前列腺组织切片进行氯乙可乐定(CEC)敏感和不敏感的α-1肾上腺素能受体特性分析。三种不同物种之间,[3H]哌唑嗪结合位点的平均平衡解离常数(Kd)无显著差异。人、犬和大鼠前列腺中CEC不敏感的[3H]哌唑嗪结合位点密度(Bmax)分别为1.71±0.32、0.35±0.04和0.84±0.11 fmol/mg湿重。人、犬和大鼠前列腺中CEC敏感的[3H]哌唑嗪结合位点的Bmax分别为1.32±0.83、0.44±0.11和0.25±0.10 fmol/mg湿重。在去氧肾上腺素存在下,大鼠前列腺引起的收缩反应始终可忽略不计。人及犬前列腺在去氧肾上腺素激发后的平均最大力(去氧肾上腺素Emax)分别为0.125±0.025 g力/mm2横截面积和0.096±0.014 g力/mm2横截面积。CEC分别使人和犬的去氧肾上腺素收缩反应失活80%和53%。人、犬和大鼠前列腺中平滑肌面积密度的平均百分比分别为38.8%、12.9%和<1%。(摘要截短至250字)