Nakazawa M, Taguchi Y, Yang X P, Chiba S
Department of Pharmacology, Shinshu University School of Medicine, Matsumoto 390-8621, Japan.
Auton Autacoid Pharmacol. 2002 Oct-Dec;22(5-6):253-9. doi: 10.1046/j.1474-8673.2002.00267.x.
1 The present study attempted to pharmacologically characterize the subtypes of alpha-adrenoceptors mediating the vasoconstriction in the isolated and perfused canine vesical artery. 2 Noradrenaline (NA) and phenylephrine (PE, an alpha1-adrenoceptor agonist) induced a dose-dependent vasoconstriction, whereas xylazine (an alpha2-agonist) did not induce any clear vascular constrictor response. 3 Prazosin at 0.01 microM and rauwolscine at 0.1 microM failed to affect the NA-induced vasoconstriction. Prazosin at 0.1 microM antagonized the vasoconstrictor responses to NA, with pKB value of 7.8. 4 WB 4101 at 0.01-0.1 microM dose-dependently inhibited the responses to NA, with a pKB value of 8.9. The vasoconstrictor responses to NA were not significantly affected by chloroethylclonidine (10-30 microM) or BMY 7378 (0.1 microM). 5 The present results indicate that the canine vesical arteries dominantly contain alpha1-adrenoceptors but have no alpha2-adrenoceptors, and the functional subtype of alpha1-adrenoceptor is characterized as an alpha1A-adrenoceptor subtype.
1 本研究试图从药理学角度对介导离体灌注犬膀胱动脉血管收缩的α-肾上腺素能受体亚型进行表征。2 去甲肾上腺素（NA）和苯肾上腺素（PE，一种α1-肾上腺素能受体激动剂）可引起剂量依赖性血管收缩，而赛拉嗪（一种α2-激动剂）未引起任何明显的血管收缩反应。3 0.01微摩尔的哌唑嗪和0.1微摩尔的育亨宾未能影响NA诱导的血管收缩。0.1微摩尔的哌唑嗪可拮抗对NA的血管收缩反应，pKB值为7.8。4 0.01 - 0.1微摩尔剂量的WB 4101可剂量依赖性地抑制对NA的反应，pKB值为8.9。氯乙可乐定（10 - 30微摩尔）或BMY 7378（0.1微摩尔）对NA诱导的血管收缩反应无显著影响。5 目前的结果表明，犬膀胱动脉主要含有α1-肾上腺素能受体，但不含α2-肾上腺素能受体，且α1-肾上腺素能受体的功能亚型为α1A-肾上腺素能受体亚型。
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