大鼠前列腺中的毒蕈碱受体亚型
Muscarinic receptor subtypes in the rat prostate gland.
作者信息
Lau W A, Pennefather J N
机构信息
Department of Pharmacology, Monash University, Clayton, Vic., Australia.
出版信息
Eur J Pharmacol. 1998 Feb 19;343(2-3):151-6. doi: 10.1016/s0014-2999(97)01535-5.
Muscarinic receptor subtypes mediating carbachol-induced contractions of the rat prostatic smooth muscle were determined. The rank order of potency of muscarinic receptor antagonists in blocking the effects of carbachol was (mean pKB estimates in parentheses): atropine (8.90) >> para-fluorohexahydrosiladifenidol (7.75) > or = hexahydrosiladifenidol (7.62) > methoctramine (6.89) > or = pirenzepine (6.68) > or = himbacine (6.67). The specific binding of [3H]quinuclidinyl benzilate to the rat prostatic homogenates was competitively inhibited by (mean pKi values in parentheses): atropine (8.89) >> hexahydrosiladifenidol (7.86) > para-fluorohexahydrosiladifenidol (7.28) > or = himbacine (7.22) > pirenzepine (6.63) > or = methoctramine (6.38). These profiles, whilst different, indicate the probable involvement of muscarinic M3 receptors in the carbachol-induced contraction.
确定了介导卡巴胆碱诱导大鼠前列腺平滑肌收缩的毒蕈碱受体亚型。毒蕈碱受体拮抗剂阻断卡巴胆碱作用的效价顺序为（括号内为平均pKB估计值）：阿托品（8.90）>>对氟六氢硅二苯醇（7.75）≥六氢硅二苯醇（7.62）>甲溴东莨菪碱（6.89）≥哌仑西平（6.68）≥辛巴辛（6.67）。[3H]喹核醇基苯甲酸酯与大鼠前列腺匀浆的特异性结合受到以下物质的竞争性抑制（括号内为平均pKi值）：阿托品（8.89）>>六氢硅二苯醇（7.86）>对氟六氢硅二苯醇（7.28）≥辛巴辛（7.22）>哌仑西平（6.63）≥甲溴东莨菪碱（6.38）。这些情况虽有所不同，但表明毒蕈碱M3受体可能参与了卡巴胆碱诱导的收缩过程。
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