哌唑嗪对大鼠输精管α 1a -肾上腺素受体的效价低,对α 1d -肾上腺素受体的效价高

J. R. Docherty
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引用次数: 9

摘要

我们研究了α1-肾上腺素能受体亚型介导大鼠输精管附睾部分对去甲肾上腺素的收缩。在没有或存在去甲肾上腺素转运阻断剂可卡因的情况下,对去甲肾上腺素的收缩进行了研究。在不含可卡因的情况下,RS100329对去甲肾上腺素的收缩有拮抗作用,而BMY7378则无拮抗作用,因此主要由α α -肾上腺素受体介导。在可卡因的存在下,去甲肾上腺素的效力增加,特别是在低浓度和阶段性收缩方面。RS100329对低浓度去甲肾上腺素的收缩有抗性,但BMY7378对其有拮抗作用,表明α 1d -肾上腺素受体还参与了可卡因放大的收缩。在没有可卡因的情况下,哌唑嗪作为α 1a -肾上腺素受体介导的反应的拮抗剂表现出相对较低的效力。在可卡因存在的情况下,哌唑嗪对α 1d肾上腺素受体介导的成分表现出更高的效力。综上所述,在大鼠输精管的功能研究中,哌唑嗪对α1D-而不是α 1a -肾上腺素受体具有先前未报道的选择性。α1A-和α 1d肾上腺素受体介导大鼠输精管收缩。先前在大鼠输精管中报道的prazosin效价和受体亚型的范围可以用这两种亚型的存在来解释。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Prazosin has low potency at α1A-adrenoceptors and high potency at α1D-adrenoceptors in rat vas deferens

  1. We have investigated α1-adrenoceptor subtypes mediating contractions to noradrenaline in epididymal portions of rat vas deferens.
  2. Contractions to noradrenaline were investigated in the absence or presence of the noradrenaline transporter blocker cocaine.
  3. In the absence of cocaine, contractions to noradrenaline were potently antagonized by RS100329, but not by BMY7378, and so are mediated mainly by α1A-adrenoceptors.
  4. In the presence of cocaine, noradrenaline potency was increased, particularly in terms of low concentrations and phasic contractions. Contractions to low concentrations of noradrenaline in the presence of cocaine were resistant to RS100329 but potently antagonized by BMY7378, demonstrating that α1D-adrenoceptors are additionally involved in contractions amplified by cocaine.
  5. In the absence of cocaine, prazosin exhibited relatively low potency as an antagonist against the α1A-adrenoceptor-mediated component to the response. In the presence of cocaine, prazosin exhibited higher potency against the α1D-adrenoceptor-mediated component.
  6. In conclusion, prazosin has previously unreported selectivity for α1D- over α1A-adrenoceptors in functional studies of rat vas deferens. Contractions of rat vas deferens are mediated by α1A- and α1D-adrenoceptors. The range of prazosin potencies and of receptor subtypes previously reported in rat vas deferens may be explained by the presence of these two subtypes.
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