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Characterization of #alpha#_1-adrenoceptor subtypes mediating noradrenaline-induced contraction of rat epididymal vas deferens in calcium-free medium

机译:在无钙培养基中介导去甲肾上腺素诱导的大鼠附睾输精管收缩的#alpha#_1-肾上腺素受体亚型的表征

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摘要

The #alpha#_1-adrenoceptor subtype mediating noradrenaline (NA)-induced contractions of rat epididymal vas deferens in Ca~(2+)-free/EGTA (1 mM) medium was studied using competitive antagonists. The effects of chloroethylclonidine (CEC) was investigated in Ca~(2+)-free and normal Krebs' medium and RT-PCR was used to identify #alpha#_1- adrenoceptor specific mRNA in epididymal vas deferens. In Ca~(2+)-free medium, NA evoked sustained contractions but was less potent (pD_2, 5.9) than in normal Krebs' medium (pD_2, 7.3). The contractions in Ca~(2+)-free medium, NA evoked sustained contractions but was less potent (pD_2, 7.6) and BMY 7378 (pK_B, 6.8) consistent with activation of #alpha#_(1A)-subtype. Repeated pretreatment with CEC (100 #mu#M) reduced the potency of NA and maximum contractions in normal and Ca~(2+)-free media. CEC-sensitivity in normal Krebs' medium was enhanced by prior treatment with phenoxybenzamine. mRNA for #alpha#_(1a)- and #alpha#_(1b)- adrenoceptors were detected in Ca~(2+)-free medium by the stimulation of #alpha#_(-A)-adrenoceptors. Two factors affecting CEC-sensitivity of NA-induced contractions in this tissue are discussed.
机译:使用竞争性拮抗剂研究了在无Ca〜(2 +)/ EGTA(1 mM)培养基中调和去甲肾上腺素(NA)诱导的大鼠附睾输精管收缩的#alpha#_1-肾上腺素受体亚型。在无Ca〜(2+)和正常Krebs培养基中研究了氯乙基可乐定(CEC)的作用,并使用RT-PCR鉴定附睾输精管中的#alpha#_1-肾上腺素受体特异性mRNA。在不含Ca〜(2+)的培养基中,NA引起持续收缩,但效力低于普通克雷布斯培养基(pD_2,7.3)(pD_2,5.9)。在无Ca〜(2+)的培养基中,NA引起持续收缩,但效力较弱(pD_2,7.6)和BMY 7378(pK_B,6.8)与#alpha #_(1A)-亚型的激活一致。在正常和不含Ca〜(2+)的培养基中,用CEC(100#mu#M)重复进行预处理会降低NA的效力和最大收缩。预先用苯氧基苯甲胺治疗可增强正常克雷布斯培养基中的CEC敏感性。通过刺激#alpha #_(-A)-肾上腺素受体,在不含Ca〜(2+)的培养基中检测到#alpha #_(1a)-和#alpha #_(1b)-肾上腺素受体的mRNA。讨论了影响该组织中NA诱导的收缩的CEC敏感性的两个因素。

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