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首页> 外文期刊>European Journal of Pharmacology: An International Journal >Effect of alpha2-adrenoceptor stimulation on isolated canine Purkinje fiber contraction.
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Effect of alpha2-adrenoceptor stimulation on isolated canine Purkinje fiber contraction.

机译:α2-肾上腺素能受体刺激对离体犬浦肯野纤维收缩的影响。

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We have recently identified the presence of postjunctional alpha2-adrenoceptors in canine Purkinje fibers. In this study, we examined the effects of alpha2-adrenoceptor stimulation on the contraction strength of isolated Purkinje fibers. Exposure to the alpha2-adrenoceptor specific agonist and antagonist, UK 14,304 (5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine) and yohimbine (17-hydroxyyohimban-16-carboxylic acid methyl ester hydrochloride) alone at 0.1 microM respectively, did not produce any significant effect on Purkinje contraction strength. Purkinje contraction strength was augmented by isoproterenol (0.1 microM), forskolin (0.1 microM), or 8-bromo-adenosine cyclic 2',3'-monophosphate (8-bromo-cAMP, 10 microM). UK 14,304 significantly reversed the effects of isoproterenol and forskolin but not those of 8-bromo-cAMP on Purkinje contraction strength. After incubation with pertussis toxin, the positive inotropic effect of forskolin on Purkinje contraction strength remained intact, but the forskolin effect could no longer be reversed by UK 14,304. These results suggest that the postjunctional alpha2-adrenoceptors in canine Purkinje fibers are coupled to a pertussis toxin-sensitive G protein, probably Gi. Stimulation of the alpha2-adrenoceptor antagonizes the effect of beta-adrenoceptor stimulation on Purkinje contraction strength in an accentuated antagonism manner.
机译:我们最近发现犬浦肯野纤维中存在结后α2-肾上腺素受体。在这项研究中,我们检查了α2-肾上腺素受体刺激对孤立的浦肯野纤维收缩强度的影响。暴露于α2-肾上腺素受体特异性激动剂和拮抗剂,英国14,304(5-溴-N-(4,5-二氢-1H-咪唑-2-基)-6-喹喔啉胺)和育亨宾(17-hydroxyyohimban-16-carboxy分别为0.1 microM的乙酸甲酯盐酸盐)对浦肯野的收缩强度没有产生任何显着影响。异丙肾上腺素(0.1 microM),毛喉素(0.1 microM)或8-溴-腺苷环2',3'-单磷酸酯(8-bromo-cAMP,10 microM)增强了Purkinje的收缩强度。 UK 14,304显着逆转了异丙肾上腺素和毛喉素的作用,但没有逆转8-溴-cAMP对浦肯野收缩强度的作用。与百日咳毒素一起孵育后,福司可林对浦肯野收缩力的正性肌力作用保持不变,但是UK 14,304不能再逆转福司可林的作用。这些结果表明,犬浦肯野纤维中的结后α2-肾上腺素受体与百日咳毒素敏感的G蛋白(可能是Gi)偶联。 α2-肾上腺素受体的刺激以增强的拮抗方式拮抗β-肾上腺素受体刺激对浦肯野收缩强度的作用。

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