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犬基底动脉α肾上腺素能受体的药理学特性

Pharmacological characterization of the alpha adrenoceptors of the dog basilar artery.

作者信息

Sakakibara Y, Fujiwara M, Muramatsu I

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):1-7. doi: 10.1007/BF00491469.

Abstract

The effects of alpha adrenoceptor agonists and antagonists on the postsynaptic alpha receptors were examined in the dog basilar, mesenteric and renal arteries and the type of alpha adrenoceptors present was characterized. In the basilar artery, noradrenaline, clonidine and phenylephrine produced almost the same maximal contraction, the pD2 values being 6.51 +/- 0.11, 5.49 +/- 0.16 and 5.65 +/- 0.13, respectively. Yohimbine (1-3 x 10(-8) M) inhibited the contractile responses to noradrenaline and clonidine competitively and the response to phenylephrine noncompetitively. Corynanthine (10(-6) M) had no effect on such contractile responses. In the mesenteric and renal arteries, the maximal responses to noradrenaline and phenylephrine were markedly greater than those to clonidine. Yohimbine (10(-7) - 10(-5) M) and corynanthine (10(-7) - 10(-5) M) both antagonized noradrenaline competitively in these vessels. In the basilar, mesenteric and renal arteries preloaded with 3H-noradrenaline, 3H-efflux induced by electrical transmural stimulation was attenuated by clonidine (10(-10) - 10(-7) M), while phenylephrine (10(-10) - 10(-8) M) was without effect. Yohimbine at considerably lower concentrations than corynanthine increased the 3H-efflux elicited by electrical stimulation. These results indicate that presynaptic and postsynaptic alpha receptors of the dog basilar artery are largely alpha 2 in contrast to those of peripheral arteries.

摘要

在犬的基底动脉、肠系膜动脉和肾动脉中,研究了α肾上腺素能受体激动剂和拮抗剂对突触后α受体的作用,并对所存在的α肾上腺素能受体类型进行了表征。在基底动脉中,去甲肾上腺素、可乐定和去氧肾上腺素产生几乎相同的最大收缩反应,其pD2值分别为6.51±0.11、5.49±0.16和5.65±0.13。育亨宾(1 - 3×10⁻⁸M)竞争性抑制对去甲肾上腺素和可乐定的收缩反应,而非竞争性抑制对去氧肾上腺素的反应。育亨宾(10⁻⁶M)对这种收缩反应无影响。在肠系膜动脉和肾动脉中,对去甲肾上腺素和去氧肾上腺素的最大反应明显大于对可乐定的反应。育亨宾(10⁻⁷ - 10⁻⁵M)和育亨宾(10⁻⁷ - 10⁻⁵M)在这些血管中均竞争性拮抗去甲肾上腺素。在预先用³H - 去甲肾上腺素加载的基底动脉、肠系膜动脉和肾动脉中,可乐定(10⁻¹⁰ - 10⁻⁷M)可减弱电透壁刺激诱导的³H流出,而去氧肾上腺素(10⁻¹⁰ - 10⁻⁸M)则无此作用。与外周动脉相比,育亨宾在比育亨宾低得多的浓度下就能增加电刺激引起的³H流出。这些结果表明,犬基底动脉的突触前和突触后α受体主要是α₂型,与外周动脉的α受体不同。

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