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布那唑嗪,一种α1肾上腺素受体阻滞剂,可使犬肠系膜血管中的共递质以不同方式释放。

Bunazosin, an alpha 1-adrenoceptor blocker, differentially releases co-transmitters in dog mesenteric vessels.

作者信息

Komori K, Nagao T, Zhang G L, Ibengwe J K, Fujioka M, Suzuki H

机构信息

Department of Pharmacology, Faculty of Medicine, Kyushu University, Fukuoka, Japan.

出版信息

Eur J Pharmacol. 1989 May 2;164(1):111-20. doi: 10.1016/0014-2999(89)90237-9.

Abstract

The effects of bunazosin on the electrical and mechanical responses of smooth muscle cells elicited by exogenously applied noradrenaline (NA) and by perivascular nerve stimulation were studied in the isolated mesenteric artery and vein of the dog. NA (above 10(-7) M in the artery and above 3 X 10(-8) M in the vein) depolarized the membrane. Perivascular nerve stimulation evoked an excitatory junction potential (e.j.p.) and slow depolarization in both vessels. Bunazosin and prazosin inhibited the NA-induced depolarization and slow depolarization in the artery but not in the vein. The NA actions in the vein were inhibited by yohimbine. Bunazosin (above 10(-6) M) increased the amplitude of the e.j.p. but decreased the outflow of NA during nerve stimulation. The amplitude and conduction velocity of the compound action potential of perivascular nerves were inhibited by higher concentrations of bunazosin (above 10(-5) M). The results provide evidence that bunazosin has selective inhibitory actions at alpha 1-adrenoceptors. This drug exerted differential effects on the release of co-transmitters which generate the e.j.p. and the slow depolarization, as bunazosin increased the former and decreased the latter. This suggests that e.j.p. is generated by a substance other than NA.

摘要

在犬离体肠系膜动脉和静脉中,研究了布那唑嗪对外源性去甲肾上腺素(NA)和血管周围神经刺激所引发的平滑肌细胞电反应和机械反应的影响。NA(在动脉中浓度高于10^(-7) M,在静脉中高于3×10^(-8) M)使细胞膜去极化。血管周围神经刺激在两种血管中均诱发兴奋性接头电位(e.j.p.)和缓慢去极化。布那唑嗪和哌唑嗪抑制动脉中NA诱导的去极化和缓慢去极化,但对静脉无此作用。静脉中的NA作用可被育亨宾抑制。布那唑嗪(高于10^(-6) M)增加e.j.p.的幅度,但在神经刺激期间减少NA的释放。较高浓度的布那唑嗪(高于10^(-5) M)抑制血管周围神经复合动作电位的幅度和传导速度。结果表明布那唑嗪对α1 -肾上腺素能受体具有选择性抑制作用。该药物对产生e.j.p.和缓慢去极化的共递质释放产生不同影响,因为布那唑嗪增加前者而减少后者。这表明e.j.p.不是由NA产生的物质所引起。

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