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介导去甲肾上腺素引起豚鼠主动脉收缩的α1-肾上腺素能受体亚型

Alpha 1-adrenoceptor subtype(s) mediating noradrenaline-induced contractions of the guinea-pig aorta.

作者信息

Oriowo M A

机构信息

Department of Pharmacology & Toxicology, Faculty of Medicine, Kuwait University, Safat.

出版信息

Fundam Clin Pharmacol. 1994;8(3):214-9. doi: 10.1111/j.1472-8206.1994.tb00801.x.

Abstract

The effect of alpha 1-adrenoceptor subtype selective antagonists, WB 4101, SZL-49 and chloroethylclonidine on noradrenaline-induced contractions of the guinea-pig aorta has been studied in an attempt to identify the alpha 1-adrenoceptor subtype(s) involved in the response. Noradrenaline and SDZ NVI 085 induced contractions of the aorta. Noradrenaline-induced contractions were competitively antagonised by WB 4101 (pA2 = 8.92, slope = 1.05). The contractions were significantly reduced by SZL-49 but not by chloroethylclonidine, indicating an action on alpha 1A-adrenoceptor subtype. Noradrenaline-induced contractions of the aorta were not inhibited by nifedipine (10(-6) M). The results are interpreted to suggest that alpha 1A-adrenoceptor subtype mediates noradrenaline-induced contractions of the guinea-pig aorta and that activation of alpha 1A-adrenoceptor subtype in the guinea-pig aorta is probably linked to intracellular Ca++ release.

摘要

研究了α1-肾上腺素能受体亚型选择性拮抗剂WB 4101、SZL-49和氯乙可乐定对去甲肾上腺素诱导的豚鼠主动脉收缩的影响,以试图确定参与该反应的α1-肾上腺素能受体亚型。去甲肾上腺素和SDZ NVI 085诱导主动脉收缩。WB 4101竞争性拮抗去甲肾上腺素诱导的收缩(pA2 = 8.92,斜率 = 1.05)。SZL-49可显著降低收缩,但氯乙可乐定则无此作用,表明其作用于α1A-肾上腺素能受体亚型。硝苯地平(10(-6) M)不抑制去甲肾上腺素诱导的主动脉收缩。结果表明,α1A-肾上腺素能受体亚型介导去甲肾上腺素诱导的豚鼠主动脉收缩,并且豚鼠主动脉中α1A-肾上腺素能受体亚型的激活可能与细胞内Ca++释放有关。

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