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兔离体脾动脉中多巴胺受体的特征

Characteristics of the dopamine receptors in the rabbit isolate splenic artery.

作者信息

Hilditch A, Drew G M

出版信息

Eur J Pharmacol. 1981 Jul 10;72(4):287-96. doi: 10.1016/0014-2999(81)90566-5.

Abstract

After blockade of alpha- and beta-adrenoceptors, the tension induced by PGF2alpha in splenic artery strips was relaxed by dopamine, 6, 7-ADTN, N-methyldopamine, apomorphine, N, N-di-n-propyl 5, 6-ADTN, N, N-di-n-propyl 6, 7-ADTN and Sandoz 27-403; their equipotent concentrations (relative to dopamine = 1) were 0.2: 0.3: 0.4: 1.1: 3.9 and 3.9 respectively. 5, 6 ADTN, N-methyl 5,6ADTN, N, N-diethyldopamine, N, N-di-n-propyldopamine and SKF 38393 were weakly active or inactive at relaxing the splenic artery strip. Bulbocapnine and cis-alpha-flupenthixol were specific, competitive, reversible antagonists of dopamine. Fluphenazine, clozapine, trifluoperazine, haloperidol and spiroperidol also antagonised dopamine, but were relatively weak antagonists and a small part of their action was non-specific. Sulpiride was inactive against dopamine. SKF 38393 selectively antagonised the effects of dopamine demonstrating that SKF 38393 has affinity, but little efficacy at the dopamine receptors in the splenic artery. The findings with both agonists and antagonists suggest that the vascular dopamine receptors in the rabbit splenic artery resemble those in the dog renal and mesenteric vascular beds.

摘要

在阻断α和β肾上腺素能受体后,多巴胺、6,7 - ADTN、N - 甲基多巴胺、阿扑吗啡、N,N - 二正丙基5,6 - ADTN、N,N - 二正丙基6,7 - ADTN和山德士27 - 403可使PGF2α在脾动脉条带中诱导产生的张力松弛;它们的等效浓度(相对于多巴胺 = 1)分别为0.2:0.3:0.4:1.1:3.9和3.9。5,6 - ADTN、N - 甲基5,6 - ADTN、N,N - 二乙基多巴胺、N,N - 二正丙基多巴胺和SKF 38393在松弛脾动脉条带方面活性较弱或无活性。荷包牡丹碱和顺式 - α - 氟哌噻吨是多巴胺的特异性、竞争性、可逆性拮抗剂。氟奋乃静、氯氮平、三氟拉嗪、氟哌啶醇和螺哌利多也拮抗多巴胺,但它们是相对较弱的拮抗剂,且其作用的一小部分是非特异性的。舒必利对多巴胺无活性。SKF 38393选择性地拮抗多巴胺的作用,表明SKF 38393对脾动脉中的多巴胺受体具有亲和力,但效能较低。激动剂和拮抗剂的研究结果均表明,兔脾动脉中的血管多巴胺受体与犬肾和肠系膜血管床中的相似。

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