Separation of peripheral dopamine receptors by a selective DA1 antagonist, SCH 23390.
Separation of peripheral dopamine receptors by a selective DA1 antagonist, SCH 23390.
复制标题
通过选择性 DA1 拮抗剂 SCH 23390 分离外周多巴胺受体。
DOI：
10.1161/01.hyp.6.2_pt_2.i25
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发表时间：
1984
期刊：
影响因子：
--
通讯作者：
Barnett,A
中科院分区：
文献类型：
--
作者：
Goldberg,LI;Glock,D;Kohli,JD;Barnett,A
静脉注射(静脉注射)输注23390.0 5、0.15和0.5微克/kg/(R-(+)-8-chloro-2，3，4，5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-剂量依赖性拮抗多巴胺(DA)所致的肾血管扩张作用。最高的输注速度为0.5微克/公斤/分钟，对这种DA1受体介导的反应产生明显的拮抗作用。相反，高10倍的输注速度，5微克/公斤/分钟，并不能拮抗DA2介导的以下反应：阿朴吗啡和吡贝地尔增加未经治疗的犬的股骨血流量；N，N-二正丙基多巴胺(DPDA)抑制心脏加速器神经刺激产生的心动过速。静脉注射0.5微克/公斤/分钟或更大的SCH 23390不影响α1、α2、β1和β2肾上腺素能、组胺、5羟色胺和胆碱能受体激动剂的作用，也不影响缓激肽产生的血管扩张作用。在这些研究中使用的输液速度下，SCH 23390不影响动脉血压或心率。这些数据表明，SCH 23390是迄今为止所描述的最特异和最有选择性的DA1受体拮抗剂。因此，SCH 23390在研究DA的潜在生理和病理作用以及对DA受体的分类方面应该是非常有用的。
Intravenous (i.v.) infusions of SCH 23390 (R-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7- ol) produced dose-related antagonism of dopamine (DA)-induced renal vasodilation in phenoxybenzamine-treated dogs at infusion rates of 0.05, 0.15, and 0.5 microgram/kg/min. The highest rate of infusion, 0.5 microgram/kg/min, resulted in pronounced antagonism of this DA1-receptor-mediated response. In contrast, a 10 times higher infusion rate, 5 micrograms/kg/min, did not antagonize the following DA2-mediated responses: increase in femoral blood flow produced by apomorphine and piribedil in untreated dogs; and N,N-di-n-propyl DA (DPDA)-induced inhibition of the tachycardia produced by cardiac accelerator nerve stimulation. Infusions of 0.5 micrograms/kg/min or greater of SCH 23390 did not affect the actions of agonists of alpha1-, alpha2-, beta1-, and beta2-adrenergic, histamine, serotonin, and cholinergic receptors, or the vasodilation produced by bradykinin. At the infusion rates used in these studies, SCH 23390 did not affect arterial blood pressure or heart rate. These data indicate that SCH 23390 is the most specific and selective antagonist of DA1 receptors thus far described. Accordingly, SCH 23390 should be extremely useful in investigations of potential physiological and pathological roles of DA and in the classification of DA receptors.