2 DOPAMINE-RECEPTORS - BIOCHEMISTRY, PHYSIOLOGY AND PHARMACOLOGY
2 DOPAMINE-RECEPTORS - BIOCHEMISTRY, PHYSIOLOGY AND PHARMACOLOGY
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DOI：
10.1016/0024-3205(84)90519-8
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发表时间：
1984-01-01
期刊：
影响因子：
6.1
通讯作者：
KEBABIAN, JW
中科院分区：
文献类型：
--
作者：
STOOF, JC;KEBABIAN, JW
1979年，基于有限数量的激动剂和拮抗剂区分这两种实体的能力，确定了两类多巴胺（DA）受体（指定为D-1和D-2）。在过去的5年中，已经鉴定了对每类受体具有选择性的激动剂和拮抗剂。使用这些选择性药物，它已经有可能属性的生理和生化过程中的DA的影响，刺激D-1或D-2受体。因此，DA诱导的增强牛甲状旁腺的激素释放和放电的神经分泌细胞在CNS中的滞流神经节已被归因于D-1受体的刺激。DA对垂体催乳素和α-MSH的释放以及脑内乙酰胆碱、DA和β-内啡肽的释放也有抑制作用，DA对家兔颈动脉体化学感觉放电的抑制作用和DA引起的滞水蛙中枢神经系统神经分泌细胞的超极化作用均归因于D-2受体的兴奋作用，DA-1和DA-2在心血管系统中被鉴定。DA-1受体的刺激增加血管环AMP含量并引起肾血管中血管平滑肌的松弛，而DA-2受体的刺激抑制去甲肾上腺素从某些节后交感神经元的释放。然而，最近对区分D-1和D-2受体的新开发药物的研究表明，中枢神经和内分泌系统或心血管系统中多巴胺受体分类的独立开发的图式是相似的，尽管可能不完全相同。
In 1979, two categories of dopamine (DA) receptors (designated as D-1 and D-2) were identified on the basis of the ability of a limited number of agonists and antagonists to discriminate between these two entities. In the past 5 years agonists and antagonists selective for each category of receptor have been identified. Using these selective drugs it has been possible to attribute the effects of DA upon physiological and biochemical processes to the stimulation of either a D-1 or a D-2 receptor. Thus, DA-induced enhancement of both hormone release from bovine parathyroid gland and firing of neurosecretory cells in the CNS of Lymnaea stagnalis has been attributed to stimulation of a D-1 receptor. Likewise, the DA-induced inhibition of the release of prolactin andα-MSH from the pituitary gland, as well as of acetylcholine, DA and β-endorphin from brain, the DA-induced inhibition of chemo-sensory discharge in rabbit carotid body and the DA-induced hyperpolarization of neurosecretory cells in the CNS of Lymnaea stagnalis have been attributed to stimulation of a D-2 receptor.Independently two categories of DA receptors (designated as DA-1 and DA-2) were identified in the cardiovascular system. Stimulation of a DA-1 receptor increases the vascular cyclic AMP content and causes a relaxation of vascular smooth muscle in renal blood vessels, whereas stimulation of a DA-2 receptor inhibits the release of norepinephrine from certain postganglionic sympathetic neurons. Recent studies with the newly developed drugs discriminating between D-1 and D-2 receptors suggest however that the independently developed schemata for classification of dopamine receptors in either the central nervous and endocrine systems or the cardiovascular system are similar although maybe not completely identical.