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神经节多巴胺受体的生化与药理学特性

Biochemical and pharmacological characterization of ganglionic dopamine receptors.

作者信息

Sabouni M H, Alkadhi K A, Lokhandwala M F

出版信息

Clin Exp Hypertens A. 1987;9(5-6):873-87. doi: 10.3109/10641968709161455.

Abstract

The presence and the subtype of dopamine receptors in sympathetic ganglia were investigated. Using dopamine as well as preferential agonists and antagonists for the DA-1 and DA-2 receptor subtypes, we have studied dopamine receptors in both dog and rat sympathetic ganglia. Dopamine, fenoldopam, a DA-1 receptor agonist, and quinpirole, a DA-2 receptor agonist, caused significant inhibition of ganglionic transmission. The inhibitory action of quinpirole was selectively antagonized by the DA-2 receptor antagonist S-sulpiride but not by the DA-1 receptor antagonist R-sulpiride. In contrast, the inhibition of ganglionic transmission produced by fenoldopam was antagonized by R-sulpiride but not S-sulpiride. The selective DA-1 receptor antagonist, SCH 23390 did not alter the inhibitory effect of fenoldopam at the ganglia. Dopamine and fenoldopam increased vascular but not ganglionic cyclic AMP. The increase in vascular cyclic AMP was antagonized by the DA-1 receptor antagonists SCH 23390 and R-sulpiride. Quinpirole caused a modest but significant decrease in ganglionic cyclic AMP, sensitive to blockade by S-sulpiride. These results show that dopamine and selective DA-1 and DA-2 receptor agonists inhibit ganglionic transmission by activating two distinct subtypes of dopamine receptors located on sympathetic ganglia.

摘要

研究了交感神经节中多巴胺受体的存在及其亚型。使用多巴胺以及DA - 1和DA - 2受体亚型的选择性激动剂和拮抗剂,我们对犬和大鼠的交感神经节中的多巴胺受体进行了研究。多巴胺、非诺多泮(一种DA - 1受体激动剂)和喹吡罗(一种DA - 2受体激动剂)均能显著抑制神经节传递。喹吡罗的抑制作用可被DA - 2受体拮抗剂S - 舒必利选择性拮抗,而不能被DA - 1受体拮抗剂R - 舒必利拮抗。相反,非诺多泮对神经节传递的抑制作用可被R - 舒必利拮抗,而不能被S - 舒必利拮抗。选择性DA - 1受体拮抗剂SCH 23390不会改变非诺多泮对神经节的抑制作用。多巴胺和非诺多泮可增加血管而非神经节中的环磷酸腺苷(cAMP)。血管中cAMP的增加可被DA - 1受体拮抗剂SCH 23390和R - 舒必利拮抗。喹吡罗可使神经节中的cAMP适度但显著降低,且对S - 舒必利的阻断敏感。这些结果表明,多巴胺以及选择性DA - 1和DA - 2受体激动剂通过激活位于交感神经节上的两种不同亚型的多巴胺受体来抑制神经节传递。

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