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M-1和M-2毒蕈碱受体介导的大鼠新纹状体中对多巴胺敏感的腺苷酸环化酶的抑制作用:D-2多巴胺受体的许可作用

M-1 and M-2 muscarinic receptor-mediated inhibition of dopamine-sensitive adenylate cyclase in rat neostriatum: a permissive role for D-2 dopamine receptors.

作者信息

Schoffelmeer A N, Hogenboom F, Mulder A H

机构信息

Department of Pharmacology, Free University, Amsterdam, The Netherlands.

出版信息

J Pharmacol Exp Ther. 1988 May;245(2):658-63.

PMID:2452877
Abstract

The interactions between dopamine and muscarinic receptor subtypes coupled to adenylate cyclase in superfused rat neostriatal slices were investigated using the efflux of cyclic AMP, in the presence of the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine, as a highly sensitive parameter of cyclic AMP production. Cyclic AMP efflux induced by simultaneous activation of (stimulatory) D-1 and (inhibitory) D-2 dopamine receptors by dopamine was reduced profoundly by the muscarinic receptor agonist oxotremorine and by inhibition of acetylcholinesterase with physostigmine, but not by the M-1 muscarinic receptor agonist McN-A-343. In contrast, upon blockade of D-2 receptors with (-)-sulpiride, dopamine-stimulated cyclic AMP efflux was inhibited by oxotremorine and physostigmine as well as by McN-A-343. Cyclic AMP efflux induced by isoprenaline, adenosine or vasoactive intestinal peptide was not affected by oxotremorine. The M-1 receptor-selective antagonist pirenzepine, unlike the nonselective antagonist atropine, was about 10 times less potent in antagonizing the inhibitory effects of (a near-maximally effective concentration of) oxotremorine upon simultaneous D-1 and D-2 receptor activation that upon selective D-1 receptor activation (i.e., upon blockade of D-2 receptors). In the latter case, pirenzepine was about 5 times more effective as an antagonist when muscarinic receptors were activated by McN-A-343 than upon exposure of the slices to oxotremorine or physostigmine, whereas the potency of atropine was independent of the agonist used.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在磷酸二酯酶抑制剂3-异丁基-1-甲基黄嘌呤存在的情况下,使用环磷酸腺苷(cAMP)流出作为cAMP产生的高敏感参数,研究了多巴胺与灌注大鼠新纹状体切片中与腺苷酸环化酶偶联的毒蕈碱受体亚型之间的相互作用。多巴胺同时激活(刺激性)D-1和(抑制性)D-2多巴胺受体所诱导的cAMP流出,被毒蕈碱受体激动剂氧化震颤素以及用毒扁豆碱抑制乙酰胆碱酯酶显著降低,但不受M-1毒蕈碱受体激动剂McN-A-343的影响。相反,在用(-)-舒必利阻断D-2受体后,氧化震颤素、毒扁豆碱以及McN-A-343均可抑制多巴胺刺激的cAMP流出。异丙肾上腺素、腺苷或血管活性肠肽所诱导的cAMP流出不受氧化震颤素的影响。与非选择性拮抗剂阿托品不同,M-1受体选择性拮抗剂哌仑西平在拮抗(接近最大有效浓度的)氧化震颤素对同时激活D-1和D-2受体的抑制作用时,其效力比对选择性D-1受体激活(即阻断D-2受体时)的抑制作用弱约10倍。在后一种情况下,当毒蕈碱受体由McN-A-343激活时,哌仑西平作为拮抗剂的效力比切片暴露于氧化震颤素或毒扁豆碱时高约5倍,而阿托品的效力与所用激动剂无关。(摘要截短于250字)

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