sigma配体对非洲爪蟾卵母细胞中与g蛋白激活K+ (GIRK)通道共表达的mu-、delta-和kappa-阿片受体的影响

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小林T，池田K，市川T, Togashi S，熊西T

sigma配体对非洲爪蟾卵母细胞中与g蛋白激活K+ (GIRK)通道共表达的mu-、delta-和kappa-阿片受体的影响

中华药物学杂志，1999,9(1):73-80。

PubMed ID

8872359 (PubMed视图

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摘要

1.利用阿片受体与g蛋白激活的K+ (GIRK)通道的功能偶联，我们研究了不同结构和药理类别的sigma配体，(+)- n-烯丙基正美唑辛((+)- skf10047)和(+)-环唑辛，(+)-3-(3-羟基苯基)- n-(1-丙基)哌啶((+)- 3ppp)， 1,3-二-(2-托利基)胍(DTG)， carbetapentane和氟哌啶醇对与克隆mu-共注射的非洲狐猴卵母细胞内K+电流响应的影响。delta和kappa阿片受体mRNA和GIRK1 mRNA。2.(+)- skf10047作为delta和kappa激动剂(EC50值(microM)分别为0.618和0.652)和mu-拮抗剂(IC50值(microM) = 8.51)。(+)-环唑辛作为kappa-激动剂和mu-拮抗剂(IC50 = 33.2)。(+)-3PPP作为kappa激动剂(EC50 = 18.08)和mu-拮抗剂。DTG作为mu和kappa激动剂(EC50分别大于30和14.88)。卡betapantane作为kappa激动剂和mu-拮抗剂(IC50 = 11.2)。氟哌啶醇作为mu和delta激动剂(EC50分别为5.683和7.389)。 3. All currents induced by sigma ligands were reduced by 1 microM naloxone, an opioid receptor antagonist, and blocked by 300 microM Ba2+, a GIRK channel blocker. It was also indicated that the antagonism by naloxone at the delta-- and kappa-opioid receptors was weaker than that of naloxone at the mu-opioid receptor. The sigma ligands tested had no effect on the current responses in the oocytes injected with each of the opioid receptor mRNAs alone or with the GIRK1 mRNA alone. 4. We conclude that various sigma ligands directly interact with the cloned mu-, delta- and kappa-opioid receptors in Xenopus oocytes. Our results suggest that the effects of the sigma ligands may be partly mediated by the opioid receptors.

引用本文的药物库数据

药物靶点

药物	目标	种类	生物	药理作用	行动
Pentoxyverine	kappa型阿片受体	蛋白质	人类	未知的	受体激动剂	细节
Pentoxyverine	mu型阿片受体	蛋白质	人类	未知的	拮抗剂	细节