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μ、δ和κ阿片受体激动剂对腺苷酸环化酶活性的不同作用。

Differential effect of mu, delta, and kappa opioid agonists on adenylate cyclase activity.

作者信息

De Montis G M, Devoto P, Preti A, Tagliamonte A

出版信息

J Neurosci Res. 1987;17(4):435-9. doi: 10.1002/jnr.490170416.

DOI:10.1002/jnr.490170416
PMID:2887665
Abstract

D-Ala2, D-Leu5-enkephalin (DADLE) and dynorphin1-13 (Dyn1-13) inhibited striatal adenylate cyclase activity, both basal and dopamine-stimulated (DA), in rats and guinea pigs. The kappa-agonists bremazocine (BRZ), U-50,488 (trans-3,4-dicloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide), and U-69,593 (5 alpha, 7 alpha 8 beta)-(-)-N-methyl-N-(7-(1-pyrrolidinyl-1-oxaspiro (4.5)dec-8yl) benzeneacetamide inhibited only the basal adenylate cyclase activity, and such an effect was restricted to guinea pig striatum, an area known to contain a high density of kappa-binding sites. Moreover, BRZ was found to antagonize the inhibitory effect of both DADLE and Dyn1-13 in rat striatum.

摘要

D-丙氨酸2、D-亮氨酸5-脑啡肽(DADLE)和强啡肽1-13(Dyn1-13)抑制大鼠和豚鼠纹状体腺苷酸环化酶活性,包括基础活性和多巴胺刺激的活性。κ激动剂布马佐辛(BRZ)、U-50,488(反式-3,4-二氯-N-甲基-N-[2-(1-吡咯烷基)-环己基]-苯乙酰胺)和U-69,593(5α,7α,8β)-(-)-N-甲基-N-(7-(1-吡咯烷基-1-氧杂螺(4.5)癸-8基)苯乙酰胺仅抑制基础腺苷酸环化酶活性,且这种作用仅限于豚鼠纹状体,该区域已知含有高密度的κ结合位点。此外,发现BRZ可拮抗DADLE和Dyn1-13对大鼠纹状体的抑制作用。

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Differential effect of mu, delta, and kappa opioid agonists on adenylate cyclase activity.μ、δ和κ阿片受体激动剂对腺苷酸环化酶活性的不同作用。
J Neurosci Res. 1987;17(4):435-9. doi: 10.1002/jnr.490170416.
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Bremazocine differentially antagonizes responses to selective mu and delta opioid receptor agonists in rat hippocampus.布瑞马佐辛对大鼠海马体中选择性μ和δ阿片受体激动剂的反应具有差异性拮抗作用。
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J Med Chem. 1990 Apr;33(4):1171-6. doi: 10.1021/jm00166a014.

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