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The specific opioid kappa-agonist U-50,488H inhibits low Km GTPase.

作者信息

Ueda H, Misawa H, Fukushima N, Takagi H

出版信息

Eur J Pharmacol. 1987 Jun 12;138(1):129-32. doi: 10.1016/0014-2999(87)90348-7.

DOI:10.1016/0014-2999(87)90348-7
PMID:3040426
Abstract

DAGO, a specific opioid mu-agonist stimulated the low Km GTPase activity of membranes of the guinea-pig striatum at 1-1000 nM and this effect was antagonized by naloxone 10-100 nM. On the other hand, U-50,488H, a specific opioid kappa-agonist inhibited the low Km GTPase activity of membranes of the guinea-pig cerebellum at 1-100 nM. As this effect was antagonized by MR2266 but not by naloxone, the findings suggest that opioid mu- and kappa-receptor stimulation is probably linked to the stimulation and inhibition of low Km GTPase, respectively.

摘要

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引用本文的文献

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Reconstitution of rat brain mu opioid receptors with purified guanine nucleotide-binding regulatory proteins, Gi and Go.用纯化的鸟嘌呤核苷酸结合调节蛋白Gi和Go对大鼠脑μ阿片受体进行重组。
Proc Natl Acad Sci U S A. 1988 Sep;85(18):7013-7. doi: 10.1073/pnas.85.18.7013.