Effects of morphine glucuronides on the function of opioid receptors in human SK-N-SH cells

被引：15

作者：

Baker, L ^{[1
]}

Dye, A ^{[1
]}

Ratka, A ^{[1
]}

机构：

[1] Idaho State Univ, Coll Pharm, Dept Pharmaceut Sci, Pocatello, ID 83209 USA

来源：

NEUROSCIENCE LETTERS | 2000年 / 281卷 / 01期

关键词：

morphine-6-glucuronide; morphine-3-glucuronide; opioid receptors; cAMP; G-proteins; pertussis toxin; neuroblastoma cells;

D O I：

10.1016/S0304-3940(00)00796-5

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) are active metabolites of morphine. The effects of M3G and M6G on the opioid receptor transduction system has not yet been fully elucidated. Formation of cAMP after treatment with various doses of morphine, M3G, and M6G was studied. M6G and morphine, but not M3G, showed a dose dependent inhibition of cAMP accumulation. Naloxone blocked the inhibitory effect of M6G, M3G, and morphine. Pretreatment with M3G did not change the effects of morphine and M6G, The G-protein inhibitor PTX, prevented morphine, M3G, and M6G effects on cAMP. M3G and M6G vary in their ability to interact with the opioid receptor effector system. Inhibition of cAMP evoked by activation of opioid receptors and inhibitory G-proteins may play a role in the actions of M6G and M3G. (C) 2000 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：1 / 4

页数：4

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