Alcohol interactions with brain opiate receptors.

Alcohol interactions with brain opiate receptors.
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酒精与大脑阿片受体的相互作用。

DOI:
10.1016/0024-3205(83)90031-0
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发表时间:
1983
期刊:
影响因子:
6.1
通讯作者:
Hoffman,PL
Hoffman,PL
中科院分区:
医学2区
文献类型:
--
作者:
Tabakoff,B;Hoffman,PL

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乙醇在体外加入小鼠尾状体膜,在250-1000 mM的乙醇浓度范围内,抑制0.2 nM~3 H-二氢吗啡(~H-DHM)的高亲和力结合。在较低的生理可获得的乙醇浓度(例如:50 mM)下,~H-DHM结合显著增加。在50-1,000 mM浓度范围内,乙醇抑制0.5nM~3H-[D-AlA2,D-Leu5]Enkepha L与小鼠尾状核组织的结合,而无乙醇刺激则以假竞争的方式抑制阿片的结合,因此,用来评价乙醇作用的配基浓度是重要的。用膜不同的其他醇获得的结果:水分配系数表明,酒精对阿片剂结合的影响不仅仅依赖于醇的膜无序性质。
Ethanol, added in vitro to mouse caudate membranes, inhibited high-affinity binding of 0.2 nM 3 H-dihydromorphine (3 H-DHM) over an ethanol concentration range of 250–1,000 mM. At lower, physiologically-attainable ethanol concentrations (eg: 50 mM), 3 H-DHM binding was significantly increased. Over the concentration range of 50–1,000 mM, ethanol inhibited 0.5 nM 3 H-[D-Ala 2, D-Leu 5] enkepha l in (3 H-ENK) binding to mouse caudate tissue, and no stimulation of Ethanol inhibits opiate binding in a pseudo-competitive manner and, therefore, the concentration of ligand used to assess the effects of ethanol is of major importance. Results obtained with other alcohols which differ in their membrane: water partition coefficients suggest that alcohol effects on opiate binding are not solely dependent on the membrane-disordering properties of the alcohols.