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通过放射受体分析法测定的阿片类镇痛药的血浆水平。

Plasma levels of opioid analgesics determined by radioreceptor assay.

作者信息

Ensinger H A, Doevendans J E

出版信息

Arzneimittelforschung. 1984;34(5):609-13.

PMID:6540579
Abstract

Plasma levels of opioid drugs, Mr 1268 MS (3-(2-methyl-3-furylmethyl)-1,2,3,4,5,6-hexahydro-6 alpha,11 alpha-dimetyl-2,6-methano-3-benzazocin-8-ol methane sulfonate), Mr 2033 CL ( [2 alpha, 3(S*), 6 alpha, 11 R*]-(+/-)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-[(tetrahydro-2-furanyl) methyl]-2,6-methano-3-benzazocin-8-ol hydrochloride), MRZ 2549 BR ( (2-methoxypropyl)-1,2,3,4,5,6-hexahydro-6 alpha, 11 alpha-dimethyl-2,6-methano-3-benzazocin-8-ol hydrobromide), and pentazocine, have been determined by a radioreceptor assay after enteral and parenteral administration to human volunteers as well as to laboratory animals (monkeys and dogs), using [3H]dihydromorphine as radioligand and freshly prepared membrane homogenates of rat brains. The concentration of parent compound drug has been evaluated after a specific extraction from plasma. The method described presents a universal possibility for the determination of opioid drugs of different structures in plasma and other body fluids.

摘要

在给人类志愿者以及实验动物(猴子和狗)经肠内和非肠道给药后,使用[3H]二氢吗啡作为放射性配体以及新鲜制备的大鼠脑匀浆膜,通过放射受体分析法测定了阿片类药物、Mr 1268 MS(3-(2-甲基-3-呋喃基甲基)-1,2,3,4,5,6-六氢-6α,11α-二甲基-2,6-亚甲基-3-苯并氮杂环辛-8-醇甲磺酸盐)、Mr 2033 CL([2α, 3(S*), 6α, 11 R*]-(±)-1,2,3,4,5,6-六氢-6,11-二甲基-3-[(四氢-2-呋喃基)甲基]-2,6-亚甲基-3-苯并氮杂环辛-8-醇盐酸盐)、MRZ 2549 BR((2-甲氧基丙基)-1,2,3,4,5,6-六氢-6α, 11α-二甲基-2,6-亚甲基-3-苯并氮杂环辛-8-醇氢溴酸盐)和喷他佐辛在血浆中的水平。从血浆中进行特定提取后,对母体化合物药物的浓度进行了评估。所描述的方法为测定血浆和其他体液中不同结构的阿片类药物提供了一种通用的可能性。

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