慢性吗啡上调由[3H]环FOXY标记的μ-阿片受体结合位点：一种适用于正电子发射断层扫描的新型阿片拮抗剂。

Chronic morphine upregulates a mu-opiate binding site labeled by [3H]cycloFOXY: a novel opiate antagonist suitable for positron emission tomography.

作者信息

Rothman R B, McLean S, Bykov V, Lessor R A, Jacobson A E, Rice K C, Holaday J W

机构信息

Laboratory of Preclinical Pharmacology, St. Elizabeths Hospital, NIMH, Washington, DC 20032.

出版信息

Eur J Pharmacol. 1987 Oct 6;142(1):73-81. doi: 10.1016/0014-2999(87)90655-8.

DOI:10.1016/0014-2999(87)90655-8

PMID:2826178

Abstract

CycloFOXY (17-cyclopropylmethyl-3,14-dihydroxy-4,5-alpha-epoxy-6-beta- fluoromorphinan) is a novel opiate antagonist synthesized as a ligand suitable for in vivo visualization of opiate receptors using positron emission transaxial tomography. In this paper we report that [3H]cycloFOXY labels two distinct opiate binding sites in rat brain membranes, tentatively identified as mu and kappa. Furthermore, chronic administration of morphine results in a selective up-regulation of the mu binding site. The implications of this finding for models of the opioid receptors and the mechanism of the sodium effect are discussed.

摘要

环福可昔（17 - 环丙基甲基 - 3,14 - 二羟基 - 4,5 - α - 环氧 - 6 - β - 氟吗啡喃）是一种新型阿片类拮抗剂，它被合成作为一种配体，适用于使用正电子发射断层扫描在体内可视化阿片受体。在本文中，我们报告[3H]环福可昔标记大鼠脑膜中两个不同的阿片结合位点，初步鉴定为μ和κ。此外，长期给予吗啡会导致μ结合位点的选择性上调。本文讨论了这一发现对阿片受体模型和钠效应机制的意义。