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Title: Chronic morphine upregulates a mu-opiate binding site labeled by [3H]cycloFOXY: a novel opiate antagonist suitable for positron emission tomography. Author: Rothman RB, McLean S, Bykov V, Lessor RA, Jacobson AE, Rice KC, Holaday JW. Journal: Eur J Pharmacol; 1987 Oct 06; 142(1):73-81. PubMed ID: 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.[Abstract] [Full Text] [Related] [New Search]