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Title: In vivo (/sup 3/H)flunitrazepam binding: imaging of receptor regulation

Abstract

The use of (/sup 3/H)flunitrazepam as a ligand to measure alterations in benzodiazepine receptors in vivo in rats was investigated. Animals were injected with (/sup 3/H)flunitrazepam i.v., arterial samples of (/sup 3/H)flunitrazepam were obtained and, later, the animals were sacrificed to assay brain binding. (/sup 3/H)flunitrazepam enters the brain rapidly and binds to benzodiazepine receptors. About two-thirds of this binding is blocked by predosing the animals with 5 mg/kg of clonazepam. The amount of remaining (nonspecific) binding correlates very well (r = 0.88) with the amount of radioactivity found in plasma at the time of death. A series of rats were lesioned unilaterally with kainic acid in the caudate-putamen several months before the infusion of (/sup 3/H)flunitrazepam. In vivo autoradiography in lesioned rats showed that benzodiazepine binding in globus pallidus and substantia nigra on the side of the lesion was increased significantly as compared to the intact side. The observed changes in benzodiazepine binding were similar to those observed previously in lesioned rats using in vitro techniques. Thus, benzodiazepine receptor regulation can be imaged quantitatively using in vivo binding techniques.

Authors:
; ;
Publication Date:
Research Org.:
Univ. of Michigan, Ann Arbor
OSTI Identifier:
5098009
Resource Type:
Journal Article
Journal Name:
J. Pharmacol. Exp. Ther.; (United States)
Additional Journal Information:
Journal Volume: 2
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; TRANQUILIZERS; RADIORECEPTOR ASSAY; AUTORADIOGRAPHY; BRAIN; LIGANDS; RATS; RECEPTORS; TRITIUM COMPOUNDS; ANIMALS; BODY; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; DRUGS; ISOTOPE APPLICATIONS; LABELLED COMPOUNDS; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; ORGANIC COMPOUNDS; ORGANS; PROTEINS; PSYCHOTROPIC DRUGS; RODENTS; TRACER TECHNIQUES; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Ciliax, B J, Penney, Jr, J B, and Young, A B. In vivo (/sup 3/H)flunitrazepam binding: imaging of receptor regulation. United States: N. p., 1986. Web.
Ciliax, B J, Penney, Jr, J B, & Young, A B. In vivo (/sup 3/H)flunitrazepam binding: imaging of receptor regulation. United States.
Ciliax, B J, Penney, Jr, J B, and Young, A B. 1986. "In vivo (/sup 3/H)flunitrazepam binding: imaging of receptor regulation". United States.
@article{osti_5098009,
title = {In vivo (/sup 3/H)flunitrazepam binding: imaging of receptor regulation},
author = {Ciliax, B J and Penney, Jr, J B and Young, A B},
abstractNote = {The use of (/sup 3/H)flunitrazepam as a ligand to measure alterations in benzodiazepine receptors in vivo in rats was investigated. Animals were injected with (/sup 3/H)flunitrazepam i.v., arterial samples of (/sup 3/H)flunitrazepam were obtained and, later, the animals were sacrificed to assay brain binding. (/sup 3/H)flunitrazepam enters the brain rapidly and binds to benzodiazepine receptors. About two-thirds of this binding is blocked by predosing the animals with 5 mg/kg of clonazepam. The amount of remaining (nonspecific) binding correlates very well (r = 0.88) with the amount of radioactivity found in plasma at the time of death. A series of rats were lesioned unilaterally with kainic acid in the caudate-putamen several months before the infusion of (/sup 3/H)flunitrazepam. In vivo autoradiography in lesioned rats showed that benzodiazepine binding in globus pallidus and substantia nigra on the side of the lesion was increased significantly as compared to the intact side. The observed changes in benzodiazepine binding were similar to those observed previously in lesioned rats using in vitro techniques. Thus, benzodiazepine receptor regulation can be imaged quantitatively using in vivo binding techniques.},
doi = {},
url = {https://www.osti.gov/biblio/5098009}, journal = {J. Pharmacol. Exp. Ther.; (United States)},
number = ,
volume = 2,
place = {United States},
year = {Fri Aug 01 00:00:00 EDT 1986},
month = {Fri Aug 01 00:00:00 EDT 1986}
}