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Isoguvacine binding, uptake, and release: relation to the GABA system

Journal Article:

Abstract

Isoguvacine (1,2,3,6-tetrahydropyridine-4-carboxylic acid) is a GABA (gamma-aminobutyric acid) agonist with limited conformational flexibility. In these studies we investigated the binding, uptake, and release of (3H) isoguvacine by use of tissue preparations of rat CNS, comparing the results with similar studies of (3H)GABA. The results from these investigations indicate that isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the post-synaptic GABA recognition site; that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA. The ability of isoguvacine and gamma-hydroxybutyric acid to decrease the K+-stimulated Ca2+-dependent release process was also investigated. The results indicate that isoguvacine interactions have many of the biochemical features of GABA synaptic function, isoguvacine being, however, less potent than GABA.
Publication Date:
Jun 01, 1983
Product Type:
Journal Article
Reference Number:
EDB-84-018034
Resource Relation:
Journal Name: J. Neurochem.; (United Kingdom); Journal Volume: 40:6
Subject:
59 BASIC BIOLOGICAL SCIENCES; CENTRAL NERVOUS SYSTEM; RECEPTORS; CALCIUM; CELL MEMBRANES; POTASSIUM; PYRIDINES; RATS; RETENTION; TRITIUM; TRITIUM COMPOUNDS; UPTAKE; ALKALI METALS; ALKALINE EARTH METALS; ANIMALS; AZINES; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; CELL CONSTITUENTS; ELEMENTS; HETEROCYCLIC COMPOUNDS; HYDROGEN ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; LIGHT NUCLEI; MAMMALS; MEMBRANES; METALS; NERVOUS SYSTEM; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; RADIOISOTOPES; RODENTS; VERTEBRATES; YEARS LIVING RADIOISOTOPES; 551001* - Physiological Systems- Tracer Techniques
OSTI ID:
5515222
Research Organizations:
Department of Neuroscience, Children's Hospital Medical Center, Boston, Massachusetts
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: CODEN: JONRA
Submitting Site:
HEDB
Size:
Pages: 1701-1708
Announcement Date:

Journal Article:

Citation Formats

White, W F, and Snodgrass, S R. Isoguvacine binding, uptake, and release: relation to the GABA system. United Kingdom: N. p., 1983. Web.
White, W F, & Snodgrass, S R. Isoguvacine binding, uptake, and release: relation to the GABA system. United Kingdom.
White, W F, and Snodgrass, S R. 1983. "Isoguvacine binding, uptake, and release: relation to the GABA system." United Kingdom.
@misc{etde_5515222,
title = {Isoguvacine binding, uptake, and release: relation to the GABA system}
author = {White, W F, and Snodgrass, S R}
abstractNote = {Isoguvacine (1,2,3,6-tetrahydropyridine-4-carboxylic acid) is a GABA (gamma-aminobutyric acid) agonist with limited conformational flexibility. In these studies we investigated the binding, uptake, and release of (3H) isoguvacine by use of tissue preparations of rat CNS, comparing the results with similar studies of (3H)GABA. The results from these investigations indicate that isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the post-synaptic GABA recognition site; that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA. The ability of isoguvacine and gamma-hydroxybutyric acid to decrease the K+-stimulated Ca2+-dependent release process was also investigated. The results indicate that isoguvacine interactions have many of the biochemical features of GABA synaptic function, isoguvacine being, however, less potent than GABA.}
journal = {J. Neurochem.; (United Kingdom)}
volume = {40:6}
journal type = {AC}
place = {United Kingdom}
year = {1983}
month = {Jun}
}