Stereospecificity of 2,4-diaminobutyric acid with respect to inhibition of 4-aminobutyric acid uptake and binding.

British journal of pharmacology ·Vol. 59 ·No. 1 ·1977-01-00 ·Pages 218-9

Johnston GA, Twitchin B

Abstract

S(+)-2,4-Diaminobutyric acid is at least 20 times more potent than the R(-) stereoisomer as an inhibitor of the sodium-dependent uptake of 4-aminobutyric acid (GABA) in rat brain slices. Both isomers, however, are equipotent as inhibitors of sodium-independent binding of GABA to membranes from rat brain. The latter finding may be relevant to the reported neurotoxicity in rats of both isomers of 2,4-diaminobutyric acid after intracisternal injection.

MeSH Terms

Aminobutyrates/metabolism,pharmacology Animals Biological Transport Brain/drug effects,metabolism In Vitro Techniques Rats Stereoisomerism Structure-Activity Relationship gamma-Aminobutyric Acid/metabolism

Chemicals

Aminobutyrates gamma-Aminobutyric Acid

Authors & Affiliations

2 authors, click to expand affiliations / ORCID

Johnston G A

Twitchin B

References (14)

14 references, click to expand

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The effects of L-2,4-diaminobutyric acid on the uptake of gamma-aminobutyric acid by a synaptosomal fraction from rat brain.
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Effect of centrally acting drugs on the uptake of gamma-aminobutyric acid (GABA) by slices of rat cerebral cortex.
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Competitive inhibition of GABA uptake in rat brain slices by some GABA analogues of restricted conformation.
J Neurochem. 1972 Aug;19(8):1855-61 PMID: 5047849
The in vivo inactivation of GABA and other inhibitory amino acids in the cat nervous system.
Exp Brain Res. 1976 Jun 30;25(4):413-28 PMID: 954900
Indirect effects of amino-acids on sympathetic ganglion cells mediated through the release of gamma-aminobutyric acid from glial cells.
Br J Pharmacol. 1976 May;57(1):73-91 PMID: 1276543
Transport of L-proline by rat brain slices.
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Uptake and metabolism of gamma-aminobutyric acid by neurones and glial cells.
Biochem Pharmacol. 1975 May 1;24(9):933-8 PMID: 1156449
GABA uptake in rat central nervous system: comparison of uptake in slices and homogenates and the effects of some inhibitors.
J Neurochem. 1971 Oct;18(10):1939-50 PMID: 5118346
Determination of gamma-aminobutyric acid and other free amino acids in whole brains of rats poisoned with beta, beta'-iminodipropionitrile and alpha, gamma-diaminobutyric acid with, or without, administration of thyroxine.
J Neurochem. 1966 Dec;13(12):1461-7 PMID: 5962024
The excitation and depression of spinal neurones by structurally related amino acids.
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Elevation of brain gamma-aminobutyric acid in the mouse by L-2,4-diaminobutyric acid.
Trans Am Neurol Assoc. 1974;99:49-51 PMID: 4156893
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Article Info

Journal

British journal of pharmacology

Abbr.

Br J Pharmacol

ISSN

0007-1188

DOI

10.1111/j.1476-5381.1977.tb06998.x

Published

1977-01-00

Pages

218-9

Language

English

Region

England

NLM ID

7502536

PMCID

PMC1667714

Subset

External Links

PubMed source DOI: 10.1111/j.1476-5381.1977.tb06998.x PMC Full Text View journal details

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Stereospecificity of 2,4-diaminobutyric acid with respect to inhibition of 4-aminobutyric acid uptake and binding.

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