| Action of 4-amino-2-fluorobutanoic acid and other structural analogues on gamma-aminobutyric acid transport by channel catfish brain. | |
| | |
MedLine Citation:
|
PMID: 12670027 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Gamma-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in mammalian brain. The synaptic action of GABA is terminated by a sodium- and chloride-linked transport system. The GABA transporter is known as GAT and several isoforms have been identified. Many components of a GABA neurotransmitter system, including a GABA transport system, are present in channel catfish brain. Using a synaptosomal preparation of catfish brain, we examined the kinetics of inhibition of GABA transport by 4-amino-2-fluorobutanoic acid and several other structural analogues of GABA. The transport constant (Kt) for GABA uptake was 4.46 microM, and 4-amino-2-fluorobutanoic acid produced a noncompetitive type of inhibition (Ki = 12.5 microM). The most potent inhibitors were tiagabine (Ki = 0.23 microM) and (R,S)nipecotic acid (Ki = 2.2 microM), both of which exhibited competitive inhibition. Like 4-amino-2-fluorobutanoic acid, homo-beta-proline (Ki = 9.4 microM) inhibited noncompetitively. Other analogues exhibited competitive inhibition. These observations suggest that the GABA transport system in channel catfish is remarkably similar to that in mammalian brain. |
| | |
Authors:
|
Glenda J Crites; Linda A Malizia; Godfrey Tunnicliff |
Related Documents
:
|
21163157 - Alkaptonuria. 6539767 - Peptide antibiotic k-582 production in relation to amino acid metabolism in metarrhiziu... 3550527 - Immunocytochemical localization of gaba in cat myenteric plexus. 20467257 - Effects of ultra high molecular weight poly-gamma-glutamic acid from bacillus subtilis ... 14621397 - Hypocalcaemia and dcad for the pasture-based transition cow--a review. 12215187 - Improvement of the probiotic effect of micro-organisms by their combination with maltod... |
Publication Detail:
|
Type: In Vitro; Journal Article |
Journal Detail:
|
Title: Journal of basic and clinical physiology and pharmacology Volume: 13 ISSN: 0792-6855 ISO Abbreviation: J Basic Clin Physiol Pharmacol Publication Date: 2002 |
Date Detail:
|
Created Date: 2003-04-02 Completed Date: 2003-10-06 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 9101750 Medline TA: J Basic Clin Physiol Pharmacol Country: England |
Other Details:
|
Languages: eng Pagination: 179-92 Citation Subset: IM |
Affiliation:
|
Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Evansville, IN 47712, USA. gtunnic@iupui.edu |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Biological Transport, Active / drug effects Brain Chemistry / drug effects* Chlorides / metabolism GABA Antagonists / pharmacology* Ictaluridae / metabolism* Nerve Tissue Proteins / metabolism Sodium / metabolism, pharmacology Sodium Channels / drug effects, metabolism Temperature gamma-Aminobutyric Acid / analogs & derivatives*, metabolism*, pharmacology* |
| Chemical | |
Reg. No./Substance:
|
0/4-amino-2-fluorobutanoic acid; 0/Chlorides; 0/GABA Antagonists; 0/Nerve Tissue Proteins; 0/Sodium Channels; 56-12-2/gamma-Aminobutyric Acid; 7440-23-5/Sodium |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Genetic differentiation within metapopulations of Euphydryas aurinia and Melitaea phoebe in China.
Next Document: In vitro effects of dantrolene sodium and verapamil on noradrenaline-induced contractions of rabbit ...