Document Detail

GABA(B) auto- versus hetero-receptor sensitivity: implications for novel pharmacotherapy.
MedLine Citation:
PMID:  10587096     Owner:  NLM     Status:  MEDLINE    
After uncoupling G-protein dependent post-synaptic GABA(B) receptors--without altering GABA(B) nerve terminal receptors--we demonstrate that the GABA(B) agonist, CGP44533, exhibits less efficacy and potency at GABA(B) auto- versus hetero-receptors. CGP44533 (1 and 10 microM) depressed monosynaptic GABA(A)-mediated transmission by 2 and 35%, but depressed glutamate mediated transmission by 41 and 78%, respectively. These data suggest a differential pharmacological sensitivity for CGP44533 at glutamate versus GABA releasing neurons.
B Yu; K Yamada; J P Gallagher
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Neuropharmacology     Volume:  38     ISSN:  0028-3908     ISO Abbreviation:  Neuropharmacology     Publication Date:  1999 Nov 
Date Detail:
Created Date:  1999-12-20     Completed Date:  1999-12-20     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  0236217     Medline TA:  Neuropharmacology     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1805-9     Citation Subset:  IM    
Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston 77555-1031, USA.
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MeSH Terms
Autoreceptors / drug effects*,  metabolism
GABA Agonists / pharmacology*
Glutamic Acid / drug effects,  metabolism
Neurons / drug effects*,  metabolism
Patch-Clamp Techniques
Rats, Sprague-Dawley
Receptors, GABA-B / drug effects*,  metabolism
Septal Nuclei / drug effects*,  metabolism
Synaptic Transmission / drug effects*
Reg. No./Substance:
0/Autoreceptors; 0/GABA Agonists; 0/Receptors, GABA-B; 56-86-0/Glutamic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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