Document Detail


Modulation of antagonist binding to serotonin1A receptors from bovine hippocampus by metal ions.
MedLine Citation:
PMID:  11860184     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. The serotonin1A (5-HT1A) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. They appear to be involved in various behavioral and cognitive functions. Although specific 5-HT1A agonists have been discovered more than a decade back, the development of selective 5-HT1A antagonists has been achieved only recently. 2. We have examined the modulation of the specific antagonist [3H]p-MPPF binding to 5-HT1A receptors from bovine hippocampal membranes by monovalent and divalent metal ions. Our results show that the antagonist binding to 5-HT1A receptors is inhibited by both monovalent and divalent cations in a concentration-dependent manner. This is accompanied by a concomitant reduction in binding affinity. 3. Our results also show that the specific antagonist p-MPPF binds to all available receptors in the bovine hippocampal membrane irrespective of their state of G-protein coupling and other serotonergic ligands such as 5-HT and OH-DPAT effectively compete with the specific antagonist [3H]p-MPPF. 4. These results are relevant to ongoing analyses of the overall modulation of ligand binding in G-protein-coupled seven transmembrane domain receptors.
Authors:
K G Harikumar; A Chattopadhyay
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cellular and molecular neurobiology     Volume:  21     ISSN:  0272-4340     ISO Abbreviation:  Cell. Mol. Neurobiol.     Publication Date:  2001 Oct 
Date Detail:
Created Date:  2002-02-25     Completed Date:  2002-08-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8200709     Medline TA:  Cell Mol Neurobiol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  453-64     Citation Subset:  IM    
Affiliation:
Centre for Cellular and Molecular Biology, Hyderabad, India.
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MeSH Terms
Descriptor/Qualifier:
8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
Aminopyridines / pharmacokinetics
Animals
Cations / pharmacology*
Cattle
Cell Membrane / physiology
Hippocampus / physiology*
Kinetics
Ligands
Magnesium / pharmacology
Manganese / pharmacology
Metals / pharmacology*
Piperazines / pharmacokinetics
Potassium / pharmacology
Receptors, Serotonin / drug effects,  physiology*
Receptors, Serotonin, 5-HT1
Serotonin Antagonists / pharmacokinetics*
Sodium / pharmacology
Chemical
Reg. No./Substance:
0/4-(2' methoxyphenyl)-1-(2'-(N-(2''-pyridinyl)-4-fluorobenzamido)ethyl)piperazine; 0/Aminopyridines; 0/Cations; 0/Ligands; 0/Metals; 0/Piperazines; 0/Receptors, Serotonin; 0/Receptors, Serotonin, 5-HT1; 0/Serotonin Antagonists; 7439-95-4/Magnesium; 7439-96-5/Manganese; 7440-09-7/Potassium; 7440-23-5/Sodium; 78950-78-4/8-Hydroxy-2-(di-n-propylamino)tetralin

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


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