Document Detail


The mGlu(4) receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide acts as a direct agonist at mGlu(6) receptors.
MedLine Citation:
PMID:  18593581     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Effects of the mGlu(4) receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC) were tested on closely related mGlu6 receptors. Modulation of native calcium currents in isolated sympathetic neurons from rat superior cervical ganglion by expressed mGlu(4) and mGlu(6) receptor was used to assay receptor activity. Glutamate concentration-response curves with and without PHCCC confirmed that the drug is an allosteric modulator of mGlu(4) receptor, without direct agonist activity. Conversely, PHCCC directly activates the mGlu(6) receptor and does not enhance activity of glutamate. Therefore, PHCCC is a direct mGlu(6) receptor agonist, but lacks allosteric modulatory properties.
Authors:
Donald Beqollari; Paul J Kammermeier
Publication Detail:
Type:  Journal Article     Date:  2008-06-19
Journal Detail:
Title:  European journal of pharmacology     Volume:  589     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  2008 Jul 
Date Detail:
Created Date:  2008-07-28     Completed Date:  2008-10-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  49-52     Citation Subset:  IM    
Affiliation:
Department of Pharmacology and Physiology, University of Rochester Medical Center, Rochester, NY 14642, USA.
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MeSH Terms
Descriptor/Qualifier:
Allosteric Regulation
Animals
Benzopyrans / pharmacology*
Calcium / metabolism
Excitatory Amino Acid Agonists / pharmacology*
Glutamic Acid / metabolism
Membrane Potentials
Neurons / drug effects*,  metabolism
Rats
Receptors, Metabotropic Glutamate / agonists*,  drug effects*,  metabolism
Superior Cervical Ganglion / cytology,  drug effects*,  metabolism
Chemical
Reg. No./Substance:
0/Benzopyrans; 0/Excitatory Amino Acid Agonists; 0/N-phenyl-7-(hydroxyimino)cyclopropa(b)chromen-1a-carboxamide; 0/Receptors, Metabotropic Glutamate; 0/metabotropic glutamate receptor 4; 0/metabotropic glutamate receptor 6; 56-86-0/Glutamic Acid; 7440-70-2/Calcium

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


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