| The mGlu(4) receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide acts as a direct agonist at mGlu(6) receptors. | |
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MedLine Citation:
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PMID: 18593581 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Donald Beqollari; Paul J Kammermeier |
Publication Detail:
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Type: Journal Article Date: 2008-06-19 |
Journal Detail:
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Title: European journal of pharmacology Volume: 589 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 2008 Jul |
Date Detail:
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Created Date: 2008-07-28 Completed Date: 2008-10-24 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: Netherlands |
Other Details:
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Languages: eng Pagination: 49-52 Citation Subset: IM |
Affiliation:
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Department of Pharmacology and Physiology, University of Rochester Medical Center, Rochester, NY 14642, USA. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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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