1 40 1 Text A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text. URL Address <a href="http://doi.org/10.1124/jpet.104.073155" target="_blank" rel="noreferrer noopener">http://doi.org/10.1124/jpet.104.073155</a> Pages 502–508 Issue 2 Volume 312 Dublin Core The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/. Title A name given to the resource Activation of metabotropic glutamate receptor 1 dimers requires glutamate binding in both subunits. Publisher An entity responsible for making the resource available The Journal of pharmacology and experimental therapeutics Date A point or period of time associated with an event in the lifecycle of the resource 2005 2005-02 Subject The topic of the resource Blotting; Calcium Channels/drug effects/metabolism; DNA/biosynthesis/genetics; Dose-Response Relationship; Drug; Fluorescent Antibody Technique; Genes; Glutamic Acid/*metabolism; Humans; Membrane Potentials/drug effects; Metabotropic Glutamate/genetics/*metabolism; myc/genetics; Patch-Clamp Techniques; Plasmids/genetics; Receptors; Signal Transduction/drug effects; Superior Cervical Ganglion/cytology/drug effects/metabolism; Sympathetic Nervous System/cytology/drug effects/metabolism; Western Creator An entity primarily responsible for making the resource Kammermeier Paul J; Yun June Description An account of the resource Group I metabotropic glutamate receptors (mGluRs) form stable, disulfide-linked homodimers. Lack of a verifiably monomeric mGluR1 mutant has led to difficulty in assessing the role of dimerization in the molecular mechanism of mGluR1 activation. The related GABA(B) receptor exhibits striking intradimer cross talk (ligand binding at one subunit effectively produces G protein activation at the other), but it is unclear whether group I mGluRs exhibit analogous cross talk. Signaling of heterologously expressed mGluR1 was examined in isolated rat sympathetic neurons by measuring glutamate-mediated inhibition of native calcium currents. To examine mGluR1 activity when only one dimer subunit has access to glutamate ligand, wildtype mGluR1 was coexpressed with mGluR1 Y74A, a mutant with impaired glutamate binding, and the activity of the heterodimer (mutant/wild type) was examined. The mGluR1 Y74A mutant alone had a dose-response curve that was shifted by about 2 orders of magnitude. The half-maximal dose of glutamate shifted from 1.3 (wild-type mGluR1) to about 450 (mGluR1 Y74A) microM. However, the maximal effect was similar. Wild-type mGluR1 was expressed with excess Y74A mGluR1 to generate a receptor population consisting largely of mutant homodimers and mutant/wild-type heterodimers but without detectable wild-type homodimers. Under these conditions, no glutamate-mediated calcium current inhibition was observed below approximately 300 microM glutamate, although wild-type mGluR1 protein was detectable with immunofluorescence. These data suggest that mutant/wild-type heterodimeric receptors are inactive at ligand concentrations favoring glutamate association with receptor dimers at only one subunit. Identifier An unambiguous reference to the resource within a given context <a href="http://doi.org/10.1124/jpet.104.073155" target="_blank" rel="noreferrer noopener">10.1124/jpet.104.073155</a> Rights Information about rights held in and over the resource Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s). 2005 Blotting Calcium Channels/drug effects/metabolism Department of Integrative Medical Sciences DNA/biosynthesis/genetics Dose-Response Relationship Drug Fluorescent Antibody Technique Genes Glutamic Acid/*metabolism Humans Kammermeier Paul J Membrane Potentials/drug effects Metabotropic Glutamate/genetics/*metabolism myc/genetics NEOMED College of Medicine Patch-Clamp Techniques Plasmids/genetics Receptors Signal Transduction/drug effects Superior Cervical Ganglion/cytology/drug effects/metabolism Sympathetic Nervous System/cytology/drug effects/metabolism The Journal of pharmacology and experimental therapeutics Western Yun June