Article: κ-opioid receptor agonist inhibits the cholera toxin-sensitive G protein in the heart

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Titleκ-opioid receptor agonist inhibits the cholera toxin-sensitive G protein in the heart
AuthorsYu, XC1
Diao, TM1
Pei, JM1
Zhang, WM1
Wong, NS1
Wong, TM1
Issue Date2001
PublisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/
CitationJournal Of Cardiovascular Pharmacology, 2001, v. 38 n. 2, p. 232-239 [How to Cite?]
DOI: http://dx.doi.org/10.1097/00005344-200108000-00009
AbstractTo explore the signaling mechanisms of the negative modulation of β-adrenoceptors by κ-opioid receptors (κ-OR) in the heart, the possibility of the interaction at the level of G protein and receptor was determined. Cholera toxin, an activator of the stimulatory G protein (Gs), elevated electrically induced intracellular Ca2+ ([Ca2+]i) transients and induced ribosylation of the α-subunit of Gs (Gsα) in rat ventricular myocytes. The effects were significantly attenuated by U50,488H, a specific agonist of κ-OR, and were abolished by nor-binaltorphimine, a selective κ-OR antagonist. The content of Gsα, however, was not affected by U50,488H. Receptor binding experiments showed that neither Bmax nor Kd of the binding of [3H]CGP-12177, a β-adrenoceptor antagonist, was affected by U50,488H. The current study provides the first evidence that κ-OR stimulation inhibits the ribosylation of the α-subunit of the Gs protein, thus inhibiting the action of cholera toxin on the protein.
ISSN0160-2446
2011 Impact Factor: 2.287
2011 SCImago Journal Rankings: 0.219
DOIhttp://dx.doi.org/10.1097/00005344-200108000-00009
ISI Accession Number IDWOS:000170020200009
ReferencesReferences in Scopus
DC Field
Value
dc.contributor.authorYu, XC
dc.contributor.authorDiao, TM
dc.contributor.authorPei, JM
dc.contributor.authorZhang, WM
dc.contributor.authorWong, NS
dc.contributor.authorWong, TM
dc.date.accessioned2012-05-29T06:03:53Z
dc.date.available2012-05-29T06:03:53Z
dc.date.issued2001
dc.description.abstractTo explore the signaling mechanisms of the negative modulation of β-adrenoceptors by κ-opioid receptors (κ-OR) in the heart, the possibility of the interaction at the level of G protein and receptor was determined. Cholera toxin, an activator of the stimulatory G protein (Gs), elevated electrically induced intracellular Ca2+ ([Ca2+]i) transients and induced ribosylation of the α-subunit of Gs (Gsα) in rat ventricular myocytes. The effects were significantly attenuated by U50,488H, a specific agonist of κ-OR, and were abolished by nor-binaltorphimine, a selective κ-OR antagonist. The content of Gsα, however, was not affected by U50,488H. Receptor binding experiments showed that neither Bmax nor Kd of the binding of [3H]CGP-12177, a β-adrenoceptor antagonist, was affected by U50,488H. The current study provides the first evidence that κ-OR stimulation inhibits the ribosylation of the α-subunit of the Gs protein, thus inhibiting the action of cholera toxin on the protein.
dc.description.natureLink_to_subscribed_fulltext
dc.identifier.citationJournal Of Cardiovascular Pharmacology, 2001, v. 38 n. 2, p. 232-239 [How to Cite?]
DOI: http://dx.doi.org/10.1097/00005344-200108000-00009
dc.identifier.doihttp://dx.doi.org/10.1097/00005344-200108000-00009
dc.identifier.epage239
dc.identifier.isiWOS:000170020200009
dc.identifier.issn0160-2446
2011 Impact Factor: 2.287
2011 SCImago Journal Rankings: 0.219
dc.identifier.issue2
dc.identifier.pmid11483873
dc.identifier.scopuseid_2-s2.0-0034917623
dc.identifier.spage232
dc.identifier.urihttp://hdl.handle.net/10722/147461
dc.identifier.volume38
dc.languageeng
dc.publisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/
dc.publisher.placeUnited States
dc.relation.ispartofJournal of Cardiovascular Pharmacology
dc.relation.referencesReferences in Scopus
dc.subject.mesh3,4-Dichloro-N-Methyl-N-(2-(1-Pyrrolidinyl)-Cyclohexyl)-Benzeneacetamide, (Trans)-Isomer - Pharmacology
dc.subject.meshAnalgesics, Non-Narcotic - Pharmacology
dc.subject.meshAnimals
dc.subject.meshBinding Sites
dc.subject.meshCalcium - Metabolism
dc.subject.meshCholera Toxin - Pharmacology
dc.subject.meshElectric Stimulation
dc.subject.meshGtp-Binding Protein Alpha Subunits, Gs - Antagonists & Inhibitors - Metabolism
dc.subject.meshHeart Ventricles - Cytology - Drug Effects
dc.subject.meshMyocardium - Cytology - Metabolism
dc.subject.meshPropanolamines - Metabolism
dc.subject.meshRats
dc.subject.meshRats, Sprague-Dawley
dc.subject.meshReceptors, Adrenergic, Beta - Metabolism
dc.subject.meshReceptors, Opioid, Kappa - Agonists - Metabolism - Physiology
dc.titleκ-opioid receptor agonist inhibits the cholera toxin-sensitive G protein in the heart
dc.typeArticle
Author Affiliations
  1. The University of Hong Kong