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Article: Muscarinic receptor subtypes in human and guinea pig lung

TitleMuscarinic receptor subtypes in human and guinea pig lung
Authors
Issue Date1989
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejphar
Citation
European Journal Of Pharmacology, 1989, v. 164 n. 2, p. 223-230 How to Cite?
AbstractMuscarinic receptor subtypes in human and guinea pig lung membranes were characterised using selective muscarinic antagonists. Competition experiments were carried out against [3H](-)-quinuclidinyl benzilate binding at 25°C in Tris-HCl buffer; non-specific binding was determined in the presence of 1 μM atropine. Of all the antagonists examined, only the M1-selective antagonist pirenzepine exhibited a heterogeneous binding profile (n(H) < 1.0), best described by two-binding sites of high and low affinity. Binding of [3H]pirenzepine confirmed the presence of a high proportion of high affinity (M1) receptors (60% of total) in human peripheral lung. The high potency of M3-selective antagonists 4-diphenylacetoxy-N-methyl-piperidine methiodide (4-DAMP) and hexahydrosiladifenidol suggested the presence of M3 receptors, but the low potency of AF-DX 116 and methoctramine indicated that there was no significant population of M2 receptors present. The existence of muscarinic receptor subtypes in lung may have important clinical implication but their cellular localisation remains to be determined.
Persistent Identifierhttp://hdl.handle.net/10722/161776
ISSN
2015 Impact Factor: 2.73
2015 SCImago Journal Rankings: 1.115
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorMak, JCWen_US
dc.contributor.authorBarnes, PJen_US
dc.date.accessioned2012-09-05T05:14:52Z-
dc.date.available2012-09-05T05:14:52Z-
dc.date.issued1989en_US
dc.identifier.citationEuropean Journal Of Pharmacology, 1989, v. 164 n. 2, p. 223-230en_US
dc.identifier.issn0014-2999en_US
dc.identifier.urihttp://hdl.handle.net/10722/161776-
dc.description.abstractMuscarinic receptor subtypes in human and guinea pig lung membranes were characterised using selective muscarinic antagonists. Competition experiments were carried out against [3H](-)-quinuclidinyl benzilate binding at 25°C in Tris-HCl buffer; non-specific binding was determined in the presence of 1 μM atropine. Of all the antagonists examined, only the M1-selective antagonist pirenzepine exhibited a heterogeneous binding profile (n(H) < 1.0), best described by two-binding sites of high and low affinity. Binding of [3H]pirenzepine confirmed the presence of a high proportion of high affinity (M1) receptors (60% of total) in human peripheral lung. The high potency of M3-selective antagonists 4-diphenylacetoxy-N-methyl-piperidine methiodide (4-DAMP) and hexahydrosiladifenidol suggested the presence of M3 receptors, but the low potency of AF-DX 116 and methoctramine indicated that there was no significant population of M2 receptors present. The existence of muscarinic receptor subtypes in lung may have important clinical implication but their cellular localisation remains to be determined.en_US
dc.languageengen_US
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejpharen_US
dc.relation.ispartofEuropean Journal of Pharmacologyen_US
dc.subject.meshAdamantane - Analogs & Derivatives - Pharmacologyen_US
dc.subject.meshAdulten_US
dc.subject.meshAgeden_US
dc.subject.meshAnimalsen_US
dc.subject.meshAtropine - Pharmacologyen_US
dc.subject.meshGuinea Pigsen_US
dc.subject.meshHumansen_US
dc.subject.meshLung - Drug Effects - Metabolismen_US
dc.subject.meshMiddle Ageden_US
dc.subject.meshParasympatholytics - Pharmacologyen_US
dc.subject.meshPiperidines - Pharmacologyen_US
dc.subject.meshPirenzepine - Pharmacologyen_US
dc.subject.meshProtease Inhibitors - Pharmacologyen_US
dc.subject.meshQuinuclidinyl Benzilate - Diagnostic Useen_US
dc.subject.meshReceptors, Muscarinic - Drug Effects - Metabolismen_US
dc.subject.meshSpecies Specificityen_US
dc.titleMuscarinic receptor subtypes in human and guinea pig lungen_US
dc.typeArticleen_US
dc.identifier.emailMak, JCW:judymak@hku.hken_US
dc.identifier.authorityMak, JCW=rp00352en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1016/0014-2999(89)90462-7-
dc.identifier.pmid2759174en_US
dc.identifier.scopuseid_2-s2.0-0024371807en_US
dc.identifier.volume164en_US
dc.identifier.issue2en_US
dc.identifier.spage223en_US
dc.identifier.epage230en_US
dc.identifier.isiWOS:A1989AB79200006-
dc.publisher.placeNetherlandsen_US
dc.identifier.scopusauthoridMak, JCW=7103323094en_US
dc.identifier.scopusauthoridBarnes, PJ=36064679400en_US

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