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Article: Characterization and autoradiographic mapping of [3H]CP96,345, a nonpeptide selective NK1

TitleCharacterization and autoradiographic mapping of [3H]CP96,345, a nonpeptide selective NK1
Authors
Issue Date1995
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/peptides
Citation
Peptides, 1995, v. 16 n. 5, p. 867-872 How to Cite?
AbstractWe have studied binding and distribution of NK1 receptors in guinea pig lung using [3H]CP96,345. Kinetic studies showed that specific binding of [3H]CP96,345 was rapid and reversible, giving a kinetic dissociation constant (K(d)) of 0.28 ± 0.05 nM. The specific binding was also saturable and Scatchard analysis indicated a single class of binding site with an equilibrium K(d) of 0.12 ± 0.03 nM and maximum binding capacity (B(max)) of 107.0 ± 10.3 fmol/mg of protein. Competition studies showed the rank order of affinity for agonists and antagonists as follows: SP > NKA = septide >> NKB = senktide; CP96,345 > FK88 > FK224 > L668169. NK3 agonists, NK2-selective antagonists, and a calcium channel blocker, diltiazem, showed no displacement, indicating high selectivity for NK1 receptors. Autoradiographic mapping showed specific labeling over airway smooth muscle from central to peripheral airways, submucosal glands, and nerve fibers of trachea. The labeling of airway epithelium was increased with diminishing size of airways. Pulmonary blood vessels were also moderately labeled and there was sparse labeling over alveolar walls. [3H]CP96,345 may provide a useful tool to evaluate NK1 receptor expression in peripheral organs.
Persistent Identifierhttp://hdl.handle.net/10722/162108
ISSN
2015 Impact Factor: 2.535
2015 SCImago Journal Rankings: 1.128
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorZhang, XLen_US
dc.contributor.authorMak, JCWen_US
dc.contributor.authorBarnes, PJen_US
dc.date.accessioned2012-09-05T05:17:23Z-
dc.date.available2012-09-05T05:17:23Z-
dc.date.issued1995en_US
dc.identifier.citationPeptides, 1995, v. 16 n. 5, p. 867-872en_US
dc.identifier.issn0196-9781en_US
dc.identifier.urihttp://hdl.handle.net/10722/162108-
dc.description.abstractWe have studied binding and distribution of NK1 receptors in guinea pig lung using [3H]CP96,345. Kinetic studies showed that specific binding of [3H]CP96,345 was rapid and reversible, giving a kinetic dissociation constant (K(d)) of 0.28 ± 0.05 nM. The specific binding was also saturable and Scatchard analysis indicated a single class of binding site with an equilibrium K(d) of 0.12 ± 0.03 nM and maximum binding capacity (B(max)) of 107.0 ± 10.3 fmol/mg of protein. Competition studies showed the rank order of affinity for agonists and antagonists as follows: SP > NKA = septide >> NKB = senktide; CP96,345 > FK88 > FK224 > L668169. NK3 agonists, NK2-selective antagonists, and a calcium channel blocker, diltiazem, showed no displacement, indicating high selectivity for NK1 receptors. Autoradiographic mapping showed specific labeling over airway smooth muscle from central to peripheral airways, submucosal glands, and nerve fibers of trachea. The labeling of airway epithelium was increased with diminishing size of airways. Pulmonary blood vessels were also moderately labeled and there was sparse labeling over alveolar walls. [3H]CP96,345 may provide a useful tool to evaluate NK1 receptor expression in peripheral organs.en_US
dc.languageengen_US
dc.publisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/peptidesen_US
dc.relation.ispartofPeptidesen_US
dc.subject.meshAnimalsen_US
dc.subject.meshAutoradiography - Methodsen_US
dc.subject.meshBinding, Competitiveen_US
dc.subject.meshBiphenyl Compounds - Metabolismen_US
dc.subject.meshGuinea Pigsen_US
dc.subject.meshHypnotics And Sedatives - Metabolismen_US
dc.subject.meshKineticsen_US
dc.subject.meshLung - Metabolismen_US
dc.subject.meshRadioligand Assayen_US
dc.subject.meshReceptors, Neurokinin-1 - Analysis - Antagonists & Inhibitors - Metabolismen_US
dc.subject.meshTrachea - Metabolismen_US
dc.subject.meshTritiumen_US
dc.titleCharacterization and autoradiographic mapping of [3H]CP96,345, a nonpeptide selective NK1en_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.doi10.1016/0196-9781(95)00052-Len_US
dc.identifier.pmid7479328-
dc.identifier.scopuseid_2-s2.0-0029151672en_US
dc.identifier.volume16en_US
dc.identifier.issue5en_US
dc.identifier.spage867en_US
dc.identifier.epage872en_US
dc.identifier.isiWOS:A1995RK76700014-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridZhang, XL=10243737400en_US
dc.identifier.scopusauthoridMak, JCW=7103323094en_US
dc.identifier.scopusauthoridBarnes, PJ=36064679400en_US

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