Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/10274
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dc.contributor.authorNayler, W Gen
dc.contributor.authorGu, X Hen
dc.date.accessioned2015-05-15T23:40:42Z
dc.date.available2015-05-15T23:40:42Z
dc.date.issued1991-04-01en
dc.identifier.citationJournal of Cardiovascular Pharmacology; 17(4): 587-92en
dc.identifier.govdoc1711625en
dc.identifier.otherPUBMEDen
dc.identifier.urihttps://ahro.austin.org.au/austinjspui/handle/1/10274en
dc.description.abstractAmlodipine is a newly developed long-acting dihydropyridine-based calcium antagonist. To characterize the binding properties of this compound, saturation binding studies were undertaken, using (-)[3H]amlodipine and rat cardiac membrane fragments. (-)[3H]Amlodipine bound to a single population of high-affinity binding sites with a KD of 1.68 +/- 0.12 nM, a Bmax of 0.34 +/- 0.08 pmol/mg protein, and a Hill coefficient approaching unity. Binding required up to 5 h to reach asymptote, and was pH- and temperature-sensitive. The specific binding was totally inhibited by (-) amlodipine and (-) D600 (IC50 values of 9.20 +/- 5.56 and 6.58 +/- 6.57 nM, respectively) and only partially inhibited by (+) PN 200-110, (-) Bay K 8644, (+) D600, and d-cis diltiazem (IC50 values of 60 +/- 10, 160 +/- 20, 250 +/- 40, and 200 +/- 30 nM, respectively). These results indicate that in addition to its ability to bind to the dihydropyridine and benzothiazepine recognition sites in rat cardiac membrane fragments, (-)[3H]amlodipine also binds strongly to the recognition sites for the phenylalkylamine-based calcium antagonists. The results also show that the inhibition of (-)[3H]amlodipine binding by D600 is stereospecific with (-) greater than (+)D600. Dissociation of bound (-)[3H]amlodipine was slowed under acidotic (pH 6.0) and accelerated under alkalotic (pH 10.0) conditions.en
dc.language.isoenen
dc.subject.otherAmlodipineen
dc.subject.otherAnimalsen
dc.subject.otherFemaleen
dc.subject.otherGallopamil.pharmacologyen
dc.subject.otherHydrogen-Ion Concentrationen
dc.subject.otherIn Vitro Techniquesen
dc.subject.otherIsradipineen
dc.subject.otherKineticsen
dc.subject.otherMembranes.metabolismen
dc.subject.otherMyocardium.metabolismen
dc.subject.otherNifedipine.analogs & derivatives.metabolismen
dc.subject.otherOxadiazoles.pharmacologyen
dc.subject.otherRatsen
dc.subject.otherRats, Inbred Strainsen
dc.subject.otherStereoisomerismen
dc.subject.otherTemperatureen
dc.title(-)[3H]amlodipine binding to rat cardiac membranes.en
dc.typeJournal Articleen
dc.identifier.journaltitleJournal of Cardiovascular Pharmacologyen
dc.identifier.affiliationDepartment of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australiaen
dc.description.pages587-92en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/1711625en
dc.type.austinJournal Articleen
item.openairetypeJournal Article-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.languageiso639-1en-
item.fulltextNo Fulltext-
item.cerifentitytypePublications-
item.grantfulltextnone-
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