Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/10567
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dc.contributor.authorNayler, W Gen
dc.contributor.authorGu, X Hen
dc.date.accessioned2015-05-16T00:04:06Z
dc.date.available2015-05-16T00:04:06Z
dc.date.issued1991-08-01en
dc.identifier.citationJournal of Human Hypertension; 5 Suppl 1(): 55-9en
dc.identifier.govdoc1834847en
dc.identifier.otherPUBMEDen
dc.identifier.urihttp://ahro.austin.org.au/austinjspui/handle/1/10567en
dc.description.abstractAmlodipine is a 'second generation', long-acting calcium antagonist. To characterise the binding properties of this drug 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 1.64 +/- 0.17 nM, a Bmax of 0.45 +/- 0.08 pmol/mg protein and a Hill coefficient approaching unity. Binding was slow and required up to 5 hours to reach asymptote during incubation at 25 degrees C. The specific binding was totally inhibited by (-)amlodipine and (-)D600 and partially inhibited by (+)PN200-110, Bay K8644, (+)D600 and d-cis diltiazem. These results indicate that (-)[3H]amlodipine interacts strongly with the phenylalkylamine as well as the dihydropyridine binding sites. It also interacts with the benzothiazepine binding sites. The inhibition of (-)[3H]amlodipine binding by D600 is stereospecific, (-) greater than (+)D600. Bound (-)[3H]amlodipine dissociated slowly from its binding sites, less than 40% dissociation occurring during 5 hours of incubation (k-1 = 1.53 x 10(-3) min-1). These results indicate that the binding profile of amlodipine differs from that of other dihydropyridine-based Ca2+ antagonists. In addition they explain its slow onset of action, and slowed recovery on withdrawal.en
dc.language.isoenen
dc.subject.otherAmlodipineen
dc.subject.otherAnimalsen
dc.subject.otherBinding Sitesen
dc.subject.otherCalcium Channel Blockers.metabolism.pharmacologyen
dc.subject.otherDose-Response Relationship, Drugen
dc.subject.otherFemaleen
dc.subject.otherHydrogen-Ion Concentrationen
dc.subject.otherNifedipine.analogs & derivatives.antagonists & inhibitors.metabolismen
dc.subject.otherRatsen
dc.subject.otherRats, Inbred Strainsen
dc.subject.otherTime Factorsen
dc.titleThe unique binding properties of amlodipine: a long-acting calcium antagonist.en
dc.typeJournal Articleen
dc.identifier.journaltitleJournal of human hypertensionen
dc.identifier.affiliationDepartment of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria.en
dc.description.pages55-9en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/1834847en
dc.type.austinJournal Articleen
item.openairetypeJournal Article-
item.fulltextNo Fulltext-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.grantfulltextnone-
item.cerifentitytypePublications-
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