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https://ahro.austin.org.au/austinjspui/handle/1/10567
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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Nayler, W G | en |
dc.contributor.author | Gu, X H | en |
dc.date.accessioned | 2015-05-16T00:04:06Z | |
dc.date.available | 2015-05-16T00:04:06Z | |
dc.date.issued | 1991-08-01 | en |
dc.identifier.citation | Journal of Human Hypertension; 5 Suppl 1(): 55-9 | en |
dc.identifier.govdoc | 1834847 | en |
dc.identifier.other | PUBMED | en |
dc.identifier.uri | https://ahro.austin.org.au/austinjspui/handle/1/10567 | en |
dc.description.abstract | Amlodipine 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.iso | en | en |
dc.subject.other | Amlodipine | en |
dc.subject.other | Animals | en |
dc.subject.other | Binding Sites | en |
dc.subject.other | Calcium Channel Blockers.metabolism.pharmacology | en |
dc.subject.other | Dose-Response Relationship, Drug | en |
dc.subject.other | Female | en |
dc.subject.other | Hydrogen-Ion Concentration | en |
dc.subject.other | Nifedipine.analogs & derivatives.antagonists & inhibitors.metabolism | en |
dc.subject.other | Rats | en |
dc.subject.other | Rats, Inbred Strains | en |
dc.subject.other | Time Factors | en |
dc.title | The unique binding properties of amlodipine: a long-acting calcium antagonist. | en |
dc.type | Journal Article | en |
dc.identifier.journaltitle | Journal of human hypertension | en |
dc.identifier.affiliation | Department of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria. | en |
dc.description.pages | 55-9 | en |
dc.relation.url | https://pubmed.ncbi.nlm.nih.gov/1834847 | en |
dc.type.austin | Journal Article | en |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.cerifentitytype | Publications | - |
item.fulltext | No Fulltext | - |
item.grantfulltext | none | - |
item.languageiso639-1 | en | - |
item.openairetype | Journal Article | - |
Appears in Collections: | Journal articles |
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