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https://ahro.austin.org.au/austinjspui/handle/1/10274
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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 | 2015-05-15T23:40:42Z | |
dc.date.available | 2015-05-15T23:40:42Z | |
dc.date.issued | 1991-04-01 | en |
dc.identifier.citation | Journal of Cardiovascular Pharmacology; 17(4): 587-92 | en |
dc.identifier.govdoc | 1711625 | en |
dc.identifier.other | PUBMED | en |
dc.identifier.uri | https://ahro.austin.org.au/austinjspui/handle/1/10274 | en |
dc.description.abstract | Amlodipine 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.iso | en | en |
dc.subject.other | Amlodipine | en |
dc.subject.other | Animals | en |
dc.subject.other | Female | en |
dc.subject.other | Gallopamil.pharmacology | en |
dc.subject.other | Hydrogen-Ion Concentration | en |
dc.subject.other | In Vitro Techniques | en |
dc.subject.other | Isradipine | en |
dc.subject.other | Kinetics | en |
dc.subject.other | Membranes.metabolism | en |
dc.subject.other | Myocardium.metabolism | en |
dc.subject.other | Nifedipine.analogs & derivatives.metabolism | en |
dc.subject.other | Oxadiazoles.pharmacology | en |
dc.subject.other | Rats | en |
dc.subject.other | Rats, Inbred Strains | en |
dc.subject.other | Stereoisomerism | en |
dc.subject.other | Temperature | en |
dc.title | (-)[3H]amlodipine binding to rat cardiac membranes. | en |
dc.type | Journal Article | en |
dc.identifier.journaltitle | Journal of Cardiovascular Pharmacology | en |
dc.identifier.affiliation | Department of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australia | en |
dc.description.pages | 587-92 | en |
dc.relation.url | https://pubmed.ncbi.nlm.nih.gov/1711625 | 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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