{"@context":{"@vocab":"https://cir.nii.ac.jp/schema/1.0/","rdfs":"http://www.w3.org/2000/01/rdf-schema#","dc":"http://purl.org/dc/elements/1.1/","dcterms":"http://purl.org/dc/terms/","foaf":"http://xmlns.com/foaf/0.1/","prism":"http://prismstandard.org/namespaces/basic/2.0/","cinii":"http://ci.nii.ac.jp/ns/1.0/","datacite":"https://schema.datacite.org/meta/kernel-4/","ndl":"http://ndl.go.jp/dcndl/terms/","jpcoar":"https://github.com/JPCOAR/schema/blob/master/2.0/"},"@id":"https://cir.nii.ac.jp/crid/1362825895367801728.json","@type":"Article","productIdentifier":[{"identifier":{"@type":"DOI","@value":"10.1016/0922-4106(91)90096-z"}},{"identifier":{"@type":"URI","@value":"https://api.elsevier.com/content/article/PII:092241069190096Z?httpAccept=text/xml"}},{"identifier":{"@type":"URI","@value":"https://api.elsevier.com/content/article/PII:092241069190096Z?httpAccept=text/plain"}},{"identifier":{"@type":"PMID","@value":"1663043"}}],"dc:title":[{"@value":"Effects of four diltiazem stereoisomers on binding of d-cis-[3H]diltiazem and (+)-[3H]PN200-110 to rabbit T-tubule calcium channels"}],"description":[{"notation":[{"@value":"Diltiazem, a benzothiazepine Ca2+ antagonist, has four stereoisomeric forms: d- and l-isomers of the cis and trans forms. All four isomers were shown to completely inhibit the binding of d-cis-[3H]diltiazem to rabbit T-tubule Ca2+ channels. The potency of the inhibition was in the order: d-cis greater than l-cis greater than d-trans = l-trans. The Hill slope for each inhibition was close to unity. The l-cis, d-trans and l-trans isomers had no effect on dissociation of the d-cis[3H]diltiazem-benzothiazepine receptor complex. These results indicate that all four isomers bind to benzothiazepine receptors. Furthermore, all of the isomers modulated (+)-[3H]PN200-110 binding. At 37 degrees C, only the d-cis isomer stimulated the binding, whereas the others showed inhibition. At 2 degrees C, all of them inhibited the binding. Both trans isomers exerted virtually the same, weak effects on the binding. It is concluded that the effects of diltiazem on radioligand binding to Ca2+ channels are highly stereospecific for the d-cis isomer."}]}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1382825895367801729","@type":"Researcher","foaf:name":[{"@value":"Shota Ikeda"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825895367801730","@type":"Researcher","foaf:name":[{"@value":"Jun-Ichiro Oka"}]},{"@id":"https://cir.nii.ac.jp/crid/1382825895367801728","@type":"Researcher","foaf:name":[{"@value":"Taku Nagao"}]}],"publication":{"publicationIdentifier":[{"@type":"PISSN","@value":"09224106"},{"@type":"PISSN","@value":"http://id.crossref.org/issn/00142999"}],"prism:publicationName":[{"@value":"European Journal of Pharmacology: Molecular Pharmacology"}],"dc:publisher":[{"@value":"Elsevier BV"}],"prism:publicationDate":"1991-11","prism:volume":"208","prism:number":"3","prism:startingPage":"199","prism:endingPage":"205"},"reviewed":"false","dc:rights":["https://www.elsevier.com/tdm/userlicense/1.0/"],"url":[{"@id":"https://api.elsevier.com/content/article/PII:092241069190096Z?httpAccept=text/xml"},{"@id":"https://api.elsevier.com/content/article/PII:092241069190096Z?httpAccept=text/plain"}],"createdAt":"2003-03-04","modifiedAt":"2021-06-05","foaf:topic":[{"@id":"https://cir.nii.ac.jp/all?q=Dihydropyridines","dc:title":"Dihydropyridines"},{"@id":"https://cir.nii.ac.jp/all?q=Muscles","dc:title":"Muscles"},{"@id":"https://cir.nii.ac.jp/all?q=Receptors,%20Drug","dc:title":"Receptors, Drug"},{"@id":"https://cir.nii.ac.jp/all?q=Stereoisomerism","dc:title":"Stereoisomerism"},{"@id":"https://cir.nii.ac.jp/all?q=Receptors,%20Nicotinic","dc:title":"Receptors, Nicotinic"},{"@id":"https://cir.nii.ac.jp/all?q=Calcium%20Channel%20Blockers","dc:title":"Calcium Channel Blockers"},{"@id":"https://cir.nii.ac.jp/all?q=Tritium","dc:title":"Tritium"},{"@id":"https://cir.nii.ac.jp/all?q=Diltiazem","dc:title":"Diltiazem"},{"@id":"https://cir.nii.ac.jp/all?q=Kinetics","dc:title":"Kinetics"},{"@id":"https://cir.nii.ac.jp/all?q=Radioligand%20Assay","dc:title":"Radioligand Assay"},{"@id":"https://cir.nii.ac.jp/all?q=Animals","dc:title":"Animals"},{"@id":"https://cir.nii.ac.jp/all?q=Calcium%20Channels","dc:title":"Calcium Channels"},{"@id":"https://cir.nii.ac.jp/all?q=Isradipine","dc:title":"Isradipine"},{"@id":"https://cir.nii.ac.jp/all?q=Rabbits","dc:title":"Rabbits"}],"relatedProduct":[{"@id":"https://cir.nii.ac.jp/crid/1390001204287387392","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@language":"en","@value":"Desensitization and Selective Down-Regulation of Rat Cardiac, .BETA.1-Adrenoceptors by Prolonged In Vivo Infusion of T-0509, .BETA.1-Adrenoceptor Full Agonist."},{"@value":"Desensitization and Selective Down-Regulation of Rat Cardiac β1-Adrenoceptors by Prolonged In Vivo Infusion of T-0509, a β1-Adrenoceptor Full Agonist"}]},{"@id":"https://cir.nii.ac.jp/crid/1390001204287808000","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@language":"en","@value":"Energy Preserving Effect of l-cis Diltiazem in Isolated Ischemic and Reperfused Guinea Pig Hearts. A 31P-NMR Study."}]},{"@id":"https://cir.nii.ac.jp/crid/1390282679261564032","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@language":"en","@value":"Treatment With l-cis Diltiazem Before Reperfusion Reduces Infarct Size in the Ischemic Rabbit Heart In Vivo."},{"@value":"Treatment With 1-cis Diltiazem Before Reperfusion Reduces Infarct Size in the Ischemic Rabbit Heart In Vivo"}]},{"@id":"https://cir.nii.ac.jp/crid/1390282679261870208","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@language":"en","@value":"Quaternary Diltiazem Can Act from Both Sides of the Membrane in Ventricular Myocytes."}]}],"dataSourceIdentifier":[{"@type":"CROSSREF","@value":"10.1016/0922-4106(91)90096-z"},{"@type":"OPENAIRE","@value":"doi_dedup___::dd91957c4010c939f4b956f3a355bb4e"},{"@type":"CROSSREF","@value":"10.1254/jjp.83.225_references_DOI_KQm3imn9xOUmctgrm9bJ2HQzJgX"},{"@type":"CROSSREF","@value":"10.1254/jjp.61.263_references_DOI_KQm3imn9xOUmctgrm9bJ2HQzJgX"},{"@type":"CROSSREF","@value":"10.1254/jjp.80.319_references_DOI_KQm3imn9xOUmctgrm9bJ2HQzJgX"},{"@type":"CROSSREF","@value":"10.1254/jjp.69.343_references_DOI_KQm3imn9xOUmctgrm9bJ2HQzJgX"}]}