{"@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/1362262943381290880.json","@type":"Article","productIdentifier":[{"identifier":{"@type":"DOI","@value":"10.1111/j.1476-5381.1995.tb15923.x"}},{"identifier":{"@type":"URI","@value":"https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1111%2Fj.1476-5381.1995.tb15923.x"}},{"identifier":{"@type":"URI","@value":"https://bpspubs.onlinelibrary.wiley.com/doi/pdf/10.1111/j.1476-5381.1995.tb15923.x"}}],"dc:title":[{"@value":"The in vitro pharmacology of ZM 241385, a potent, non‐xanthine, A<sub>2a</sub>selective adenosine receptor antagonist"}],"description":[{"type":"abstract","notation":[{"@value":"<jats:p><jats:list list-type=\"explicit-label\"><jats:list-item><jats:p>This paper describes the<jats:italic>in vitro</jats:italic>pharmacology of ZM 241385 (4‐(2‐[7‐amino‐2‐(2‐furyl) [1,2,4]‐triazolo[2,3‐a][1,3,5]triazin‐5‐yl amino]ethyl) phenol), a novel non‐xanthine adenosine receptor antagonist with selectivity for the A<jats:sub>2a</jats:sub>receptor subtype.</jats:p></jats:list-item><jats:list-item><jats:p>ZM 241385 had high affinity for A<jats:sub>2a</jats:sub>receptors. In rat phaeochromocytoma cell membranes, ZM 241385 displaced binding of tritiated 5′‐N‐ethylcarboxamidoadenosine (NECA) with a pIC<jats:sub>50</jats:sub>of 9.52, (95% confidence limits, c.l., 9.02–10.02). In guinea‐pig isolated Langendorff hearts, ZM 241385 antagonized vasodilatation of the coronary bed produced by 2‐chloroadenosine (2‐CADO) and 2‐[<jats:italic>p</jats:italic>‐(2‐carboxyethyl) phenethylamino]‐5′‐N‐ethylcarboxamidoadenosine (CGS21680) with pA<jats:sub>2</jats:sub>values of 8.57 (c.l., 8.45‐8.68) and 9.02 (c.l., 8.79‐9.24) respectively 3 ZM 241385 had low potency at A<jats:sub>2b</jats:sub>receptors and antagonized the relaxant effects of adenosine in the guinea‐pig aorta with a pA<jats:sub>2</jats:sub>of 7.06, (c.l., 6.92‐7.19).</jats:p></jats:list-item><jats:list-item><jats:p>ZM 241385 had a low affinity at A<jats:sub>1</jats:sub>receptors. In rat cerebral cortex membranes it displaced tritiated<jats:bold>R</jats:bold>‐phenylisopropyladenosine (<jats:bold>R</jats:bold>‐PIA) with a pIC<jats:sub>50</jats:sub>of 5.69 (c.l., 5.57‐5.81). ZM 241385 antagonized the bradycardie action of 2‐CADO in guinea‐pig atria with a pA<jats:sub>2</jats:sub>of 5.95 (c.l., 5.72‐6.18).</jats:p></jats:list-item><jats:list-item><jats:p>ZM 241385 had low affinity for A<jats:sub>3</jats:sub>receptors. At cloned rat A<jats:sub>3</jats:sub>receptors expressed in Chinese hamster ovary cells, it displaced iodinated aminobenzyl‐5′‐N‐methylcarboxamido adenosine (AB‐MECA) with a pIC<jats:sub>50</jats:sub>of 3.82 (c.l., 3.67‐4.06).</jats:p></jats:list-item><jats:list-item><jats:p>ZM 241385 had no significant additional pharmacological effects on the isolated tissues used in these studies at concentrations three orders of magnitude greater than those which block A<jats:sub>2a</jats:sub>receptors. At 10 μm it displayed only minor inhibition of the bradycardic effects in guinea‐pig atria to some concentrations of carbachol. At 10 μ<jats:sc>m</jats:sc>, ZM 241385 had a small inhibitory effect on relaxant effects of isoprenaline in guinea‐pig aortae but no effect on sodium nitrite‐induced relaxation. ZM 241385 (100 μ<jats:sc>m</jats:sc>) was without effect on phenylephrine‐induced tone in guinea‐pig aortae.</jats:p></jats:list-item><jats:list-item><jats:p>ZM 241385 (10 μ<jats:sc>m</jats:sc>) had no inhibitory effect on rat hepatocyte phosphodiesterase types I, II, III and IV but caused a small inhibition of the calcium calmodulin‐activated type I enzyme.</jats:p></jats:list-item><jats:list-item><jats:p>ZM 241385 is the most selective adenosine A<jats:sub>2a</jats:sub>receptor antagonist yet described and is therefore a useful tool for characterization of responses mediated by A<jats:sub>2</jats:sub>adenosine receptors.</jats:p></jats:list-item></jats:list></jats:p>"}]}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1382262943381290882","@type":"Researcher","foaf:name":[{"@value":"S.M. Poucher"}]},{"@id":"https://cir.nii.ac.jp/crid/1382262943381290883","@type":"Researcher","foaf:name":[{"@value":"J.R. Keddie"}]},{"@id":"https://cir.nii.ac.jp/crid/1382262943381290880","@type":"Researcher","foaf:name":[{"@value":"P. Singh"}]},{"@id":"https://cir.nii.ac.jp/crid/1382262943381290881","@type":"Researcher","foaf:name":[{"@value":"S.M. Stoggall"}]},{"@id":"https://cir.nii.ac.jp/crid/1382262943381290884","@type":"Researcher","foaf:name":[{"@value":"P.W.R. Caulkett"}]},{"@id":"https://cir.nii.ac.jp/crid/1382262943381290885","@type":"Researcher","foaf:name":[{"@value":"G. Jones"}]},{"@id":"https://cir.nii.ac.jp/crid/1382262943381290886","@type":"Researcher","foaf:name":[{"@value":"M.G. Collis"}]}],"publication":{"publicationIdentifier":[{"@type":"PISSN","@value":"00071188"},{"@type":"EISSN","@value":"14765381"}],"prism:publicationName":[{"@value":"British Journal of Pharmacology"}],"dc:publisher":[{"@value":"Wiley"}],"prism:publicationDate":"1995-07","prism:volume":"115","prism:number":"6","prism:startingPage":"1096","prism:endingPage":"1102"},"reviewed":"false","dc:rights":["http://onlinelibrary.wiley.com/termsAndConditions#vor"],"url":[{"@id":"https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1111%2Fj.1476-5381.1995.tb15923.x"},{"@id":"https://bpspubs.onlinelibrary.wiley.com/doi/pdf/10.1111/j.1476-5381.1995.tb15923.x"}],"createdAt":"2012-07-19","modifiedAt":"2025-04-04","relatedProduct":[{"@id":"https://cir.nii.ac.jp/crid/1360306905621271424","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@value":"Photoresponsive Adenosine Derivatives for the Optical Control of Adenosine A\n                    <sub>2A</sub>\n                    Receptors in Living Cells"}]},{"@id":"https://cir.nii.ac.jp/crid/1360567182229381120","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@value":"Royal jelly coordinately enhances hippocampal neuronal expression of somatostatin and neprilysin genes conferring neuronal protection against toxic soluble amyloid-β oligomers implicated in Alzheimer’s disease pathogenesis"}]},{"@id":"https://cir.nii.ac.jp/crid/1390282679262745600","@type":"Article","resourceType":"学術雑誌論文(journal article)","relationType":["isReferencedBy"],"jpcoar:relatedTitle":[{"@language":"en","@value":"Effects of YT-146 (2-(1-Octynyl) Adenosine), an Adenosine A2A Receptor Agonist, on cAMP Production and Noradrenaline Release in PC12 Cells."},{"@language":"ja-Kana","@value":"Effects of YT-146 2 1 Octynyl Adenosine"},{"@value":"Effects of YT-146 [2-(1-Octynyl) Adenosine], an Adenosine A2A Receptot Agonist, on cAMP Production and Noradrenaline Release in PC12 Cells"}]}],"dataSourceIdentifier":[{"@type":"CROSSREF","@value":"10.1111/j.1476-5381.1995.tb15923.x"},{"@type":"CROSSREF","@value":"10.1021/acschembio.4c00583_references_DOI_MFQpSJ77YVNk9cIIF8vyKOawloV"},{"@type":"CROSSREF","@value":"10.1254/jjp.78.269_references_DOI_MFQpSJ77YVNk9cIIF8vyKOawloV"},{"@type":"CROSSREF","@value":"10.1016/j.jff.2018.10.006_references_DOI_MFQpSJ77YVNk9cIIF8vyKOawloV"}]}