The Binding Affinity of Azasetron Hydrochloride for Various Kinds of Receptors.
| Accession number;99A0958265 |
| Title;The Binding Affinity of Azasetron Hydrochloride for Various Kinds of Receptors. |
| Author;HAGA KEIICHIRO(Yoshitomi Pharm. Ind., Ltd., Chem. Res. Lab.) TAKEHARA SHUZO(Yoshitomi Pharm. Ind., Ltd., Chem. Res. Lab.) KATO AKIRA(Yoshitomiseiyaku Soyakuken) MATSUMOTO YASUHIRO(Yoshitomiseiyaku Soyakuken) |
Journal Title;Japanese Pharmacology & Therapeutics
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Journal Code:Z0947A
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ISSN:0386-3603
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VOL.27;NO.9;PAGE.1501-1505(1999)
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| Figure&Table&Reference;TBL.2, REF.22 |
| Pub. Country;Japan |
| Language;Japanese |
| Abstract;The binding affinity of azasetron hydrochloride (azasetron), a potent 5-hydroxy-tryptamine(5-HT)3 receptor antagonist, for the 5-HT1A, 5-HT2, 5-HT4, dopamine D1, D2, D3, D4, adrenaline .ALPHA.1, .ALPHA.2, .BETA., muscarine, histamine H1, benzodiazepine, cholecystokinin(CCK)A, CCKB or sigma receptors was investigated in comparison with those of other 5-HT3 receptor antagonists, ondansetron hydrochloride (ondansetron), granisetron hydrochloride (granisetron) and metoclopramide hydrochloride (metoclopramide). Azasetron has very little affinity for all the kinds of receptors tested in the same way of ondansetron and granisetron. These results indicate that azasetron, ondansetron and granisetron are highly selective 5-HT3 receptor antagonists. On the other hand, metoclopramide has higher affinity to dopamine D2 and D3 receptors than that to 5-HT3 receptor, therefore it is not a selective 5-HT3 receptor antagonist. (author abst.) |
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