The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist
| Autor: | Shoji Hidenori, Fukuda Takemi, Inaba Ken-ichi, Tetsuya Tahara, Setoguchi Michihide |
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| Rok vydání: | 1991 |
| Předmět: |
Serotonin
Time Factors medicine.drug_class Vomiting medicine.medical_treatment Azasetron Pharmacology Bridged Bicyclo Compounds Radioligand Assay 5-HT3 Receptor Antagonist Dogs Antineoplastic Combined Chemotherapy Protocols Oxazines Medicine Antiemetic Animals Cyclophosphamide Chemotherapy business.industry Ferrets Receptor antagonist Bridged Bicyclo Compounds Heterocyclic Receptors Neurotransmitter Kinetics Dopamine receptor Doxorubicin Receptors Serotonin Toxicity Antiemetics Serotonin Antagonists medicine.symptom Cisplatin business Whole-Body Irradiation medicine.drug |
| Zdroj: | European journal of pharmacology. 196(3) |
| ISSN: | 0014-2999 |
| Popis: | Y-25130( (+/-)N-(1-azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro - 2H-1,4-benzoxazine-8-carboxamide hydrochloride) is a potent and selective 5-HT3 receptor antagonist free of dopamine receptor blocking activity. This compound was effective against emesis induced in animals by cytotoxic drugs or by total body X-radiation. When given prophylactically, the doses required to completely inhibit cisplatin-induced emesis in dogs and doxorubicin and cyclophosphamide-induced emesis in ferrets were 0.1 and 0.3 mg/kg i.v., respectively. Y-25130, at the dose of 0.3 mg/kg i.v., almost completely inhibited X-radiation-induced emesis in ferrets. When given during emesis, the doses required to completely inhibit cisplatin-induced emesis in dogs and doxorubicin- and cyclophosphamide-induced emesis in ferrets were 0.1 and 0.3 mg/kg i.v., respectively. The i.v. dose of 0.3 mg/kg of Y-25130 was enough to almost completely inhibit cisplatin-induced emesis in dogs for 24 h. From these results, it is suggested that Y-25130 may become an effective antiemetic drug against emesis induced by anticancer therapy. |
| Databáze: | OpenAIRE |
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