Antiemetic activity of the new 5-HT3 antagonist DAU 6215 in animal models of cancer chemotherapy and radiation
| Autor: | A. Donetti, A. Sagrada, M. Turconi, Massimo Nicola, E. Montagna, D. R. Algate, Schiantarelli Pierino, R. Micheletti, E. M. Rimoldi, P. Bonali |
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| Rok vydání: | 1991 |
| Předmět: |
Male
Cancer Research Time Factors Metoclopramide medicine.drug_class Vomiting medicine.medical_treatment Drug Evaluation Preclinical Pharmacology Toxicology Ondansetron Bridged Bicyclo Compounds Dogs 5-HT3 antagonist medicine Potency Antiemetic Animals Pharmacology (medical) Chemotherapy Dose-Response Relationship Drug business.industry Antagonist Ferrets Imidazoles Neoplasms Experimental Bridged Bicyclo Compounds Heterocyclic Disease Models Animal Oncology Doxorubicin Antiemetics Benzimidazoles Female Serotonin Antagonists medicine.symptom Cisplatin business medicine.drug |
| Zdroj: | Cancer chemotherapy and pharmacology. 28(6) |
| ISSN: | 0344-5704 |
| Popis: | The antiemetic activity of DAU 6215, a novel antagonist of 5-HT3 receptors, was investigated in animal models of cytotoxic treatment-evoked emesis and compared with the antiemetic activity of ondansetron and metoclopramide. In dogs, vomiting was induced by i.v. cisplatin; in ferrets, the emetic response was elicited by i.v. doxorubicin or X-ray exposure. Pretreatment with 0.1–1 mg/kg DAU 6215 given i.v. or p.o. prevented the vomiting response to the different emetic agents. In the dog, the antiemetic potency of metoclopramide was 30 times lower than that of DAU 6215. Ondansetron was less potent than DAU 6215 against cisplatin and doxorubicin but was equally effective in the radiotherapy protocol. In this model, lengthening of the pretreatment time to 2 h did not affect the antiemetic efficacy of DAU 6215, whereas it decreased that of ondansetron. The results demonstrate that DAU 6215 is a highly effective and long-lasting inhibitor of cytotoxic treatment-induced emesis in different animal species. |
| Databáze: | OpenAIRE |
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