Azasetron hydrochloride

Описание

Nazasetron (azasetron) hydrochloride is the fourth in the class of highly potent 5- HT₃ receptor antagonists to reach the market for prophylaxis of severe nausea and vomiting induced by cytotoxic chemotherapy and by total body X-radiation. In a study with 146 cancer patients suffering from emesis induced by cisplatin, nazasetron was reported to be markedly effective in 72% of subjects. Nazasetron is devoid of dopamine D₂ receptor blocking activity and therefore is free of the extrapyrimidal side effects associated with other commonly used antiemetics such as metoclopramide and domperidone. Nazasetron has been reported to be potentially useful for the treatment of gastrointestinal motility dysfunction, such as gastric stasis, vomiting and irritable bowel syndrome.

Химические свойства

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Использование

Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

Биологическая активность

A selective and potent 5-HT 3 antagonist (K i = 2.9 nM).