D-dopaminergic receptor and 5-HT serotoninergic receptor antagonists having antiemetic profile

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Metoclopramide is the prototype of the orthopramide family and is used clinically as a stimulant of upper gastrointestinal motility and as an antiemetic. Its antiemetic potential is attributed mainly to the antagonist activity at D-dopaminergic receptors in the chemoreceptor trigger zone of the central nervous system. Besides, ondansetron was the first selective 5-HT serotoninergic receptor antagonist used in clinics as an antiemetic. Herein, the antiemetic profile of different chemical classes of D-dopaminergic receptor and 5-HT serotoninergic receptor antagonists will be discussed, which may be helpful in the development of potent antiemetic agents.

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