Metoclopramide is an orally bioavailable serotonin (5-HT) receptor 5-HT3 antagonist with Ki and IC50 values of 995 and 308 nM, respectively, in rat cortical membranes. It is also a dopamine receptor 2 (D2) antagonist (IC50 = 483 nM in rat brain synaptic membranes). Oral administration of metoclopramide inhibits emesis induced by cisplatin and apomorphine in ferrets and dogs with ED50 values of 6.17 and 0.45 mg/kg, respectively. Metoclopramide reversibly inhibits human acetylcholinesterase (AChE) isolated from the caudate nucleus (Kis = 9.3 and 82 μM for competitive and non-competitive inhibition, respectively). Formulations containing metoclopramide have been used as anti-emetic and antipsychotic agents.

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