Description
Metoclopramide-d
3 is intended for use as an internal standard for the quantification of metoclopramide by GC- or LC-MS. Metoclopramide is an orally bioavailable serotonin (5-HT) receptor 5-HT
3 antagonist with K
i and IC
50 values of 995 and 308 nM, respectively, in rat cortical membranes. It is also a dopamine D
2 receptor antagonist (IC
50 = 483 nM in rat brain synaptic membranes). Oral administration of metoclopramide inhibits emesis induced by cisplatin and apomorphine in ferrets and dogs with ED
50 values of 6.17 and 0.45 mg/kg, respectively. Metoclopramide reversibly inhibits human acetylcholinesterase (AChE) isolated from the caudate nucleus (K
is = 9.3 and 82 μM for competitive and non-competitive inhibition, respectively). Formulations containing metoclopramide have been used as anti-emetic and antipsychotic agents.
References
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10.1248/cpb.50.941[2] JRG-MICHAEL CHEMNITIUS . INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF METOCLOPRAMIDE: REVERSIBLE INHIBITION OF CHOLINESTERASES FROM HUMAN CENTRAL NERVOUS SYSTEM AND BLOOD[J]. Pharmacological research, 1996, 34 1: Pages 65-72. DOI:
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10.1007/bf00174864
