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Metoclopramide-d3 is intended for use as an internal standard for the quantification of metoclopramide (Item Nos. 39844 | 23360) by GC- or LC-MS. Metoclopramide is a dual antagonist of the serotonin (5-HT) receptor subtype 5-HT3 and dopamine D2 receptor (IC50s = 308 and 483 nM, respectively).1 It also reversibly inhibits acetylcholinesterase (AChE) isolated from human postmortem caudate nucleus (Kis = 9.3 and 82 μM for competitive and non-competitive inhibition, respectively).2 Oral administration of metoclopramide inhibits emesis induced by the DNA cross-linking agent cisplatin (Item No. 13119) in ferrets (ED50 = 6,170 µg/kg) and the dopamine receptor agonist apomorphine in dogs (ED50 = 0.45 mg/kg).3,1 Metoclopramide also inhibits apomorphine-induced climbing and stereotypy in mice (ED50s = 2.2 and 6.5 mg/kg, respectively).4 Formulations containing metoclopramide have been used in the treatment of gastroesophageal reflux disease (GERD) and diabetic gastroparesis.
WARNING This product is not for human or veterinary use.