产品描述:
Metoclopramide is a dual antagonist of the serotonin (5-HT) receptor subtype 5-HT3 and dopamine D2 receptor (IC50s = 308 and 483 nM, respectively).{36216} 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).{36217} 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).{36215,36216} Metoclopramide also inhibits apomorphine-induced climbing and stereotypy in mice (ED50s = 2.2 and 6.5 mg/kg, respectively).{36219} Formulations containing metoclopramide have been used in the treatment of gastroesophageal reflux disease (GERD) and diabetic gastroparesis.