Metoclopramide

Metoclopramide is a dual antagonist of the serotonin (5-HT) receptor subtype 5-HT3 and dopamine D2 receptor (IC50s = 308 and 483 nM, respectively). 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). Oral administration of metoclopramide inhibits emesis induced by the DNA cross-linking agent cisplatin (Cay-13119) in ferrets (ED50 = 6,170 µg/kg) and the dopamine receptor agonist apomorphine in dogs (ED50 = 0.45 mg/kg). Metoclopramide also inhibits apomorphine-induced climbing and stereotypy in mice (ED50s = 2.2 and 6.5 mg/kg, respectively). Formulations containing metoclopramide have been used in the treatment of gastroesophageal reflux disease (GERD) and diabetic gastroparesis.Formal Name: 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxy-benzamide. CAS Number: 364-62-5. Molecular Formula: C14H22ClN3O2. Formula Weight: 299.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble, DMSO: Soluble, Water: Slightly Soluble. SMILES: ClC1=CC(C(NCCN(CC)CC)=O)=C(OC)C=C1N. InChi Code: InChI=1S/C14H22ClN3O2/c1-4-18(5-2)7-6-17-14(19)10-8-11(15)12(16)9-13(10)20-3/h8-9H,4-7,16H2,1-3H3,(H,17,19). InChi Key: TTWJBBZEZQICBI-UHFFFAOYSA-N.