For research use only. Not for therapeutic Use.
Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1].
Cardiac Na+ channels are common targets of therapeutics inducing cardiotoxicity[3].
Domperidone monomaleate (0-1000 μM) displays concentration- and state-dependent inhibitory of Nav1.5 in Human embryonic kidney HEK293 cells[3].
Domperidone monomaleate (0, 10, 100 μM) displays tonic and use-dependent block to Na currents in rat cardiomyocytes with a IC50 of 312 μM[3].
Unlike Metoclopramide, Domperidone monomaleate does not cause any adverse neurological symptoms as it has minimal penetration through the blood-brain barrier[1].
Domperidone monomaleate acts as both an antiemetic and an upper gastrointestinal tract prokinetic agent. It is rapidly absorbed after oral administration, and few side effects have been reported[2].
| Catalog Number | I043291 |
| CAS Number | 83898-65-1 |
| Synonyms | (Z)-but-2-enedioic acid;6-chloro-3-[1-[3-(2-oxo-3H-benzimidazol-1-yl)propyl]piperidin-4-yl]-1H-benzimidazol-2-one |
| Molecular Formula | C26H28ClN5O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H24ClN5O2.C4H4O4/c23-15-6-7-20-18(14-15)25-22(30)28(20)16-8-12-26(13-9-16)10-3-11-27-19-5-2-1-4-17(19)24-21(27)29;5-3(6)1-2-4(7)8/h1-2,4-7,14,16H,3,8-13H2,(H,24,29)(H,25,30);1-2H,(H,5,6)(H,7,8)/b;2-1- |
| InChIKey | OAUUYDZHCOULIO-BTJKTKAUSA-N |
| SMILES | C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O.C(=CC(=O)O)C(=O)O |
| Reference | [1]. Reddymasu SC, et al. Domperidone: review of pharmacology and clinical applications in gastroenterology. Am J Gastroenterol. 2007;102(9):2036-2045. [2]. Champion MC, et al. Domperidone, a new dopamine antagonist. CMAJ. 1986;135(5):457-461. [3]. Stoetzer C, et al. Cardiotoxic Antiemetics Metoclopramide and Domperidone Block Cardiac Voltage-Gated Na+ Channels. Anesth Analg. 2017 Jan. 124(1):52-60. |
