83898-65-1

83898-65-1 structure
83898-65-1 structure

Name domperidone maleate
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
Domperidone (TN)
Prestwick-06G02
5-Chloro-1-(1-(3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)propyl)piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one maleate
Domperidone Maleate
Description 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].
Related Catalog
In Vitro 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].
In Vivo 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].
References

[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.

Molecular Formula C26H28ClN5O6
Molecular Weight 541.98300
Exact Mass 541.17300
PSA 153.42000
LogP 3.00290
HS Code 2942000000
HS Code 2942000000
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