Domperidone (monomaleate)

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]. 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].