Domperidone (R33812) monomaleate 是一种具有口服活性和选择性的多巴胺-2 受体 (dopamine-2 receptor) 拮抗剂。Domperidone monomaleate 通过影响胃和小肠的化学感受器触发区和运动功能,起到止吐和促动力剂作用。
产品描述
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].
体外活性
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 IC 50 of 312 μM [3].
体内活性
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].
Cas No.
83898-65-1
分子式
C26H28ClN5O6
分子量
541.98
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years