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Domperidone

CAS No. : 57808-66-9

MCE 国际站：Domperidone

产品活性：Domperidone (R33812) 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 通过影响胃和小肠的化学感受器触发区和运动功能，起到止吐和促动力作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

In Vitro: Cardiac Na⁺ channels are common targets of therapeutics inducing cardiotoxicity.
Domperidone (0-1000 μM) displays concentration- and state-dependent inhibitory of Nav1.5 in Human embryonic kidney HEK293 cells.
Domperidone (0, 10, 100 μM) displays tonic and use-dependent block to Na currents in rat cardiomyocytes with a IC₅₀ of 312 μM.

In Vivo: Unlike Metoclopramide, Domperidone (R33812) does not cause any adverse neurological symptoms as it has minimal penetration through the blood-brain barrier.
Domperidone 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.

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