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Domperidone monomaleate

CAS No. : 83898-65-1

MCE 國際站：Domperidone monomaleate

產(chǎn)品活性：Domperidone (R33812) monomaleate 是一種具有口服活性和選擇性的多巴胺-2 受體 (dopamine-2 receptor) 拮抗劑。Domperidone monomaleate 通過影響胃和小腸的化學(xué)感受器觸發(fā)區(qū)和運動功能，起到止吐和促動力劑作用。

研究領(lǐng)域：GPCR/G Protein  |  Neuronal Signaling

作用靶點：Dopamine Receptor

In Vitro: Cardiac Na⁺ channels are common targets of therapeutics inducing cardiotoxicity.
Domperidone monomaleate (0-1000 μM) displays concentration- and state-dependent inhibitory of Nav1.5 in Human embryonic kidney HEK293 cells.
Domperidone monomaleate (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 monomaleate does not cause any adverse neurological symptoms as it has minimal penetration through the blood-brain barrier.
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.

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