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MedChemExpress - Model Domperidone monomaleate - 83898-65-1

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].

Domperidone monomaleate

MCE China：Domperidone monomaleate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0411A

CAS：83898-65-1

Synonyms：R33812 monomaleate

Purity：99.76%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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. [Content Brief]

[2]. Champion MC, et al. Domperidone, a new dopamine antagonist. CMAJ. 1986;135(5):457-461. [Content Brief]

[3]. Stoetzer C, et al. Cardiotoxic Antiemetics Metoclopramide and Domperidone Block Cardiac Voltage-Gated Na+ Channels. Anesth Analg. 2017 Jan. 124(1):52-60. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。