| Bioactivity | Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone 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]. | ||||||||||||
| Invitro | Cardiac Na+ channels are common targets of therapeutics inducing cardiotoxicity[3].Domperidone (0-1000 μM) displays concentration- and state-dependent inhibitory of Nav1.5 in Human embryonic kidney HEK293 cells[3].Domperidone (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 (R33812) does not cause any adverse neurological symptoms as it has minimal penetration through the blood-brain barrier[1].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[2]. | ||||||||||||
| Name | Domperidone | ||||||||||||
| CAS | 57808-66-9 | ||||||||||||
| Formula | C22H24ClN5O2 | ||||||||||||
| Molar Mass | 425.91 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Reddymasu SC, et al. Domperidone: review of pharmacology and clinical applications in gastroenterology. Am J Gastroenterol. 2007;102(9):2036-2045. [2]. Champion MC, et al. Domperidone, a new dopamine antagonist. CMAJ. 1986;135(5):457-461. [3]. Stoetzer C, et al. Cardiotoxic Antiemetics Metoclopramide and Domperidone Block Cardiac Voltage-Gated Na+ Channels. Anesth Analg. 2017 Jan. 124(1):52-60. |
Domperidone
CAS: 57808-66-9 F: C22H24ClN5O2 W: 425.91
Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic
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