Domperidone

SKU: orb1224606

Description

Domperidone(Motilium) is a dopamine blocker and an antidopaminergic reagent. It blocks the action of. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 57808-66-9
• MW: 425.92
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₄ClN₅O₂
• SMILES: O=C1NC2=CC(Cl)=CC=C2N1C3CCN(CCCN4C5=CC=CC=C5NC4=O)CC3
• Target: Dopamine Receptor
• Solubility: Ethanol: 1 mg/mL (2.34 mM); DMSO: 48 mg/mL (112.69 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Motilium | NSC 299589

Quick Database Links

Gene Symbol

Dopamine Receptor