Domperidone

SKU: orb1310958

Description

Domperidone (R33812, Motilium) is a selective dopamine D2 and D3 receptor antagonist. Its primary action in the chemoreceptor trigger zone (area postrema) makes it a valuable research tool for studying the mechanisms and treatment of nausea and vomiting in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 57808-66-9
• MW: 425.91
• Purity: 99.82%
• Formula: C₂₂H₂₄ClN₅O₂
• SMILES: ClC1=CC2=C(C=C1)N(C1CCN(CCCN3C(=O)NC4=CC=CC=C34)CC1)C(=O)N2
• Target: Dopamine Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.39 mM);DMSO:103 mg/mL (241.84 mM)

Bioactivity

• In Vivo:
  Domperidone (0.1 mg/kg) results in a significant decrease in feeding behavior and stimulation of basal metabolism, but has no effect on locomotor activity of rats in a Phenomaster system. Domperidone (1.1 mg/kg and 5.5 mg/kg, oral) significantly increases laminar microvascular blood flow (LMBF) in horses, compared with baseline values, beginning 4 hours after administration, and this effect persisted for at least 8 hours. Domperidone (0.2 mg/kg, i.v.) significantly increases laminar microvascular blood flow (LMBF) in horses, compared with baseline values, at 10 and 12 hours after administration. Domperidone can ameliorate deleterious reproductive effects and reduce weight gain associated with fescue toxicosis in heifers. Domperidone-treated mares have shorter gestation duration and foaled closer to their expected parturition date than did control mares. Domperidone-treated mares have higher Mammary gland scores and serum prolactin concentration. Domperidone (5 mg/kg, oral) increases peak plasma acetaminophen concentration and area under the curve in rats, indicating increased gastric emptying. Domperidone decreases the dopamine-induced contractile activity of midjejunal longitudinal muscle strips in rats.
• In Vitro:
  Domperidone (a D2R antagonist) inhibits Equilibrative NT1 (ENT1) activity more in the presence than in the absence of Bromocriptine and displays an IC50 value lower than that of Bromocriptine or Ergovaline in Madin-Darby bovine kidney (MDBK) cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

D2, D3, Dopamine Receptor, DopamineReceptor, dopamine, Dopamine, Domperidone, blood-brain barrier, antiemetic, adverse, inhibit, oral, neurological, nausea, Inhibitor, vomit, R33812, R-33812, R 33812, symptoms, prokinetic

Compound Identifiers

PubChem CID

3151