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Domperidone Dopamine Receptor inhibitor

Cat.No.S2461

Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting. This compound acts by blocking dopamine receptors, which helps to reduce symptoms of gastrointestinal distress. It is often prescribed for its antiemetic effects.
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Quality Control

Batch: Purity: 99.92%
99.92

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (112.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 425.91 Formula

C22H24ClN5O2

Storage (From the date of receipt)
CAS No. 57808-66-9 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O

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Mechanism of Action

Targets/IC50/Ki
Dopamine D2 receptor
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.
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. This compound (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. It (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. This chemical 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. They have higher Mammary gland scores and serum prolactin concentration. It (5 mg/kg, oral) increases peak plasma acetaminophen concentration and area under the curve in rats, indicating increased gastric emptying. This compound decreases the dopamine-induced contractile activity of midjejunal longitudinal muscle strips in rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/14552385/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8067624/
  • [6] https://pubmed.ncbi.nlm.nih.gov/23879848/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-24)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04699591 RECRUITING
GERD; Gastroesophageal Reflux; Gastroparesis
Jose Cocjin
2013-04
NCT06695962 NOT_YET_RECRUITING
Type 1 Diabetic
University Hospital, Rouen
2026-03-01 PHASE3
NCT01696734 RECRUITING
Digestive System Disorder; Dyspepsia; Esophagitis; Gastroesophageal Reflux Disease; Gastroparesis; Heartburn; Nausea and Vomiting
M.D. Anderson Cancer Center
2012-10-23 PHASE3
NCT07578402 NOT_YET_RECRUITING
Dyspepsia; Functioanl Dyspepsia; Epigastric Pain Syndrome; Epigastric Fullness
Rakibul Mostafa
2026-05-15 PHASE4
NCT06590805 RECRUITING
Physical Therapy; Electrotherapy; Dietary Modification
Haytham Ibrahim Morsi
2024-09-01
NCT05570292 COMPLETED
Gastric Residual Volume
Ain Shams University
2022-10-10 PHASE3

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