Home Neuronal Signaling Dopamine Receptor inhibitor Domperidone

research use only

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.
Domperidone Dopamine Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 425.91

Jump to

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

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05570292 Completed
Gastric Residual Volume
Ain Shams University
 October 10 2022 Phase 3
NCT04653584 Terminated
Parkinson Disease
Assistance Publique - Hôpitaux de Paris
 January 1 2021 --
NCT03837067 Completed
Parkinson''s Disease
Assistance Publique - Hôpitaux de Paris
 July 17 2018 --
NCT01710462 Withdrawn
Gastroesophageal Reflux Disease
Eurofarma Laboratorios S.A.
 August 2013 Phase 3
NCT01907633 Completed
Death Sudden Cardiac
Janssen Research & Development LLC
 December 2011 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map