Fig. 1 · Structure

Cat. No.: A10329
CAS No.: 57808-66-9
Formula: C₂₂H₂₄ClN₅O₂
Mol. Weight: 425.91

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Domperidone

Name: Domperidone
Brand: Adooq Bioscience
SKU: A10329
Availability: InStock
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Cat. No. A10329 CAS 57808-66-9

Domperidone blocks the action of dopamine. 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).

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Biological Activity

Target & Activity

Target	Activity	Value
Dopamine D2 receptor

Cellular Effect

Cell Line	Activity	Value	Description	Reference
HEK293	IC50	14.8 μM	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC50	2.3 μM	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC50	7.9 μM	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]

In Vitro Studies

Domperidone inhibited recombinant hERG current in a multi-laboratory manual patch-clamp study. Corrected IC50 estimates differed across laboratories. These measurements describe an off-target ion-channel effect and should be interpreted with the assay conditions and laboratory variability. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Domperidone inhibition of recombinant hERG current across laboratories

Cell-based study · hERG1a-expressing CHO cells (Lab 1) and HEK293 cells (Labs 2, 4, 5); Lab 3 did not participate in Phase 2. [1]

All four participating laboratories yielded fitted domperidone hERG-block IC50 estimates. Values depend on laboratory conditions and concentration correction; they are not D2-receptor potencies or treatment doses.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Inhibition of E-4031-sensitive outward ramp current	IC50 Lab 1: 0.10 ± 0.016 µM; Lab 2: 0.035 ± 0.0058 µM; Lab 4: 0.029 ± 0.0032 µM; Lab 5: 0.039 ± 0.0086 µM (fitted estimate ± 95% CI as displayed in Supplemental Table 6).	[1]

Literature-Reported Treatment Conditions

Method: Concentration-response patch-clamp recordings with baseline and terminal E-4031 subtraction; Phase 2 concentration correction used real samples for Lab 2 and satellite samples for other laboratories.
Reported limits: Total exposure duration, domperidone-specific cell counts and full nominal concentration series were not extracted. IC50 values are assay endpoints. No single common vehicle is assigned.

Methods and source locations

Compound reported in the paper: Domperidone; Compound label in the paper: Phase 2 drug

Reported compound-level effects across the study. No attribution of an anonymous lab potency to AdooQ material and no current-lot validation.

Supplemental Table 6, domperidone row 25 and unit/CI note row 36; Table 1 row 25; Table 2; Methods: Estimation of drug potencies; Fig. 4

Inhibition of E-4031-sensitive outward ramp current: Manual whole-cell patch clamp near physiological temperature; 0.2-Hz step-ramp waveform; Hill fit using drug-loss-corrected concentrations. — Supplemental Table 6: B25:C25, F25:G25, N25:O25, R25:S25; row 36; Methods: Estimation of drug potencies

In Vivo Studies

In male Wistar rats exposed to chronic intermittent hypoxia, domperidone in drinking water during the last 15 days lowered elevated mean arterial pressure. At 0.75 mg/day, respiratory frequency, tidal volume and minute ventilation did not change significantly under the tested breathing conditions. These model-specific findings do not establish human efficacy. [2]

Chronic oral domperidone in rats exposed to intermittent hypoxia

Animal study · Young adult male Wistar rats: control or 30-day chronic intermittent hypoxia (CIH), with or without oral DOM during the last 15 days. [2]

Chronic DOM reduced elevated mean arterial pressure in CIH rats. Respiratory frequency, tidal volume and minute ventilation showed no significant DOM-related differences in the tested conditions. The result does not establish human efficacy or general cardiac safety.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Mean arterial pressure in CIH rats	mean ± SD CIH: 134 ± 32 mmHg; CIH + 0.75 mg/day DOM: 95 ± 28 mmHg (p < 0.05 vs CIH); CIH + 1.5 mg/day DOM: 82 ± 25 mmHg (p < 0.01 vs CIH); 6–10 animals per caption.	[2]
Respiratory frequency, tidal volume and minute ventilation in control and CIH groups	between-group comparison No statistically significant differences reported with 0.75 mg/day DOM for 15 days; Table 1 reports mean and SD of eight individual values per group.	[2]

Conditions shared by the study groups

Route: Oral, in drinking water
Frequency: Daily delivery through drinking water
Treatment course: 15 days, during the final half of CIH exposure
Vehicle: Drinking water; additional formulation details not specified

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Chronic DOM in CIH rats 0.75 or 1.5 mg/day (MAP); 0.75 mg/day (ventilation)	CIH without DOM; parallel normoxic control and normoxic DOM groups	Lower MAP in CIH animals; no significant effect on ventilation at the lower dose.	[2]

Chronic DOM in CIH rats: Model: Young adult male Wistar rats exposed to CIH for 30 days; Reported limits: Daily doses are the authors’ reported administered amounts; measured systemic exposure was not extracted.

Methods and source locations

Compound reported in the paper: Domperidone; Compound label in the paper: DOM

Rat findings for the reported domperidone material; no formulation equivalence or SKU-specific validation claim.

Results 2.1, Fig. 2A–B and caption; Results 2.3, Table 1; Methods 4.1–4.3, 4.6

Mean arterial pressure in CIH rats: Arterial catheter recording under anesthesia; one-way ANOVA with Tukey multiple comparisons. — Results 2.1; Fig. 2B and caption; Methods 4.1, 4.2, 4.6

Respiratory frequency, tidal volume and minute ventilation in control and CIH groups: Whole-body unrestrained plethysmography during air, hypoxia and hypercapnia tests; two-way ANOVA. — Results 2.3, Table 1 and caption; Methods 4.1, 4.3, 4.6

Chronic DOM in CIH rats · Results 2.1, Fig. 2A–B and caption; Results 2.3, Table 1; Methods 4.1–4.3, 4.6

Specifications

Manufacturer	Adooq Bioscience
CAS Number	57808-66-9
Formula	C₂₂H₂₄ClN₅O₂
Molecular Weight	425.91
SMILES	C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	47 mg/mL (110.34 mM)
Water	Insoluble
Ethanol	1 mg/mL (2.34 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Alvarez Baron C, Zhao J, Yu H, et al. Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices. Scientific reports (2025). PMID: 40819150 DOI: 10.1038/s41598-025-15761-8 Source material
[2] Olea E, Docio I, Quintero M, et al. Peripheral Dopamine 2-Receptor Antagonist Reverses Hypertension in a Chronic Intermittent Hypoxia Rat Model. International journal of molecular sciences (2020). PMID: 32664461 DOI: 10.3390/ijms21144893 Source material

Publications

2 publications citing this product

Claudia Alvarez Baron, .et al. , Sci Rep, 2025, Aug 16;15(1):29995 PMID: 40819150
Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967