Domperidone - Moligand™, 10mM in DMSO , Dopamine D2 receptor antagonist, CAS No.57808-66-9, Dopamine D2 receptor antagonist

CAS: 57808-66-9 Cat. No.: D409098 Molecular Weight: 425.91 EC Number: 260-968-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

5-​chloro-​1-​[1-​[3-​(2,​3-​dihydro-​2-​oxo-​1H-​benzimidazol-​1-​yl)​propyl]​-​4-​piperidinyl]​-​1,​3-​dihydro-2H-​benzimidazol-​2-​one

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Domperidone is an oraldopamine D2 receptorantagonist, used to treat nausea and vomiting.
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. 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.
Cell Data

cell lines：SET-2 and TEL-JAK Ba/F3 cells

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

5-​chloro-​1-​[1-​[3-​(2, ​3-​dihydro-​2-​oxo-​1H-​benzimidazol-​1-​yl)​propyl]​-​4-​piperidinyl]​-​1, ​3-​dihydro-2H-​benzimidazol-​2-​one

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Dopamine D2 receptor antagonist

Product Properties

• ALogP: 3.9

Names and Identifiers

• Isomeric SMILES: C1CN(CCC1N2C3=C(C=C(C=C3)Cl)NC2=O)CCCN4C5=CC=CC=C5NC4=O
• WGK Germany: 3
• RTECS: DE2275900
• Molecular Weight: 425.91
• Reaxy-Rn: 903774
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=903774&ln=

Associated Targets(Human)

DRD2 Tclin D(2) dopamine receptor (4 Activities)

Discover Target: DRD2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor (5 Activities)

Discover Target: DRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A (2 Activities)

Discover Target: HTR2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (6 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro 5%TFA 3.06 mg/mL (17.37 mM); DMSO: 0.1 mg/mL (0.56 mM); Water: Insoluble
• Melt Point(°C): 243°C

References

1. Yang Zhou, Lei Guo, Zhiheng Zhao, Sisi Zheng, Yue Xu, Bin Xiang, Savaş Kaya.  (2018)  Anticorrosion potential of domperidone on copper in different concentration of hydrochloric acid solution.  JOURNAL OF ADHESION SCIENCE AND TECHNOLOGY,      [PMID:] [10.1080/01694243.2018.1426542]

2. Yanxia Liu, Xiuquan Yao, Chunlin Liu, Xiaofang Luo, Chao Guo, Wei Du.  (2023)  The Drug Domperidone as a Corrosion Inhibitor for X60 Steel in Hydrochloric Acid Solution.  International Journal of Electrochemical Science,      [PMID:] [10.20964/2022.04.55]