product name Domperidone
Description: Domperidone is an orally bioactive dopamine D2 receptor antagonist. Domperidone is a useful alternative to metoclopramide for treatment of gastroparesis due to better tolerability. 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.
References: J Agric Food Chem. 2011 Sep 14;59(17):9691-9; Bull Exp Biol Med. 2013 Oct;155(6):705-7.
425.91
Formula
C22H24ClN5O2
CAS No.
57808-66-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (112.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19414436
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| References | J Agric Food Chem. 2011 Sep 14;59(17):9691-9; Bull Exp Biol Med. 2013 Oct;155(6):705-7. |
