货号 | 18875-25mg |
描述 | Domperidone is a dopamine receptor antagonist that does not readily cross the blood-brain barrier.1 It demonstrates a potent affinity for the rat D2 receptor with a Ki value of 0.3 nM (IC50 = 13.6 nM) and is also reported to inhibit the rat D3 receptor with an IC50 value of 2.68 nM.2,3,4 Both antiemetic and upper gastrointestinal tract prokinetic activities of domperidone have been evaluated in clinical trials.1,5 |
别名 | Motilium;NSC 299589; |
供应商 | Cayman |
应用文献 | |
1.Champion, M.C.,Hartnet, M. and Yen, M. Domperidone, a new dopamine antagonist. Canadian Medical Association Journal 135(5), 457-461 (1986). 2.Lin, C.,McGonigle, P. and Molinoff, P.B. Characterization of D-2 dopamine receptors in a tumor of the rat anterior pituitary gland. Journal of Pharmacology and Experimental Therapeutics 242, 950-956 (1987). 3.Hirokawa, Y.,Fujiwara, I.,Suzuki, K., et al. Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity. Journal of Medicinal Chemistry 46(5), 702-715 (2003). 4.Sokoloff, P.,Giros, B.,Martres, M.P., et al. Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature 137(6289), 146-151 (1990). 5.Wilson, D.B. and Dundee, J.W. Evaluation of the anti-emetic action of domperidone. Anaesthesia 34(8), 765-767 (1979). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 425.9 |
分子式 | C22H24ClN5O2 |
CAS号 | 57808-66-9 |
稳定性 | ≥ 2 years |
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