| 货号 | 16222-50mg |
| 描述 | Pimozide is an antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively).1,2 It also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at serotonin, α-adrenergic, muscarinic cholinergic, and histamine receptors and calcium and sodium channels.2,3,4,5,6 Pimozide is metabolized in the liver primarily by cytochrome P450 (CYP) 3A4, but CYP2D6, an isoform known to be genetically variable, can also affect metabolism.7 Pimozide has diverse neuropathological applications, including in Tourette syndrome.7 |
| 别名 | NSC 170984;Orap;R 6238; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Burstein, E.S.,Ma, J.,Wong, S., et al. Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist. Journal of Pharmacology and Experimental Therapeutics 315(3), 1278-1287 (2005). 2.Seeman, P. Atypical antipsychotics: Mechanism of action. Can.J.Psychiatry 47(1), 27-38 (2002). 3.Lau, J.F.,Jeppesen, C.B.,Rimvall, K., et al. Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides. Bioorganic & Medicinal Chemistry Letters 16(20), 5303-5308 (2006). 4.Roufos, I.,Hay, S. and Schwarz, R.D. A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers. Journal of Medicinal Chemistry 39(7), 1514-1520 (1996). 5.Cusack, B.,Nelson, A. and Richelson, E. Binding of antidepressants to human brain receptors: Focus on newer generation compounds. Psychopharmacology (Berl) 114(4), 559-565 (1994). 6.Richelson, E. and Souder, T. Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sciences 68(1), 29-39 (2000). 7.Rogers, H.L.,Bhattaram, A.,Zineh, I., et al. CYP2D6 genotype information to guide pimozide treatment in adult and pediatric patients: Basis for the US Food and Drug Administration’s new dosing recommendations. J.Clin.Psychiatry 73(9), 1187-1190 (2012). | |
| 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 | 461.6 |
| 分子式 | C28H29F2N3O |
| CAS号 | 2062-78-4 |
| 稳定性 | ≥ 2 years |
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