货号 | 11983-1mg |
描述 | Sonepiprazole is a selective antagonist of the dopamine 4 (D4) receptor (Kis = 10 nM). It is highly selective over D1, D2, and D3 receptors, serotonin 1A and 2 receptors, as well as α1- and α2-adrenergic receptors (Kis > 2,000 nM).1,2 Its safety profile in rat studies is improved in comparison to classical antipsychotics but it is not effective for positive or negative symptoms of schizophrenia in patients.1,3 In a pharmacological model of stress exposure in rhesus monkeys, sonepiprazole reverses stress-induced cognitive deficits.4 |
别名 | PNU 101387;U-101387; |
供应商 | Cayman |
应用文献 | |
1.Merchant, K.M.,Gill, G.S.,Harris, D.W., et al. Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. J. Pharmacol. Exp. Ther. 279(3), 1392-1403 (1996). 2.Tenbrink, R.E.,Bergh, C.L.,Duncah, J.N., et al. (S)-(−)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. J. Med. Chem. 39(13), 2435-2437 (1996). 3.Corrigan, M.H.,Gallen, C.C.,Bonura, M.L., et al. Effectiveness of the selective D4 antagonist sonepiprazole in schizophrenia: A placebo-controlled trial. Biol. Psychiatry 55(5), 445-451 (2004). 4.Arnsten, A.F.T.,Murphy, B., and Merchant, K. The selective dopamine D4 receptor antagonist, PNU-101387G, prevents stress-induced cognitive deficits in monkeys. Neuropsychopharmacology 23(4), 405-410 (2000). | |
运输条件 | Dry ice in continental US; may vary elsewhere |
存放说明 | -80 |
纯度 | ≥98% |
计算分子量 | 401.5 |
分子式 | C21H27N3O3S |
CAS号 | 170858-33-0 |
稳定性 | ≥ 2 years |
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