S88014 |
Ocaperidone |
源叶(MedMol) | ≥98% |
- 产品描述: Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
- 靶点: 5-HT2 Receptor:0.14 nM (Ki);D2 Receptor:0.75 nM (Ki);5-HT1A Receptor:L7.6 (pEC50, h5-HT1A);5-HT1A Receptor:8.08 (pKi, h5-HT1A);a1-adrenergic receptor:0.46 nM (Ki);Histamine H1:1.6 nM (Ki);a2-adrenergic receptor:5.4 nM (Ki);DopamineReceptor; 5-HTReceptor
- 体内研究:
Ocaperidone shows a potent occupation of 5HT2 receptor via in vivo binding in the frontal cortex of rats with an ED50 of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D2 receptor in the striatum and the nucleus accumbens. Ocaperidone (R 79598) antagonizes dopamine D2 and 5-HT2, and shows a a partial generalization to buspirone with an ED50 of 0.163 mg/kg.
- 参考文献:
1. Leysen JE, et al. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Mol Pharmacol. 1992 Mar;41(3):494-508. 2. Cosi C, et al. Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT(1A) receptors expressed in HeLa cells. Eur J Pharmacol. 2001 Dec 14;433(1):55-62. 3. Rijnders HJ, et al. The discriminative stimulus properties of buspirone involve dopamine-2 receptor antagonist activity. Psychopharmacology (Berl). 1993;111(1):55-61.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.378 ml 11.891 ml 23.782 ml 5 mM 0.476 ml 2.378 ml 4.756 ml 10 mM 0.238 ml 1.189 ml 2.378 ml 50 mM 0.048 ml 0.238 ml 0.476 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)