鲁拉西
鲁拉西酮(Lurasidone)
CAS: 367514-87-2
化学式: C28H36N4O2S
| 中文名 | 鲁拉西酮 |
| 英文名 | Lurasidone |
| 别名 | 鲁拉西 卢拉西酮 鲁拉西酮 盐酸鲁拉西酮API 鲁拉西酮(仅供中间体) 鲁拉西酮LURASIDONE |
| 英文别名 | urasidone lurasidone Lurasidone Lurasidone Base Lurasidone (SM13496) (3aR,4S,7R,7aS)-2-((1R,2R)-2-(4-(1,2-Benzothiazol-3-yl)piperazin-1-ylmethyl)cyclohexylmethyl)hexahydro-4,7-methano-2H-isoindole-1,3-dione (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl}cyclohexyl]methyl}hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]Methyl}cyclohexyl]Methyl}hexahydro-1H-4,7-Methanoisoindole-1,3(2H)-dione (3aR,4S,7R,7aS)-2-[[(1R,2R)-2-[[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]methyl]hexahydro-4,7-methano-1H-isoindole-1,3(2H)-dione |
| CAS | 367514-87-2 |
| EINECS | 696-042-8 |
| 化学式 | C28H36N4O2S |
| 分子量 | 492.68 |
| InChI | InChI=1/C28H36N4O2S/c33-27-24-18-9-10-19(15-18)25(24)28(34)32(27)17-21-6-2-1-5-20(21)16-30-11-13-31(14-12-30)26-22-7-3-4-8-23(22)35-29-26/h3-4,7-8,18-21,24-25H,1-2,5-6,9-17H2/t18-,19+,20-,21-,24+,25-/m0/s1 |
| 密度 | 1.273 |
| 熔点 | 146-149°C |
| 沸点 | 623.4±55.0 °C(Predicted) |
| 闪点 | 330.8°C |
| 蒸汽压 | 1.85E-15mmHg at 25°C |
| 溶解度 | 氯仿 (微溶)，DMSO (微溶，加热)，甲醇 (微溶，加热) |
| 折射率 | 1.636 |
| 酸度系数 | 8.41±0.50(Predicted) |
| 存储条件 | -20°C Freezer |
| 外观 | 固体 |
| 颜色 | White to Off-White |
| 体外研究 | Lurasidone (SM-13496) is an antagonist of dopamine D 2 and 5-HT 7 with IC 50 s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT 1A receptor with an IC 50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D 2 and 5-HT 2A receptors higher than other tested antipsychotics. Lurasidone (SM-13496) does not increase [ 35 S]GTPγS binding to the membrane preparations for dopamine D 2 receptors by itself, but it antagonizes dopamine-stimulated [ 35 S]GTPγS binding in a concentration-dependent manner with a K B value of 2.8±1.1 nM. |
| 体内研究 | Lurasidone (SM-13496) dose-dependently increases the ratio of DOPAC/dopamine in frontal cortex and striatum, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (SM-13496) (ED 50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED 50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED 50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED 50 values 0.44 to 1.7 mg/kg). Lurasidone (SM-13496) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED 50 values are 6.3 mg/kg. Lurasidone (SM-13496) dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED 50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (SM-13496) (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p<0.01). |
| 参考资料 展开查看 | 1. [IF=3.119] Jinrui Zhang et al."In silico study on identification of novel MALT1 allosteric inhibitors."Rsc Adv. 2019 Nov;9(67):39338-39347 2. [IF=4.411] Xin Meng et al."Drug Repurposing for Influenza Virus Polymerase Acidic (PA) Endonuclease Inhibitor."Molecules. 2021 Jan;26(23):7326 |
鲁拉西 - 简介
鲁拉西酮（lysergic acid diethylamide，简称LSD）是一种强烈的致幻剂，也被称为迷幻药。它是由麦角酸经过一系列的化学合成得到的。鲁拉西酮是一种无色无臭的晶体，通常以纸片或小饼干等形式存在。
其在服用后可以产生一系列的感知和认知改变，包括视觉、听觉和情绪上的变化，使人产生幻觉和幻听等现象。鲁拉西酮被广泛用于心理研究、神经科学研究和心灵探索等领域。
鲁拉西酮的制法主要是通过对麦角酸进行化学合成得到。具体来说，首先将麦角酸与乙酸酐反应，得到乙酰麦角酐，然后通过跟乙醇反应，得到乙酰麦角酸乙酯。通过水解或酸水解，得到鲁拉西酮。
其在服用后可以产生一系列的感知和认知改变，包括视觉、听觉和情绪上的变化，使人产生幻觉和幻听等现象。鲁拉西酮被广泛用于心理研究、神经科学研究和心灵探索等领域。
鲁拉西酮的制法主要是通过对麦角酸进行化学合成得到。具体来说，首先将麦角酸与乙酸酐反应，得到乙酰麦角酐，然后通过跟乙醇反应，得到乙酰麦角酸乙酯。通过水解或酸水解，得到鲁拉西酮。
最后更新：2024-04-09 21:32:00
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