367514-87-2
基本信息
鲁拉西酮
盐酸鲁拉西酮API
鲁拉西酮LURASIDONE
lurasidone
Lurasidone Base
Lurasidone, >=98%
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-Benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]methyl]hexahydro-4,7-methano-1H-isoindole-1,3(2H)-dione
4-{[(1R,2R)-2-{[4-(2$l^{4}-thia-6-azatricyclo[5.4.0.0^{2,6}]undeca-1(11),2,4,7,9-pentaen-5-yl)piperazin-1-yl]Methyl}cyclohexyl]Methyl}-4-azatricyclo[5.2.1.0^{2,6}]deca-1(9),2(6),7-triene-3,5-dione
物理化学性质
| 熔点 | 146-149°C |
| 沸点 | 623.4±55.0 °C(Predicted) |
| 密度 | 1.273 |
| 储存条件 | -20°C冷冻 |
| 溶解度 | 氯仿（微溶）、DMSO（微溶、加热）、甲醇（微溶、加热) |
| 酸度系数(pKa) | 8.41±0.50(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至灰白色 |
| InChIKey | PQXKDMSYBGKCJA-CVTJIBDQSA-N |
| SMILES | C1(=O)[C@]2([H])[C@@]([H])([C@]3([H])C[C@@]2([H])CC3)C(=O)N1C[C@@H]1CCCC[C@H]1CN1CCN(C2C3=C(SN=2)C=CC=C3)CC1 |
| CAS 数据库 | 367514-87-2 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302 |
| 防范说明 | P280-P305+P351+P338 |
| 毒害物质数据 | 367514-87-2(Hazardous Substances Data) |
常见问题列表
2010年10月28日美国FDA批准盐酸鲁拉西酮（lurasidone HCI）每日一次片剂用于精神分裂症患者一线治疗，其商品名为Latuda。
用法与用量：推荐起始剂量为40 mg·d，有效剂量范围为40～120 mg·d，最大推荐剂量为80 mg·d。应与食物同时服用。
不良反应：常见的不良反应有嗜睡、静坐不能、恶心、帕金森病症样症状和情绪激动焦虑。鲁拉西酮无身体依赖性，较少引起体重增加，不引起葡萄糖、脂质（类脂）、ECG和QT间期改变。
| Target | Value |
|
5-HT2A
(Cell-free assay) | 0.5 nM(Ki) |
|
5-HT7 receptor
(Cell-free assay) | 0.5 nM(Ki) |
|
D2 receptor
(Cell-free assay) | 1 nM(Ki) |
|
5-HT1A receptor
(Cell-free assay) | 6.4 nM(Ki) |
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.
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).