367514-87-2
367514-87-2 結(jié)構(gòu)式
基本信息
魯拉西酮
鹽酸魯拉西酮API
魯拉西酮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
物理化學(xué)性質(zhì)
常見問題列表
2010年10月28日美國FDA批準(zhǔn)鹽酸魯拉西酮（lurasidone HCI）每日一次片劑用于精神分裂癥患者一線治療，其商品名為Latuda。
用法與用量：推薦起始劑量為40 mg·d，有效劑量范圍為40～120 mg·d，最大推薦劑量為80 mg·d。應(yīng)與食物同時(shí)服用。
不良反應(yīng)：常見的不良反應(yīng)有嗜睡、靜坐不能、惡心、帕金森病癥樣癥狀和情緒激動(dòng)焦慮。魯拉西酮無身體依賴性，較少引起體重增加，不引起葡萄糖、脂質(zhì)（類脂）、ECG和QT間期改變。
| 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).