受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | SM-13496 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
|
化学式 | C28H36N4O2S.HCl |
|||
分子量 | 529.14 | CAS No. | 367514-88-3 | |
Solubility (25°C)* | 体外 | 4-Methylpyridine | 15 mg/mL warmed with 50ºC water bath (28.34 mM) | |
DMSO | 1 mg/mL (1.88 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Lurasidone (SM-13496) is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively. |
---|---|
in vitro | Lurasidone antagonizes dopamine-stimulated [35S]GTPγS binding at human dopamine D2L receptor in a concentration-dependent manner with a KB value of 2.8 nM. Lurasidone antagonizes 5-HT-stimulated cAMP accumulation in the CHO/h5-HT7 cells with a KB value of 2.6 nM. Lurasidone partially stimulates [35S]GTPγS binding to the membrane preparation for human 5-HT1A receptors with a maximum effect of 33%. Lurasidone dose-dependently increases the ratio of DOPAC/dopamine in rat frontal cortex and striatum. [1] |
in vivo | The inhibitory actions of Lurasidone on MAP-induced hyperactivity persists for more than 8 hours, and the ED50 values of the action at 1 hour, 2 hours, 4 hours, and 8 hours after the treatment are 2.3 mg/kg, 0.87 mg/kg, 1.6 mg/kg, and 5.0 mg/kg, respectively. Lurasidone (1 mg/kg–10 mg/kg) dose-dependently inhibits conditioned avoidance response in rats with ED50 of 6.3 mg/kg. Lurasidone dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia in rats with ED50 of 5.6 mg/kg and 3.0 mg/kg, respectively. Lurasidone (0.3 mg/kg–30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the Vogel's conflict test with MED of 10 mg/kg. Lurasidone (3 mg/kg, 2 weeks) significantly suppresses hyperactivity behavior in olfactory bulbectomy model rats. Lurasidone (700 mg/kg–1000 mg/kg) slightly prolongs the duration of loss of righting reflexes elicited by hexobarbital (anesthesia) in mice in a dose-dependent manner. [1] Lurasidone (30 mg/kg, p.o.) significantly and dose-dependently reverses the MK-801-induced impairment of the passive-avoidance response of rats. [2] Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced learning impairment in the Morris water maze test in rats. Lurasidone (3 mg/kg p.o.) potently reverses MK-801-induced reference memory impairment and moderately but not significantly attenuates MK-801-induced working memory impairment in the radial-arm maze test. [3] Lurasidone (10 mg/kg) treatment increases total BDNF mRNA levels in rat prefrontal cortex and, to less extent, in hippocampus. Lurasidone (10 mg/kg) significantly increases the levels of mature BDNF protein in rat prefrontal cortex, without affect the protein levels of the neurotrophin (both precursor and mature forms) in hippocampal extracts. [4] |
Amisulpride as a potential disease-modifying drug in the treatment of tauopathies [ Alzheimers Dement, 2023, 10.1002/alz.13090] | PubMed: 37218673 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。