Molecular Formula | C28H36N4O2S |
Molar Mass | 492.684 |
Melting Point | 198-205°C |
Flash Point | 9℃ |
Storage Condition | Refrigerator |
In vitro study | Lurasidone dose-dependently antagonized [35S] gtpγs binding at the dopamine-stimulated human dopamine D2L receptor with a KB value of 2.8 nM. Lurasidone antagonized 5-HT stimulated cAMP accumulation in CHO/h5-HT7 cells with a KB value of 2.6 nM. Lurasidone partially stimulated [35S] gtpγs binding to the membrane formulation of the human 5-HT1A receptor with a maximal effect of 33%. Lurasidone dose-dependently increased the DOPAC/dopamine ratio in the frontal cortex and striatum of rats. |
In vivo study | Lurasidone inhibits MAP-induced hyperactivity, which can last more than 8 hours, with 2.3 mg/kg,0.87 mg/kg,1.6 mg/kg, the ED50 values were 1 hour, 2 hours, 4 hours and 8 hours, respectively, for the 5.0 mg/kg dose treatment. Lurasidone (1-10 mg/kg) dose-dependently suppressed the conditioned avoidance response in rats with an ED50 of 6.3 mg/kg. Lurasidone dose-dependently inhibited 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. In the Vogel conflict test, Lurasidone (0.3 mg/kg-30 mg/kg) dose-dependently significantly increased the number of startle in rats, with a MED of 10 mg/kg. Lurasidone (3 mg/kg, 2 weeks) significantly inhibited hyperactivity in olfactory bulb-excised rats. Lurasidone (700 mg/kg-1000 mg/kg) dose-dependently slightly prolonged the duration of cyclohexenobarbitone (Anesthesia)-induced loss of the righting reflex in mice. Lurasidone (30 mg/kg, p.o.) significantly dose-dependently reversed the MK-801-induced attenuation of passive response avoidance in rats. Lurasidone (3 mg/kg p.o.) effectively reversed MK-801-induced learning disorder in rats in the water maze test. In the radial arm maze test, Lurasidone (3 mg/kg p.o.) the MK-801-induced reference memory impairment was effectively reversed and the MK-801-induced working memory impairment was moderately and not significantly attenuated. Treatment with Lurasidone (10 mg/kg) increased total BDNF mRNA levels in the prefrontal cortex and hippocampus (to a lesser extent) of rats. Lurasidone (10 mg/kg) significantly increased the levels of mature BDNF protein in the prefrontal cortex of rats without affecting the protein levels of neurotrophic factors (precursor and mature forms) in hippocampal extracts. |
Risk Codes | R11 - Highly Flammable R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R39/23/24/25 - |
Safety Description | S7 - Keep container tightly closed. S16 - Keep away from sources of ignition. S36/37 - Wear suitable protective clothing and gloves. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
WGK Germany | 1 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.89 ml | 9.449 ml | 18.899 ml |
5 mM | 0.378 ml | 1.89 ml | 3.78 ml |
10 mM | 0.189 ml | 0.945 ml | 1.89 ml |
5 mM | 0.038 ml | 0.189 ml | 0.378 ml |