Lurasidone Hcl (SM 13496 Hcl) is an inhibitor of 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.
IC50 Value: 1.68 nM(Dopamine D2); 2.03 nM(5-HT2A); 0.495 nM(5-HT7); 6.75 nM(5-HT1A); 10.8 nM (noradrenaline α2C)
Target: 5-HT Receptor; Dopamine Receptor
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.
in vivo: Lurasidone (30 mg/kg, p.o.) significantly and dose-dependently reverses the MK-801-induced impairment of the passive-avoidance response of rats. 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. 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.

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