Lurasidone 是多巴胺 D2和5-HT7的拮抗剂，IC50值分别为 1.68 和 0.495 nM。它也是5-HT1A受体的部分激动剂，IC50值为 6.75 nM。

Lurasidone is an antagonist of both dopamine D2 and 5-HT7(IC50=1.68 and 0.495 nM, respectively).It also a partial agonist of 5-HT1A receptor(IC50 : 6.75 nM).

Lurasidone is administered once daily within the range of 40-160 mg/day for schizophrenia and 20-120 mg/day for bipolar depression, and its pharmacokinetic profile requires administration with food.?In adult healthy subjects and patients, a 40 mg dose results in peak plasma concentrations in 1-3 h, a mean elimination half-life of 18 h (mostly eliminated in the feces), and apparent volume of distribution of 6173 L;?it is approximately 99 % bound to serum plasma proteins.?Lurasidone's pharmacokinetics are approximately dose proportional in healthy adults and clinical populations within the approved dosing range, and this was also found in a clinical study of children and adolescents.?Lurasidone is principally metabolized by cytochrome P450 (CYP) 3A4 with minor metabolites and should not be coadministered with strong CYP3A4 inducers or inhibitors.?Lurasidone does not significantly inhibit or induce CYP450 hepatic enzymes[2].

In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as well as modest antagonism at noradrenergic α2A and α2C receptors.?Lurasidone is devoid of antihistaminic and anticholinergic activities[1].

367514-87-2

C28H36N4O2S

492.68

鲁拉西酮;SM-13496;Lurasidone

DMSO:17.83 mg/mL (36.19mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years