lurasidone

Details:

Lurasidone(SM-13496)isanantagonistofdopamineD2and5-HT7withIC50sof1.68±0.09and0.495±0.090nM,respectively.Lurasidone(SM-13496)isalsoapartialagonistof5-HT1AreceptorwithanIC50of6.75±0.97nM.InvitroreceptorbindingexperimentsrevealthatLurasidone(SM-13496)demonstratesaffinityfordopaChemicalbookmineD2and5-HT2Areceptorshigherthanothertestedantipsychotics.Lurasidone(SM-13496)doesnotincrease[35S]GTPγSbindingtothemembranepreparationsfordopamineD2receptorsbyitself,butitantagonizesdopamine-stimulated[35S]GTPγSbindinginaconcentration-dependentmannerwithaKBvalueof2.8±1.1nM.

Lurasidone is an atypical antipsychotic drug developed by Japan's DainipponSumitomo Pharmaceutical Company. It belongs to the 3.1 category of chemical drug registration and is suitable for the treatment of patients with schizophrenia. The efficacy was determined in four 6-week controlled studies in adult patients with schizophrenia. The exact mechanism of its treatment of schizophrenia is still unclear like other atypical antipsychotics, and may be related to the antagonism of dopamine D2 and serotonin 2A (5-HT2A) receptors. It is used in the treatment of schizophrenia, and studies have reported that lurasidone can improve cognitive function. On October 28, 2010, the United States FChemicalbookDA approved lurasidone hydrochloride (lurasidoneHCI) once a day tablets for the first-line treatment of patients with schizophrenia, and its trade name is Latuda. Usage and dosage: The recommended starting dose is 40mg·d, the effective dose range is 40～120mg·d, and the maximum recommended dose is 80mg·d. It should be taken with food. Adverse reactions: Common adverse reactions include drowsiness, akathisia, nausea, Parkinson's disease-like symptoms, and emotional anxiety. Lurasidone has no physical dependence, causes less weight gain, and does not cause changes in glucose, lipids (lipids), ECG and QT intervals.