Луразидон

Описание

The atypical antipsychotic lurasidone (also known as SM-13496) was approved in the United States in 2010 as an oral agent for the treatment of patients with schizophrenia. Lurasidone has potent affinity for D₂ (K_i= 1.7 nM) and 5-HT_2A (K_i= 2.0 nM) receptors and acts as an antagonist at both receptors. It is also a partial agonist at the 5-HT_1A receptor and, unlike other atypical agents, is a potent antagonist at the 5-HT₇ receptor; both of these activities are thought to confer beneficial cognitive properties. Lurasidone is further differentiated by its lack of affinity for muscarinic and histamine H₁ receptors and its weak affinity for the 5-HT_2C receptor. Antagonism at H₁ and 5-HT_2C receptors has been implicated in weight gain associated with atypical agents, while muscarinic receptor antagonism is associated with cognitive deficits.

Определение

ChEBI: An N-arylpiperazine that is (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-(piperazin-1-ylmethyl)cyclohexyl]methyl}hexahydro-1H-4,7-m thanoisoindole-1,3(2H)-dione in which position N4 of the piperazine ring is substituted by a 1,2-benzothiazol-3-yl group. Lurasidone is used (generally as the hydrochloride salt) as an atypical antipsychotic for the treatment of schizoph enia.