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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 (Ki= 1.7 nM)
and 5-HT2A (Ki= 2.0 nM) receptors and acts as an antagonist at both
receptors. It is also a partial agonist at the 5-HT1A 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-HT2C
receptor. Antagonism at H1 and 5-HT2C receptors has been implicated in
weight gain associated with atypical agents, while muscarinic receptor
antagonism is associated with cognitive deficits.
Definition
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.
lurasidone Upstream-Materialien And Downstream Produkte