An atypical antipsychotic
Lurasidone is an atypical antipsychotic that binds to dopamine D2, serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT1A, and 5-HT7, and α2C-adrenergic receptors (Kis = 1.68, 2.03, 6.75, 0.495, and 10.8 nM, respectively).1 In vivo, pre-training administration of lurasidone (1 and 3 mg/kg) reverses impairment in step-through latency and passive avoidance in a foot shock test induced by MK-801 in rats. It reverses MK-801-induced learning impairment in the Morris water maze as well as reference and working memory impairment in the radial arm maze in rats.2 Lurasidone also decreases immobility in the tail suspension and forced swim tests, indicating antidepressant-like activity in mice.3 Formulations containing lurasidone have been used in the treatment of schizophrenia and mood disorders.
1.Ishiyama, T., Tokuda, K., Ishibashi, T., et al.Lurasidone (SM-13496), a novel atypical antipsychotic drug, reverses MK-801-induced impairment of learning and memory in the rat passive-avoidance testEur. J. Pharmacol.572(2-3)160-170(2007) 2.Enomoto, T., Ishibashi, T., Tokuda, K., et al.Lurasidone reverses MK-801-induced impairment of learning and memory in the Morris water maze and radial-arm maze tests in ratsBehav. Brain Res.186(2)197-207(2008) 3.Cates, L.N., Roberts, A.J., Huitron-Resendiz, S., et al.Effects of lurasidone in behavioral models of depression. Role of the 5-HT7 receptor subtypeNeuropharmacology70211-217(2013)
Animal experiment: | SD rats are individually isolated in clear plastic cages and injected with methamphetamine (MAP) (1 mg/kg i.p.) 1 h after the administration of drugs or vehicle. In the test of persistence of the effect, Lurasidone (SM-13496) is administered 1, 2, 4, and 8 h before the MAP injection. Locomotor activity is measured for 80 min from 10 min after MAP injection. Four or five groups of 6 to 13 rats are used to calculate the ED50 value that inhibits MAP-induced hyperactivity by 50% of the animals tested[1]. |
参考文献: [1]. Ishibashi T, et al. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81. | |
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