Lurasidone (SM-13496)

An atypical antipsychotic

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库存: 现货

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10mg

￥437.00

350.00

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50mg

￥1212.00

970.00

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100mg

￥1962.00

1570.00

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货号: ajce46094
CAS: 367514-87-2
别名: 鲁拉西酮; SM-13496
分子式: C28H36N4O2S
分子量: 492.68
纯度: >98%
溶解度: DMSO : 20.83 mg/mL (42.28 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Lurasidone is an atypical antipsychotic that binds to dopamine D₂, serotonin (5-HT) receptor subtypes 5-HT_2A, 5-HT_1A, and 5-HT₇, and α_2C-adrenergic receptors (K_is = 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)

Protocol

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.
[2]. Sakine Atila Karaca, et al. Development of a validated high-performance liquid chromatographic method for the determination of Lurasidone in pharmaceuticals. Marmara Pharm J. 2017;21 (4): 931-937.