Mirogabalin besylate (DS 5565 besylate)

A calcium channel blocker

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库存: 现货

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促销价

数量
5mg

￥762.00

610.00

- +
10mg

￥1212.00

970.00

- +
50mg

￥3375.00

2700.00

- +
100mg

￥5400.00

4320.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

Mirogabalin is a calcium channel blocker with analgesic effects.¹ It binds to the α₂δ-1 and α₂δ-2 subunits of voltage-dependent Ca²⁺ channels. Mirogabalin has potent and sustained analgesic effects (ED₅₀ = 2.5 mg/kg) in rats with diabetes induced by streptozotocin . Mirogabalin does not inhibit activities associated with CNS adverse effects of analgesics, such as rotarod performance (ID₅₀ = 9.4 mg/kg) or locomotor activity (ID₅₀ = 43.9 mg/kg), at its effective dose.

1.Brown, K., Ohwada, S., Warren, V., et al.(405) A single ascending-dose study of mirogabalin in healthy subjects: Safety, tolerability, pharmacokinetic, and pharmacodynamic results.J. Pain17(4S)S76(2016)

Protocol

Animal experiment:

Rats[1]Eighty male rats are divided into groups of eight. After oral administration of Mirogabalin besylate (1, 3, 10, 30, and 100 mg/kg) or vehicle (control), locomotor activity is measured for 1 hour using the SUPERMEX system. Based on the time of peak effects of the test compounds (Mirogabalin besylate, etc.) in the rota-rod test, the pretreatment time is set at 6 hours for mirogabalin besylate and at 4 hours for pregabalin[1].

参考文献:

[1]. Domon Y, et al. Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the α2δ Subunit of Voltage-Gated Calcium Channels. J Pharmacol Exp Ther. 2018 Jun;365(3):573-582.