Flupirtine
(Synonyms: 氟吡汀,D 9998) 目录号 : GC36060An activator of Kv7 channels
Cas No.:56995-20-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Flupirtine is an activator of voltage-gated potassium channel 7 (Kv7/KCNQ).1,2,3 It induces relaxation of preconstricted pulmonary arteries isolated from wild-type and serotonin transporter-overexpressing (SERT+) mice.2 Flupirtine (30 mg/kg per day) decreases mean right ventricular pressure and right ventricular hypertrophy in hypoxia-induced and SERT+ mouse models of pulmonary arterial hypertension. It increases the paw withdrawal threshold in a rat model of streptozotocin-induced diabetic neuropathy when administered at a dose of 10 mg/kg and increases paw withdrawal latency in a rat model of carrageenan-induced paw inflammation when used in combination with morphine.3 Flupirtine also indirectly antagonizes NMDA receptors via its effects on potassium channels.1,4
1.Devulder, J.Flupirtine in pain management: Pharmacological properties and clinical useCNS Drugs25(10)867-881(2010) 2.Morecroft, I., Murray, A., Nilsen, M., et al.Treatment with the Kv7 potassium channel activator flupirtine is beneficial in two independent mouse models of pulmonary hypertensionBr. J. Pharmacol.157(7)1241-1249(2009) 3.Goodchild, C.S., Kolosov, A., Tucker, A.P., et al.Combination therapy with flupirtine and opioid: Studies in rat pain modelsPain Med.9(7)928-938(2008) 4.Kornhuber, J., Bleich, S., Wiltfang, J., et al.Flupirtine shows functional NMDA receptor antagonism by enhancing Mg2+ block via activation of voltage independent potassium channelsJ. Neural Transm. (Vienna)106(9-10)857-867(1999)
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.286 mL | 16.4301 mL | 32.8601 mL |
5 mM | 0.6572 mL | 3.286 mL | 6.572 mL |
10 mM | 0.3286 mL | 1.643 mL | 3.286 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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