NS 8593 hydrochloride是选择性 KCa2 (SK) 通道的阴性调节剂(negative modulator), 抑制 SK 电流。
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Strøbaek et al (2006) Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons. Mol.Pharmacol. 70 1771. PMID: 16926279.
[2] Sørensen (2008) Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators of small conductance Ca2+-activated K+ channels. J.Med.Chem. 51 7625. PMID: 18998663.
[3] Jenkins et al (2011) Negative gating modulation by (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine (NS8593) depends on residues in the inner pore vestibule: pharmacological evidence of deep-pore gating of KCa2 channels. Mol.Pharmacol. 79 899. PMID: 21363929.
分子式 C17H17N3.HCl |
分子量 299.8 |
CAS号 875755-24-1 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water |
Ethanol 20 mM |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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