(S)-(-)-5-Iodowillardiine是高活性的无亚型的选择性 kainate 激动剂。
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] Patneau et al (1992) Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J.Neurosci. 12 595. PMID: 1371315.
[2] Wong et al (1994) Willardiines differentiate agonist binding sites for kainate-versus AMPA-preferring glutamate receptors in DRG and hippocampal neurones. J.Neurosci. 14 3881. PMID: 7515954.
[3] Thompson et al (1996) Depolarising effects of certain derivatives of (S) willardiine upon in vitro neonatal rat dorsal roots. Br.J.Pharmacol. 117 331P.
[4] Jane et al (1997) Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J.Med.Chem. 40 3645. PMID: 9357531.
[5] Swanson et al (1998) Kainate receptors exhibit differential sensitivities to (S)-5-iodowillardiine. Mol.Pharmacol. 53 942. PMID: 9584222.
分子式 C7H8IN3O4 |
分子量 325.06 |
CAS号 140187-25-3 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO |
Water |
Ethanol |
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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