(±)-U-50488 hydrochloride是标准选择性 κ 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] Pugsley et al (1992) Cardiovascular actions of the κ-agonist, U-50-488H, in the absence and presence of opioid receptor blockade. Br.J.Pharmacol. 105 521. PMID: 1320979.
[2] Suarez-Roca and Maixner (1993) Activation of kappa opioid receptors by U-50488H and morphine enhances the release of substance P from rat trigeminal nucleus slices. J.Pharmacol.Exp.Ther. 264 648. PMID: 7679733.
[3] Pao-Luh Tao et al (1994) U-50,488 blocks the development of morphine tolerance and dependence at a very low dose in guinea pigs. Eur.J.Pharmacol. 256 281. PMID: 8045272.
[4] Su et al (1998) Blockade of the development of morphine tolerance by U-50,488, an AVP antagonist or MK 801 in the rat hippocampal slice. Br.J.Pharmacol. 123 625. PMID: 9517380.
分子式 C19H26Cl2N2O.HCl |
分子量 405.79 |
CAS号 67197-96-0 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO |
Water 25 mM |
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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