Prucalopride succinate是5-HT4受体选择高亲和性激动剂,对5-HT4a和5-HT4b的pKi值分别为8.6和8.1。
Prucalopride is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively.
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] Briejer MR, et al. Eur J Pharmacol, 2001, 423(1), 71-83.
[2] Johnson DE, et al. The 5-hydroxytryptamine4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations. J Pharmacol Exp Ther. 2012 Jun;341(3):681-91.
分子式 C22H32ClN3O7 |
分子量 485.96 |
CAS号 179474-85-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mg/mL |
Water 100 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01807000 | Healthy | Drug: Radiolabeled Prucalopride Succinate | Shire | Phase 1 | 2013-03-01 | 2014-08-22 |
NCT02047045 | Constipation | Procedure: acupuncture|Drug: Prucalopride | Guang'anmen Hospital of China Academy of Chinese Medical Sciences|Ministry of Science and Technology of the People麓s Republic of China | 2014-04-01 | 2016-10-05 | |
NCT01870674 | Healthy | Drug: YH12852|Drug: Prucalopride|Drug: Placebo | Yuhan Corporation | Phase 1 | 2013-08-01 | 2015-05-07 |
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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