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LP-211
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LP-211图片
CAS NO:1052147-86-0
规格:98%
分子量:466.62
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
LP-211是一种选择性的,可透过血脑屏障的5-HT7受体激动剂,Ki值为0.58nM,选择性高于5-HT1A受体(Ki,188nM)和D2受体(Ki,142nM)。
CAS:1052147-86-0
分子式:C30H34N4O
分子量:466.62
纯度:98%
存储:Store at -20°C

Background:

LP-211 is a selective and blood-brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).


LP-211 is a selective 5-HT7 receptor agonist, with a Ki of 0.58 nM, 324- and 245-fold selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM). LP-211 shows agonist properties with an EC50 of 0.6 μM[1].


LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean Cmax of 0.76 ± 0.32 μg/mL at 30 min[1]. LP-211 (0.003-0.3 mg/kg, i.p.) significantly increases the micturition volume in a dose-dependent manner, and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats, and such effects can be completely reversed by SB-269970[2]. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats, resulting in significant novelty-induced hyperactivity and recognition[3].


[1]. Leopoldo M, et al. Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. J Med Chem. 2008 Sep 25;51(18):5813-22. [2]. Norouzi-Javidan A, et al. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33. eCollection 2016. [3]. Beaudet G, et al. LP-211, a selective 5-HT7 receptor agonist, increases novelty-preference and promotes risk-prone behavior in rats. Synapse. 2017 Dec;71(12).