LP-211 是一种选择性的，可透过血脑屏障的 5-HT₇ 受体激动剂，K_i 值为 0.58 nM，选择性高于 5-HT_1A 受体 (K_i，188 nM) 和 D₂ 受体 (K_i，142 nM)。

LP-211 is a selective and blood?brain barrier penetrant 5-HT 7 receptor agonist, with a K i of 0.58 nM, with high selectivity over 5-HT 1A receptor (K i , 188 nM) and D 2 receptor (K i , 142 nM).

Oil

5-HT7 Receptor 0.58 nM (Ki) 5-HT1A Receptor

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. has not independently confirmed the accuracy of these methods. They are for reference only.

LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean C max of 0.76 ± 0.32 μg/mL at 30 min. 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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Pure form -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (214.31 mM; Need ultrasonic)Ethanol : 50 mg/mL (107.15 mM; Need ultrasonic)配制储备液