化学性质:
规格 | 10mM*1mLinDMSO 5mg 10mg 25mg |
CAS | 1052147-86-0 |
别名 | N/A |
化学名 | N/A |
分子式 | C30H34N4O |
分子量 | 466.62 |
溶解度 | DMSO : ≥ 106.6 mg/mL (228.45 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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).
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2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
标签:LP-211
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