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CAS No. : 1052147-86-0
MCE 国际站:LP-211
产品活性: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 0.58 nM,选择性高于 5-HT1A 受体 (Ki,188 nM) 和 D2 受体 (Ki,142 nM)。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor
In Vitro: 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.
In Vivo: 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. 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.
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