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Description: LP-211 is a potent and selective 5-HT7 receptor agonist with a Ki of 0.58 nM at rat cloned 5-HT7 receptors. It has high selectivity over 5-HT1A receptor (Ki of 188 nM) and D2 receptor (Ki=142 nM)((324- and 245-fold, respectively)). LP-211 is able to cross blood?brain barrier and has agonist properties (maximal effect = 82%, EC 50 = 0.60 microM). After intraperitoneal injection in mice, LP-211 rapidly reached the systemic circulation and entered the brain. Its brain concentration-time profile paralleled that in plasma, indicating that LP-211 rapidly and freely distributes across the blood-brain barrier. LP-211 is metabolized via N-dealkylation to the corresponding 1-arylpiperazine metabolite.
References: J Med Chem. 2008 Sep 25; 51(18):5813-22; Am J Transl Res. 2016 Jun 15; 8(6):2525-33; Synapse. 2017 Dec; 71(12). doi: 10.1002/syn.21995.
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