LP-211

LP-211 is a selective and blood brain barrier penetrant 5-HT₇ receptor agonist, with a K_i of 0.58 nM, with high selectivity over 5-HT_1A receptor (K_i, 188 nM) and D₂ receptor (K_i, 142 nM). IC50 & Target:Ki: 0.58 nM (5-HT₇ receptor), 188 nM (5-HT_1A receptor), 142 nM (D₂ receptor)^[1] In Vitro:LP-211 is a selective 5-HT₇ receptor agonist, with a K_i of 0.58 nM, 324- and 245-fold selectivity over 5-HT_1A receptor (K_i, 188 nM) and D₂ receptor (K_i, 142 nM). LP-211 shows agonist properties with an EC₅₀ of 0.6 μM^[1]. In Vivo: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^[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 (0.25-0.50 mg/kg, i.p.) improves consolidation of chamber-shape memory in rats, resulting in significant novelty-induced hyperactivity and recognition^[3].