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LP-211 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.58 nM).1 It is selective for 5-HT7 over 5-HT1A and dopamine D2 receptors (Kis = 188 and 142 nM, respectively). It induces relaxation of isolated guinea pig ileum precontracted by substance P (Item No. 24035; EC50 = 0.6 μM). LP-211 (100 nM) stimulates neurite outgrowth in primary murine striatal and cortical neurons.2
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1. Structural modifications of N-
2. Structural modifications of the serotonin 5-