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A series of N-substituted (2-phenylcyclopropyl)methylamines were designed and synthesized, with the aim of finding serotonin 2C (5-HT 2C )-selective agonists with a preference for G q signaling. A number of these compounds exhibit 5-HT 2C selectivity with a preference for G q -mediated signaling compared with β-arrestin recruitment. Furthermore, the N-methyl compound (+)-15a, which displayed an EC 50 of 23 nM in the calcium flux assay while showing no β-arrestin recruitment activity, is the most functionally selective 5-HT 2C agonist reported to date. The N-benzyl compound (+)-19, which showed an EC 50 of 24 nM at the 5-HT 2C receptor, is fully selective over the 5-HT 2B receptor. In an amphetamine-induced hyperactivity model, compound (+)-19 showed significant antipsychotic-drug-like activity. These novel compounds shed light on the role of functional selectivity at the 5-HT 2C receptor with respect to antipsychotic activity.

journal of medicinal chemistry

Discovery of <i>N</i>-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications

Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications