Zhang, Guiping published the artcileDiscovery of N-substituted (2-phenylcyclopropyl)methylamines as functionally selective serotonin 2C receptor agonists for potential use as antipsychotic medications, Application In Synthesis of 71255-09-9, the main research area is phenylcyclopropylmethylamine preparation serotonin 2C receptor agonist antipsychotic.
A series of N-substituted (2-phenylcyclopropyl)methylamines were designed and synthesized, with the aim of finding serotonin 2C (5-HT2C)-selective agonists with a preference for Gq signaling. A number of these compounds exhibit 5-HT2C selectivity with a preference for Gq-mediated signaling compared with β-arrestin recruitment. Furthermore, the N-Me compound I•HCl, which displayed an EC50 of 23 nM in the calcium flux assay while showing no β-arrestin recruitment activity, is the most functionally selective 5-HT2C agonist reported to date. The N-benzyl compound II•HCl, which showed an EC50 of 24 nM at the 5-HT2C receptor, is fully selective over the 5-HT2B receptor. In an amphetamine-induced hyperactivity model, compound II showed significant antipsychotic-drug-like activity. These compounds shed light on the role of functional selectivity at the 5-HT2C receptor with respect to antipsychotic activity.
Journal of Medicinal Chemistry published new progress about 5-HT2C agonists. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application In Synthesis of 71255-09-9.