[EN] ANALOGS OF DEXTROMETHORPHAN WITH BALANCED RECEPTOR ACTIVITIES<br/>[FR] ANALOGUES DE DEXTROMÉTHORPHANE PRÉSENTANT DES ACTIVITÉS DE RÉCEPTEUR ÉQUILIBRÉES
申请人:THE CENTER FOR NEUROLOGIC STUDY
公开号:WO2022047345A1
公开(公告)日:2022-03-03
Substituted analogs of dextromethorphan (DM) are disclosed, which are shown to have substantial binding affinity at both NMDA and sigma-1 receptors, and which are degraded by human liver enzymes more slowly than dextromethorphan. The analogs are useful as alternatives to dextromethorphan, and can provide the same benefits without requiring co-administration of a cytochrome P-450 enzyme inhibitor.
本发明涉及右旋甲氧麻黄碱(DM)的替代类似物,这些类似物显示出在NMDA和sigma-1受体上具有显著的结合亲和力,并且它们被人类肝酶降解比右旋甲氧麻黄碱更慢。这些类似物可用作右旋甲氧麻黄碱的替代品,并且可以提供相同的益处,而无需共同使用细胞色素P-450酶抑制剂。