Phosphinic acid analogues of GABA. 1. New potent and selective GABA(B) agonists

Article abstract of DOI:10.1021/jm00017a015

The antispastic agent and muscle relaxant baclofen 1 is a potent and selective agonist for bicuculline-insensitive GABA(B) receptors. For many years efforts to obtain superior GABA(B) agonists were unsuccessful. We describe the syntheses and biological pr