SGE-516

SGE-516 is a synthetic neuroactive steroid and a potent positive allosteric modulator (PAM) of both synaptic (gamma-subunit-containing) and extrasynaptic (delta-subunit-containing) GABAA receptors. Developed by Sage Therapeutics (which was acquired by Supernus in July 2025), SGE-516 is a 1,2,5-triazole analog of allopregnanolone designed with improved oral bioavailability and pharmacokinetic properties compared to endogenous neurosteroids. It has been widely utilized as a preclinical tool compound to investigate the therapeutic potential of GABAergic modulation in various central nervous system (CNS) disorders. Preclinical studies have demonstrated its efficacy in animal models of postpartum depression (PPD), Dravet syndrome, status epilepticus (including organophosphorus nerve agent-induced status epilepticus), essential tremor, and anxiety.

Other names

3alpha-hydroxy-3beta-methyl-21-(1',2',3'-triazol-2'-yl)-19-nor-5beta-pregnan-20-one3α-Hydroxy-3β-methyl-21-(1′,2′,3′-triazol-2′-yl)-19-nor-5β-pregnan-20-one