Obligate pairing of orthosteric and non-orthosteric gaba ligands in pharmaceutical formulations

Abstract

A pharmaceutical composition is provided and includes at least one orthosteric GABA receptor ligand that directly binds to at least one GABA-A receptor or at least one GABA-B receptor at the endogenous GABA binding site, and at least one non-orthosteric GABA receptor ligand that binds a site distinct from the endogenous GABA binding site on at least one GABA receptor type. This ensures the orthosteric and non-orthosteric ligands for each receptor type are co-present. The orthosteric and non-orthosteric ligands may be co-formulated for concurrent availability, such that the presence of the orthosteric ligand enables or enhances the therapeutic effect of the non-orthosteric ligand.

Dependencies are inferred from the claim text.