2-Hydroxysaclofen is a GABA<sub>B</sub> receptor antagonist and an analogue of saclofen.
2-Hydroxysaclofen binds to the GABA<sub>B</sub> receptor, but this is selective for the (S)-enantiomer, while the (R)-enantiomer does not bind to the GABA<sub>B</sub> protein.
2-Hydroxysaclofen has been reported to be more potent than saclofen.