Saclofen is an orally active and a competitive GABA B receptor antagonist with an IC 50 of 7.8 μM. Saclofen has weak antagonistic effects on GABA B1b and GABA B2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen ( HY-B0007 ) to rat cerebellar membranes and blocks Baclofen -induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats.
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