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Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats.
Saclofen (300 μM, 0-24 h) inhibits the phase changes in the circadian rhythm caused by baclofen in brain slices of the rat suprachiasmatic nucleus (SCN) [1]. Saclofen (0.1 μM-1 mM, 10 s) suppresses the increase in CHO intracellular calcium induced by GABA at high concentrations[2]. Saclofen inhibits the binding of baclofen to rat cerebellar membranes with an IC50 of 7.8 μM[3].
Saclofen (5mg/mL, i.g., single dose) improves inflammation in rats induced by lipopolysaccharides[3]. Saclofen (1mg/mL, i.p., single dose) has analgesic effects in a rat pain model induced by acetic acid[4].