Saclofen is a competitive antagonist of the GABAB receptor, exhibiting an IC50 value of 7.8 μM. It demonstrates weak antagonistic activity towards the GABAB1b and GABAB2 heterodimeric receptors. Saclofen effectively inhibits Baclofen binding to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts. Additionally, it has shown anti-inflammatory and analgesic effects in preclinical models. This makes Saclofen a valuable tool for investigating GABAB receptor functions and related biological processes.
Saclofen is a competitive antagonist of the GABAB receptor, exhibiting an IC50 value of 7.8 μM. It demonstrates weak antagonistic activity towards the GABAB1b and GABAB2 heterodimeric receptors. Saclofen effectively inhibits Baclofen binding to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts. Additionally, it has shown anti-inflammatory and analgesic effects in preclinical models. This makes Saclofen a valuable tool for investigating GABAB receptor functions and related biological processes.
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