Saclofen

Saclofen is a competitive antagonist for the GABAB receptor. The GABAB receptor is a G-protein coupled receptor. The action of saclofen on the central nervous system is understandably modest, because G-proteins rely on an enzyme cascade to alter cell behavior while ionotropic receptors immediately change the composition of neuron interstitial fluid, thus changing its behavior. However, in animal experiments, saclofen is paradoxically observed to have an antiepileptic effect. This is unexpected as the GABA receptors are inhibitory, and antagonizing them should lead to hyperactivity of the effected neurons. Possible therapeutic uses are currently being researched.