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SKF 97541 is a highly potent small molecule agonist of the GABA-B receptor (gamma-aminobutyric acid type B receptor) with an EC50 of approximately 50 nM for receptor activation[1][3][5][10]. It is at least ten times more active than baclofen as a GABA-B agonist[4][10]. SKF 97541 is also an antagonist at the GABA-A-rho (also referred to as GABAA-ρ) receptor[1][4][9]. The compound is blood-brain barrier permeable and depresses striatal synaptic potentials and hyperpolarizes nigral and septal neurons[1][3][5][7]. In animal models, it shows antidepressant and sedative effects and has been used in research trials investigating neurological and psychiatric indications such as depression and drug addiction[1][3][5][7][9][10]. SKF 97541 is a synthetic organic molecule developed for research use[8].
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