Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors ( GlyR ) ( IC 50 =565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABA A receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury.
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