New photoaffinity ligand candidates were synthesized based on 5-t-buty1-2-(4-(substituted-ethyny1)phenyl)-1, 3-dithiane for the noncompetitive blocker site on the gammaaminobutyric acid-gated chloride channel. Their half-maximal inhibition concentrations ranged from 4 to 32 nmol/L as measured by 4'-ethyny1-4-n-[2,3-3^H2]-propylbicycloorthobenzoate (3^H EBOB) assay.
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