Abstract
Radioreceptor binding assays and receptor autoradiography were used to investigate the activity of thiocolchicoside on strychnine-sensitive binding sites in rat brain and spinal cord using [ 3H]strychnine as a ligand. Thiocolchicoside displaced the binding of [ 3H]strychnine with an affinity similar to that of unlabeled glycine, and showed a Hill coefficient and proportionality parameter ( P) less than unity. The activity of thiocolchicoside toward [ 3H]strychnine binding sites was confirmed in autoradiographic studies. The results suggest that thiocolchicoside behaves as an allosteric compound acting on the strychnine-sensitive glycine receptor in rat brainstem and spinal cord, and that this interaction may provide a possible mechanism for the myorelaxant activity of this colchicoside derivative, the first clinically useful drug acting on this receptor.
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