| 9007533 |
Cimino M, Marini P, Cattabeni F: Interaction of thiocolchicoside with [3H] strychnine binding sites in rat spinal cord and brainstem. J Urol. 2004 Mar;171(3):1353-6.
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 may provide a possible mechanism for the myorelaxant activity of this colchicoside derivative, the first clinically useful drug acting on this receptor. |
31(0,1,1,1) |