Abstract
Prolonged administration of (±)-baclofen induces tolerance to its antinociceptive effect in mice. In the present study we compare the effects of 21 days administration of (−)-baclofen or GABA B (γ-aminobutyric acid B) receptor antagonist, with saline on the density of GABA B receptor binding sites in rat spinal cord using receptor autoradiography. Treatment with (−)-baclofen significantly reduced the number of silver grains (71%) whilst GABA B receptor antagonist, CGP 36742 (3-aminopropyl- n-butyl-phosphinic acid) and CGP 46381 (3-aminopropyl-cyclohexylmethylphosphinic acid), increased the grain count by 114% and 89%, respectively. These data indicate that GABA B receptors in the spinal cord can be influenced by prolonged administration of receptor ligands.
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