M. Malcangio et al., PLASTICITY OF GABA(B) RECEPTOR IN RAT SPINAL-CORD DETECTED BY AUTORADIOGRAPHY, European journal of pharmacology, 250(1), 1993, pp. 153-156
Prolonged administration of (+/-)-baclofen induces tolerance to its an
tinociceptive effect in mice. In the present study we compare the effe
cts of 21 days administration of (-)-baclofen or GABA(B) (gamma-aminob
utyric acid(B)) receptor antagonists, with saline on the density of GA
BA(B) receptor binding sites in rat spinal cord using receptor autorad
iograpy. Treatment with (-)-baclofen significantly reduced the number
of silver grains (71%) whilst GABA(B) receptor antagonists. CGP 36742
(3-aminopropyl-n-butyl-phosphinic acid) and CGP 46381 (3-aminopropyl-c
yclohexylmethylphosphinic 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.