For the present study, the changes induced on opioid peptide system in
the rat brain by a subconvulsant amount of metrazol (PTZ) (30 mg/lkg
i.p.) were investigated. Using a microdialysis procedure we found a si
gnificant opioid peptide release in hippocampus and amygdala, during t
he early 60 min, following administration. Thereafter, the values retu
rned to basal conditions. By autoradiagraphy experiments, we observed
a significant decrease of mu receptor binding in different brain areas
. Ligand binding analysis in membranes showed decreased number of rece
ptors without changes in their affinity. Randall-Sellito test indicate
d increased threshold to nociceptive stimulus, during the early 30 min
after PTZ administration. Finally, in situ hibridization procedure re
vealed increased levels of proenkephalin expression 24 h following PTZ
. Our results suggest that a subconvulsant amount of PTZ is able to ac
tivate opioid peptide system. These changes are relevant for the under
standing the epileptogenesis process and mechanisms associated.