V. Revilla et al., Effect of surgical stress on benzodiazepine receptors as a consequence of placebo pellet implantation in rat: An autoradiographic study, BRAIN RES B, 49(6), 1999, pp. 413-418
This paper reports modifications in benzodiazepine (BZ) receptors induced b
y minimally invasive surgery, such as pellet implantation, a widely used su
rgical process for chronic drug administration. The intrinsic stress induce
d by this manipulation on BZ receptors was analysed in an autoradiographic
saturation study determining the affinity (K-D) and total number (B-max) of
binding sites of a number of brain areas from the mesencephalon, cerebral
cortex, hippocampus, and cerebellum, The radioligand used for the study was
[H-3]flunitrazepam, which permitted overall characterization of BZ binding
sites. Use of the specific BZ1 agonist zolpidem as an inhibitor of this ra
dioligand permitted the direct characterization of subtype 2 (BZ2) and the
indirect characterization of subtype 1 receptor (BZ1). Significant increase
s in B-max and K-D values were observed in pellet-implanted animals with re
spect to those not implanted. The results support the notion of an upregula
tion of these receptors, mainly in BZ1 receptors, following sustained desen
sitization as a result of the surgical stress induced by pellet implantatio
n. (C) 1999 Elsevier Science Inc.