ISSN:
1435-1463
Keywords:
[3H](+)-Pentazocine
;
σ binding site
;
post-mortem time
;
gender
;
laterality
;
ontogenesis
;
aging
;
human brain
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary We investigated binding characteristics of [3H](+)-pentazocine in homogenates of post-mortem human frontal cortex. At equilibrium, specific binding was linear with protein concentration, was saturable, reversible, stereoselective, heat-labile and was nearly absent in the white matter. Saturation experiments revealed a K d of 3.68 ± 0.46nM and a Bmax of 0.636 ± 0.107 pmol/mg protein. The rank order of Ki values of competing substances was: haloperidol 〈 N,N′-di(o-tolyl)guanidine (DTG) 〈 (+)-SKF 10,047 〈 (—)-SKF 10,047. We also examined the influence of age, gender, hemisphere, post-mortem time and storage time of brain tissue at −80 °C on [3H](+)-pentazocine binding sites. Of these variables, only age was significantly related to [3]H](+)-pentazocine binding (diminished binding with increasing age). Together, our results demonstrate the presence of specific [3H](+)-pentazocine binding sites in post-mortem human brain tissue. Furthermore, the binding sites decrease with increasing age and are apparently independent of gender, hemisphere, post-mortem time and storage time of brain tissue.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01292615
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