Characterization of [3H]pentazocine binding sites in post-mortem human frontal cortex.
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 KD of 3.68 +/- 0.46nM and a B(max) 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 degrees C on [3H](+)-pentazocine binding sites. Of these variables, only age was significantly related to [3H](+)-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.
Kornhuber
J
J
Department of Psychiatry, University of Würzburg, Federal Republic of Germany.
Schoppmeyer
K
K
Bendig
C
C
Riederer
P
P
D000328:Adult; D000368:Aged; D000375:Aging / Q000378:metabolism; D001665:Binding Sites; D001667:Binding, Competitive / Q000187:drug effects; D005260:Female; D007839:Functional Laterality / Q000502:physiology; D006801:Humans; D066298:In Vitro Techniques; D007223:Infant; D007231:Infant, Newborn; D008297:Male; D008875:Middle Aged; D010423:Pentazocine / Q000378:metabolism* / Q000493:pharmacokinetics; D017397:Prefrontal Cortex / Q000378:metabolism*; D011957:Receptors, Opioid / Q000378:metabolism*; D012727:Sex Characteristics; D013237:Stereoisomerism
D011957:Receptors, Opioid; D010423:Pentazocine