Characterization of solubilized "peripheral type" benzodiazepine binding sites from rat adrenals by using [3H]PK 11195, an isoquinoline carboxamide derivative.
"Peripheral type" benzodiazepine binding sites have been solubilized with digitonin. Binding site density for the solubilized material is increased 1.7 times compared to membranes. A decrease in the affinity for [3H]-PK 11195 (a new ligand for the peripheral type benzodiazepine binding sites) was also observed. Pharmacological specificity of displacing agents was conserved during solubilization. The apparent molecular weight determined by gel filtration was 215,000 +/- 20,000. The high Bmax value of the solubilized preparation (greater than 50 pmole/mg protein) makes it advantageous as the starting point for a purification procedure.
Benavides
J
J
Menager
J
J
Burgevin
M C
MC
Ferris
O
O
Uzan
A
A
Gueremy
C
C
Renault
C
C
Le Fur
G
G
D000311:Adrenal Glands / Q000032:analysis*; D000818:Animals; D007546:Isoquinolines / Q000378:metabolism*; D008297:Male; D008970:Molecular Weight; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000032:analysis / Q000302:isolation & purification*; D012995:Solubility; D014316:Tritium
D007546:Isoquinolines; D011963:Receptors, GABA-A; D014316:Tritium; C037850:PK 11195