[3H] diazepam binding to human granulocytes.
[3H]-diazepam binds to sites on human granulocyte membranes, with little or no binding to platelets or lymphocytes. These [3H]-diazepam binding sites are of the peripheral type, being strongly inhibited by R05-4864 (Ki = 6.23nM) but only weakly by clonazepam (Ki = 14 microM). Binding of [3H] diazepam at 0 degree is saturable, specific and stereoselective. Scatchard analysis indicates a single class of sites with Bmax of 109 +/- 17f moles per mg of protein and KD of 3.07 +/- 0.53nM. Hill plots of saturation experiments gave straight lines with a mean Hill coefficient of 1.03 +/- 0.014. Binding is time dependent and reversible and it varies linearly with granulocyte protein concentration over the range 0.025-0.300 mg of protein.
Bond
P A
PA
Cundall
R L
RL
Rolfe
B
B
D001569:Benzodiazepines / Q000494:pharmacology; D003975:Diazepam / Q000097:blood*; D006098:Granulocytes / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D011963:Receptors, GABA-A / Q000032:analysis*; D014316:Tritium
D011963:Receptors, GABA-A; D014316:Tritium; D001569:Benzodiazepines; D003975:Diazepam