Presence of peripheral-type benzodiazepine binding sites on human erythrocyte membranes.
A nanomolar affinity peripheral-type benzodiazepine binding site is described in human erythrocyte membranes. [3H]PK 11195 is displaced from this binding site by unlabeled drugs with the rank order PK 11195 greater than Ro 5-4864 greater than flunitrazepam much greater than clonazepam. Neither GABA nor a non-hydrolyzable analog of GTP have an effect on binding parameters. These data provide evidence that a peripheral-type benzodiazepine binding site, pharmacologically similar to the intracellular binding site described in other tissues, is present in the plasma membrane of human erythrocytes.
Olson
J M
JM
Department of Pharmacology, University of Michigan, Ann Arbor 48104.
Ciliax
B J
BJ
Mancini
W R
WR
Young
A B
AB
D001570:Benzodiazepinones / Q000097:blood; D002998:Clonazepam / Q000097:blood; D003292:Convulsants / Q000097:blood; D004910:Erythrocyte Membrane / Q000201:enzymology / Q000378:metabolism*; D005445:Flunitrazepam / Q000097:blood; D006801:Humans; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000097:blood; D007700:Kinetics; D008995:Monoamine Oxidase / Q000097:blood; D011963:Receptors, GABA-A / Q000378:metabolism*
D001570:Benzodiazepinones; D003292:Convulsants; D007546:Isoquinolines; D011963:Receptors, GABA-A; C028513:4'-chlorodiazepam; D002998:Clonazepam; D005445:Flunitrazepam; D008995:Monoamine Oxidase; C037850:PK 11195