[Presence of a peripheral type benzodiazepine binding site on the macrophage; its possible role in immunomodulation].
Saturable binding site for 3H-flunitrazepam (KD = 43 +/- 7 nM, Bmax = 391 +/- 58 fmoles/cell, i.e. 250,000 sites/cell) is characterized on Mouse peritoneal inflammatory macrophages. The affinity for different ligands (PK 11195 greater than Ro 5-4864 greater than diazepam greater than flunitrazepam greater than clonazepam greater than Ro 15-1788) shows that this site is of peripheral type. In vivo the humoral response in Mice to Sheep red blood cells was stimulated by administration of 1 mg/kg of PK 11195 (+85%), Ro 5-4864 (+80%) and diazepam (+58%). Clonazepam and Ro 15-1788 are devoid of activity. This suggests that molecules which show affinity for the "peripheral type" benzodiazepine binding site might modulate the immune response.
Lenfant
M
M
Zavala
F
F
Haumont
J
J
Potier
P
P
D000818:Animals; D000917:Antibody Formation / Q000187:drug effects*; D001569:Benzodiazepines / Q000378:metabolism / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000494:pharmacology; D002998:Clonazepam / Q000494:pharmacology; D004912:Erythrocytes / Q000276:immunology; D000431:Ethanol / Q000494:pharmacology; D005260:Female; D005445:Flunitrazepam / Q000494:pharmacology; D008264:Macrophages / Q000276:immunology* / Q000378:metabolism; D051379:Mice; D011963:Receptors, GABA-A / Q000032:analysis / Q000276:immunology*; D012756:Sheep / Q000276:immunology
D001570:Benzodiazepinones; D011963:Receptors, GABA-A; D001569:Benzodiazepines; C028513:4'-chlorodiazepam; D000431:Ethanol; D002998:Clonazepam; D005445:Flunitrazepam
Présence d'un site de fixation de "type périphérique" des benzodiazépines sur le macrophage; son rôle éventuel dans l'immunomodulation.