Partial chemical characterization of cyclopyrrolones ((/sup 3/H) suriclone) and benzodiazepines ((/sup 3/H)flunitrazepam) binding site: Differences

Journal Article · Mon Jun 10 00:00:00 EDT 1985 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(85)90336-4· OSTI ID:5613179

Zundel, J L; Blanchard, J C; Julou, L

Rat hippocampus membranes were treated with several protein modifying reagents (iodoacetamide, N-ethylmaleimide, tetranitromethane and N-acetylimidazole). The effects of these treatments on the binding sites of cyclopyrrolones ((/sup 3/H) suriclone), a new chemical family of minor tranquilizers, and benzodiazepines ((/sup 3/H) flunitrazepam) were investigated. Here the authors show that both ligands are similarly sensitive to cysteine alkylation: (/sup 3/H) suriclone and (/sup 3/H) flunitrazepam binding are reduced by iodoacetamide and slightly increased by N-ethylmaleimide. On the contrary they are clearly differentiated by tyrosine modification: (/sup 3/H) suriclone binding is not changed whereas (/sup 3/H) flunitrazepam binding is increased by tetranitromethane and decreased by N-acetylimidazole. The present findings and published evidence suggest cyclopyrrolones and benzodiazepines bind to distinct sites or to different allosteric forms of the benzodiazepine receptor. 28 references, 6 figures.

• Research Organization: Rhone-Poulenc Sante, Vitry sur Seine Cedex, France
• OSTI ID: 5613179
• Journal Information: Life Sci.; (United States), Vol. 36:23
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
TRANQUILIZERS
CHEMICAL BONDS
RECEPTORS
BIOCHEMISTRY
CELL MEMBRANES
CHEMICAL COMPOSITION
HIPPOCAMPUS
LIGANDS
PROTEINS
RATS
REAGENTS
RESPONSE MODIFYING FACTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
BODY
BRAIN
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CHEMISTRY
DRUGS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANES
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
PSYCHOTROPIC DRUGS
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques