In vivo binding of (/sup 3/H)Ro 15-1788 in mice: comparison with the in vivo binding of (/sup 3/H)flunitrazepam

Journal Article · Fri Jan 01 04:00:00 EST 1988 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(88)90583-8· OSTI ID:6703136

Potier, M C; de Carvalho, L P; Dodd, R H; Brown, C L; Rossier, J

Benzodiazepine binding sites have generally been labelled with benzodiazepine agonists: (/sup 3/H)flunitrazepam and (/sup 3/H)diazepam in vivo. The authors studied the in vivo binding of the antagonist (/sup 3/H)Ro 15-1788 in mice and compared it to the in vivo binding of (/sup 3/H)flunitrazepam. For this in vivo labelling, mice were injected with labelled and unlabelled ligands. Animals were then sacrificed and bound radioactivity was measured after homogenization of the excised brain and filtration of the homogenate. (/sup 3/H)Ro 15-1788 is a better tool than (/sup 3/H)flunitrazepam for in vivo labelling of benzodiazepine receptors since 1) it labels specifically the central type binding sites, 2) injection of 4 times less (/sup 3/H)Ro 15-1788 than (/sup 3/H)flunitrazepam produced the same amount of bound radioactivity, 3) 70-90% of the total (/sup 3/H)Ro 15-1788 present in the brain is membrane bound instead of 45-55% with (/sup 3/H)flunitrazepam, 4) maximal binding of (/sup 3/H)Ro 15-1788 is reached within 3 min, 5) only 5% of the membrane bound (/sup 3/H)Ro 15-1788 is nonspecific instead of 15% for (/sup 3/H)flunitrazepam.

• Research Organization: C.N.R.S. Gif-sur-Yvette (France)
• OSTI ID: 6703136
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 43:16; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CELL CONSTITUENTS
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
COMPARATIVE EVALUATIONS
DRUGS
IN VIVO
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
MICE
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
PROTEINS
PSYCHOTROPIC DRUGS
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
TRANQUILIZERS
TRITIUM COMPOUNDS
VERTEBRATES