Changes in benzodiazepine receptor ligand affinity in the presence of 4,5,6,7-tetrahydroisoxazolo-(5,4-c-)-pyridin-3-ol (THIP)

Journal Article · Wed Jul 01 00:00:00 EDT 1987 · Bull. Exp. Biol. Med. (Engl. Transl.); (United States)

DOI:https://doi.org/10.1007/BF00840333· OSTI ID:5520372

Zharkovskii, A M; Shavrin, A S; Zharkovskaya, T A

The authors give data showing that benzodiazepine (BD) receptor ligands change their affinity in the presence of THIP, and that the shift of affinity induced by THIP can be used to predict the activity of these substances in vitro. Rats were used in the experiments and aliquots of the homogenate were incubated with /sup 3/H-flunitrazepam (/sup 3/H-FNZ). THIP inhibited binding of /sup 3/H-FNZ with intact membranes in proportion to its concentration. The inhibitory concentrations and inhibition constants of BD receptor ligands in the absence and presence of THIP are shown.

• Research Organization: Tartu Univ., USSR
• OSTI ID: 5520372
• Journal Information: Bull. Exp. Biol. Med. (Engl. Transl.); (United States), Vol. 103:2; Other Information: Translated from Byulleten' Ehksperimental'noj Biologii i Meditsiny; 103: No. 2, 181-183(Feb 1987)
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
DIAZO COMPOUNDS
BINDING ENERGY
RECEPTORS
NERVE CELLS
RADIORECEPTOR ASSAY
PYRIDINES
BIOLOGICAL EFFECTS
BRAIN
CELL CULTURES
CELL MEMBRANES
CYTOCHEMISTRY
DRUGS
INHIBITION
LABELLING
LIGANDS
OXAZOLES
RATS
SCINTILLATION COUNTING
STIMULATION
TRITIUM COMPOUNDS
ANIMAL CELLS
ANIMALS
AZINES
AZOLES
BIOCHEMISTRY
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
CHEMISTRY
COUNTING TECHNIQUES
ENERGY
HETEROCYCLIC COMPOUNDS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
ORGANS
PROTEINS
RODENTS
SOMATIC CELLS
TRACER TECHNIQUES
VERTEBRATES
550301* - Cytology- Tracer Techniques