Change in the properties of the opiate receptors of the brain under conditions of habituation of rats to morphine

Journal Article · Fri Feb 20 04:00:00 EST 1987 · Biochemistry (Engl. Transl.); (United States)

OSTI ID:5878904

Zaitsev, S V; Sergeeva, M G; Chichenkov, O N; Petrov, V E; Varfolomeev, S D

The influence of prolonged administration of morphine on the properties of the opiate receptors of the rat brain was investigated. For this purpose they conducted an analysis of the isotherms of binding of labeled ..mu..-, sigma-, and chi-ligands: morphine, D-Ala/sup 2/, D-Leu/sup 5/-enkephalin, and ethylketocyclazocin, with membrane preparations of the brains of rats tolerant to morphine, as well as the control animals. For a quantitative determination of the dissociation constants of the ligand-receptor complexes (K) and the concentration of the reagents ((Q)), they used differential method and the method of simulation modeling. It was shown that the values of K and (Q) for individual animals are subjected to substantial dispersion, whereas the ratios (Q)/K undergo minor individual fluctuations, both in the control group and in the group of rats tolerant to morphine. This permits the ratio (Q)/K to be singled out as one of the main parameters for comparing the properties of opiate receptors of various groups of animals. Using this criterion, as well as the method of simulated modeling, it was shown that the development of tolerance is accompanied by a change in the properties of the delta-receptors (the ratio (Q)/K decreases by a factor of more than two). In contrast to the delta-receptors, no significant influence of the tolerance on the properties of the ..mu..- and chi-receptors, as well as the ultrahigh-affinity ligand binding sites, was detected.

• Research Organization: M.V. Lomonosov Moscow State Univ., USSR
• OSTI ID: 5878904
• Journal Information: Biochemistry (Engl. Transl.); (United States), Journal Name: Biochemistry (Engl. Transl.); (United States) Vol. 51:8; ISSN BIORA
• Country of Publication: United States
• Language: English

Related Subjects

550101 -- Behavioral Biology-- Tracer Techniques
550201 -- Biochemistry-- Tracer Techniques
550301* -- Cytology-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ALKALOIDS
ANALGESICS
ANIMAL CELLS
ANIMALS
BINDING ENERGY
BIOCHEMISTRY
BIOLOGICAL EFFECTS
BODY
BRAIN
CELL CONSTITUENTS
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM DEPRESSANTS
CHEMISTRY
CHRONIC INTAKE
COMPLEXES
COMPUTERIZED SIMULATION
DISSOCIATION
DOSE-RESPONSE RELATIONSHIPS
DRUGS
ENERGY
INTAKE
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LABELLING
LIGANDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
MORPHINE
NARCOTICS
NERVE CELLS
NERVOUS SYSTEM
OPIUM
ORGANIC COMPOUNDS
ORGANS
PROTEINS
RADIORECEPTOR ASSAY
RATS
RECEPTORS
RODENTS
SIMULATION
SOMATIC CELLS
TOLERANCE
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES