Mu/sub 1/: A very high affinity subtype of enkephalin binding sites in rat brain

Journal Article · Mon Jun 10 04:00:00 EDT 1985 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(85)90334-0· OSTI ID:5483996

Lutz, R A; Cruciani, R A; Munson, P J; Rodbard, D

Displacement studies of (/sup 3/H)-(D-Ala/sup 2/-MePhe/sup 4/-Gly-ol/sup 5/)-enkephalin ((/sup 3/H)-DAGO) and (/sup 3/H)-(D-Ala/sup 2/-D-Leu/sup 5/)-enkephalin ((/sup 3/H)-DADL) by the corresponding unlabeled ligands show that there are at least three classes of sites which bind these enkephalin analogs with high affinity. Using computer modeling, the introduction of the third site significantly improved the goodness of fit in ten consecutive experiments. These sites appear to correspond to the ..mu.., delta, and ..mu../sub 1/ sites, with mean dissociation constants of 11, 1.3 and 0.9 nM for DADL and 2.5, 300 and 0.3 nM for DAGO, respectively. 15 reference, 3 figures, 1 table.

• Research Organization: National Institutes of Health, Bethesda, MD
• OSTI ID: 5483996
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 36:23; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOCHEMISTRY
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CHEMICAL BONDS
CHEMISTRY
DRUGS
ENDORPHINS
ENKEPHALINS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MATHEMATICAL MODELS
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
POLYPEPTIDES
PROTEINS
RATS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES