Evaluation of the interactions of mu and delta selective ligands with (/sup 3/H)D-Ala/sup 2/-D-Leu/sup 5/-enkephalin binding to mouse brain membranes

Journal Article · Mon Dec 12 04:00:00 EST 1983 · Life Sci.; (United States)

OSTI ID:5024599

Barrett, R W; Vaught, J L

The interactions of putative mu and delta selective ligands with (/sup 3/H)D-ala/sup 2/-D-leu/sup 5/ enkephalin (DADLE) binding to mouse brain membranes were investigated. Computerized curve fitting of displacement curves performed at three different concentrations of /sup 3/H-DADLE indicated that at one site competitive model was sufficient to explain the interactions of leu-enkephalin (LE) and D-ser/sup 2/-thr/sup 6/-leucine enkephalin with /sup 3/H-DADLE binding. A two-site competitive model was required to adequately describe the interactions of these mu selective ligands with /sup 3/H-DADLE. This two-site model was one in which the inhibitor had higher affinity for the site labeled with lower affinity by /sup 3/H-DADLE. These data indicate that: putative mu and delta selective ligands do not bind to a common high affinity site; mu selective ligands are not simple mixed inhibitors of a single site labeled by /sup 3/H-DADLE; and competitive binding models may not explain the interaction of mu ligands with /sup 3/H-DADLE binding.

• Research Organization: Rutgers Univ., Piscataway, NJ
• OSTI ID: 5024599
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 33:24; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOCHEMISTRY
BIOLOGICAL MODELS
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CHEMICAL REACTIONS
CHEMISTRY
CONFIGURATION INTERACTION
DRUGS
ENDORPHINS
ENKEPHALINS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MICE
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
POLYPEPTIDES
PROTEINS
RODENTS
TRITIUM COMPOUNDS
VERTEBRATES