Interaction of (D-Ser/sup 2/,Leu/sup 5/)enkephalin-Thr/sup 6/ (DSLET), a relatively selective delta ligand, with mu/sub 1/ opioid binding sites

Journal Article · Mon Jan 19 04:00:00 EST 1987 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(87)90348-1· OSTI ID:7093782

Itzhak, Y; Pasternak, G W

Using binding approaches, the high selectivity of (D-Ser/sup 2/,Leu/sup 5/)enkephalin-Thr/sup 6/ (DSLET) to delta, as opposed to morphine-preferring (mu/sub 2/) sites in rat brain has been confirmed. However, detailed experiments studies indicate that this ligand also labels mu/sub 1/ sites with very high affinity. Saturation studies of /sup 3/H-DSLET binding reveal curvilinear plots. Treating tissue with naloxonazine to block mu/sub 1/ sites, eliminates the higher affinity binding component. Competition studies of the other peptides against /sup 3/H-DSLET and /sup 3/H(D-Ala/sup 2/, MePhe/sup 4/, Gly(o1)/sup 5/)enkephalin (/sup 3/H-DAMPGO) binding also implied high affinity binding of these peptides to mu/sub 1/ sites. The ability of these peptides to interact with mu/sub 1/ sites may help explain some of their pharmacological actions.

• Research Organization: memorial Sloan-Kettering Cancer Center, New York, NY
• OSTI ID: 7093782
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 40:3; ISSN LIFSA
• Country of Publication: United States
• Language: English

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550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOCHEMICAL REACTION KINETICS
DRUGS
ENDORPHINS
ENKEPHALINS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MEMBRANE PROTEINS
NEUROREGULATORS
ORGANIC COMPOUNDS
PEPTIDES
PHARMACOLOGY
POLYPEPTIDES
PROTEINS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS