Site-directed alkylation of multiple opioid receptors. I. Binding selectivity

Journal Article · Tue May 01 00:00:00 EDT 1984 · Mol. Pharmacol.; (United States)

OSTI ID:6350105

James, I F; Goldstein, A

A method for measuring and expressing the binding selectivity of ligands for mu, delta, and kappa opioid binding sites is reported. Radioligands are used that are partially selective for these sites in combination with membrane preparations enriched in each site. Enrichment was obtained by treatment of membranes with the alkylating agent beta-chlornaltrexamine in the presence of appropriate protecting ligands. After enrichment for mu receptors, (/sup 3/H) dihydromorphine bound to a single type of site as judged by the slope of competition binding curves. After enrichment for delta or kappa receptors, binding sites for (/sup 3/H) (D-Ala2, D-Leu5)enkephalin and (3H)ethylketocyclazocine, respectively, were still not homogeneous. There were residual mu sites in delta-enriched membranes but no evidence for residual mu or delta sites in kappa-enriched membranes were found. This method was used to identify ligands that are highly selective for each of the three types of sites.

• Research Organization: Addiction Research Foundation, Palo Alto, CA
• OSTI ID: 6350105
• Journal Information: Mol. Pharmacol.; (United States), Vol. 25:3
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
MORPHINE
RECEPTORS
OPIUM
ALKYLATION
TRITIUM COMPOUNDS
TRACER TECHNIQUES
ALKYLATING AGENTS
BRAIN
CELL MEMBRANES
CHEMICAL BONDS
ENKEPHALINS
GUINEA PIGS
LIGANDS
MOLECULAR BIOLOGY
ALKALOIDS
ANALGESICS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM DEPRESSANTS
CHEMICAL REACTIONS
DRUGS
ENDORPHINS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANES
NARCOTICS
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
POLYPEPTIDES
PROTEINS
RODENTS
VERTEBRATES
550301* - Cytology- Tracer Techniques