Characterization of solubilized human and rat brain US -endorphin-receptor complex

Journal Article · Tue Dec 31 23:00:00 EST 1985 · Proc. Natl. Acad. Sci. U.S.A.; (United States)

DOI:https://doi.org/10.1073/pnas.83.1.67· OSTI ID:6413820

Helmeste, D M; Li, C H

Opioid receptors have been solubilized from human striatal and rat whole-brain membranes by use of 3-((3-cholamidopropyl)dimethylammonio)-1-propanesulfonate (CHAPS). Tritiated human US -endorphin (TH-US /sub h/-EP) binding revealed high-affinity competition by morphine, naloxone, and various US -EP analogues. Lack of high-affinity competition by (+/-)-3,4-dichloro-N-methyl-N-(2-(1-pyrrolidinyl)cyclohexyl)benzeneacetamide methanesulfonate (U50-488, Upjohn) indicated that k sites were not labeled by TH-US -/sub h/-EP under these conditions. Affinities were similar in both soluble and membrane preparations except for (Met)enkephalin, which appears to be rapidly degraded by the solubilized extract. Size differences between human and rat solubilized TH-US /sub h/-EP-receptor complexes were revealed by exclusion chromatography.

• Research Organization: Univ. of California, San Francisco
• OSTI ID: 6413820
• Journal Information: Proc. Natl. Acad. Sci. U.S.A.; (United States), Journal Name: Proc. Natl. Acad. Sci. U.S.A.; (United States) Vol. 83:1; ISSN PNASA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
BRAIN
CELL CONSTITUENTS
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM
DRUGS
ENDORPHINS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MAN
MEMBRANES
MOLECULAR STRUCTURE
NERVOUS SYSTEM
NEUROREGULATORS
ORGANS
PRIMATES
RADIORECEPTOR ASSAY
RATS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES