Specific (/sup 3/H)UK 14,304 binding in human cortex occurs at multiple high affinity states with alpha/sub 2/-adrenergic selectivity and differing affinities for GTP

Journal Article · Fri Jan 01 04:00:00 EST 1988 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(88)90279-2· OSTI ID:6244734

Andorn, A C; Carlson, M A; Gilkeson, R C

(/sup 3/H)UK 14,034 is a full agonist at ..cap alpha../sub 2/-adrenergic receptors. Although the characteristics of the binding of the partial ..cap alpha../sub 2/-adrenergic agonists in postmortem human brain were known, the binding of (/sup 3/H)UK 14,304 had not been studied in this tissue. Multi-site binding of this radiolabel had been reported in other tissues and guanosine triphosphate (GTP) had been shown to reduce (/sup 3/H)UK 14,304 binding. The authors now report that (/sup 3/H)UK 14,304 labels at least 2 specific binding sites in human brain that both have the characteristics of an ..cap alpha../sub 2/-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site.

• Research Organization: Case Western Reserve Univ. School of Medicine, Cleveland, OH (USA)
• OSTI ID: 6244734
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 43:22; 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
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
DRUGS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MAN
MEMBRANE PROTEINS
NERVOUS SYSTEM
NUCLEOTIDES
ORGANIC COMPOUNDS
ORGANS
PRIMATES
PROTEINS
REACTION KINETICS
RECEPTORS
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES