[3H]UK14,034 is a full agonist at α2-adrenergic receptors. Although the characteristics of the binding of the partial α2-adrenergic agonists in postmortem human brain were known, the binding of [3H]UK14,304 had not been studied in this issue. Multi-site binding of this radiolabel had been reported in other tissues and guanosine triphosphate (GTP) had been shown to reduce [3H]UK14,304 binding. We now report that [3H]UK14,304 labels at least 2 specific binding sites in human brain that both have the characteristics of an α2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site.
ASJC Scopus subject areas
- Biochemistry, Genetics and Molecular Biology(all)
- Pharmacology, Toxicology and Pharmaceutics(all)