Specific [3H]UK 14,304 binding in human cortex occurs at multiple high affinity states with alpha 2-adrenergic selectivity and differing affinities for GTP.

[3H]UK 14,034 is a full agonist at alpha 2-adrenergic receptors. Although the characteristics of the binding of the partial alpha 2-adrenergic agonists in postmortem human brain were known, the binding of [3H]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 [3H]UK 14,304 binding. We now report that [3H]UK 14,304 labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site.