Specific [3H]UK14,304 binding in human cortex occurs at multiple high affinity states with alpha2-adrenergic selectivity and differing affinities for GTP

Anne C. Andorn, Mark A. Carlson, R. Chapman Gilkeson

Research output: Contribution to journalArticle

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Abstract

[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.

Original languageEnglish (US)
Pages (from-to)1805-1812
Number of pages8
JournalLife Sciences
Volume43
Issue number22
DOIs
StatePublished - 1988

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Guanosine Triphosphate
Adrenergic Agents
Binding Sites
Brain
Adrenergic Agonists
Adrenergic Receptors
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Tissue

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Specific [3H]UK14,304 binding in human cortex occurs at multiple high affinity states with alpha2-adrenergic selectivity and differing affinities for GTP. / Andorn, Anne C.; Carlson, Mark A.; Chapman Gilkeson, R.

In: Life Sciences, Vol. 43, No. 22, 1988, p. 1805-1812.

Research output: Contribution to journalArticle

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T1 - Specific [3H]UK14,304 binding in human cortex occurs at multiple high affinity states with alpha2-adrenergic selectivity and differing affinities for GTP

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AU - Chapman Gilkeson, R.

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AB - [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.

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