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.
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.
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人类皮质中的 [3H]UK 14,304 特异性结合发生在多种高亲和力状态下，具有 α2-肾上腺素能选择性和对 GTP 的不同亲和力。
DOI：
10.1016/0024-3205(88)90279-2
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发表时间：
1988
期刊：
影响因子：
6.1
通讯作者：
Gilkeson,RC
中科院分区：
文献类型：
--
作者：
Andorn,AC;Carlson,MA;Gilkeson,RC
[3 H] UK 14，034是α2-肾上腺素能受体的完全激动剂。虽然部分α2-肾上腺素能激动剂在死后人脑中的结合特征是已知的，但[3 H] UK 14，304的结合在本问题中尚未研究。在其他组织中报告了该放射性标记的多位点结合，并且已显示三磷酸鸟苷（GTP）可降低[3 H] UK 14，304结合。[~ 3 H] UK 14，304标记了人脑中至少2个特异性结合位点，它们都具有α2肾上腺素能结合位点的特征。GTP降低这两个位点的激动剂结合，但在每个位点具有不同的效力。
[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.