[125I]SCH 23982: the ligand of choice for identifying the D-1 dopamine receptor.
[125I]SCH 23982: the ligand of choice for identifying the D-1 dopamine receptor.
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[125I]SCH 23982：用于鉴定 D-1 多巴胺受体的选择配体。
DOI：
10.1016/0014-2999(86)90768-5
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发表时间：
1986
影响因子：
5
通讯作者：
J. Kebabian
中科院分区：
文献类型：
--
作者：
A. Sidhu;J. V. van Oene;P. Dandridge;C. Kaiser;J. Kebabian
[125 I]SCH 23982，[125 I]8-碘-2，3，4，5-四氢-3-甲基-5-苯基-1H-3-苯并氮杂卓-7-醇，以高亲和力（Kd= 0.7 ± 0.05 nM）可逆结合大鼠脑尾状核中的特异性结合位点（最大结合= 108 ± 3.5 fmol/mg）。尾状核结合位点显示出与D-1受体相似的药理学性质;此外，该位点对有利于D-2受体的药物具有低亲和力。GTP降低多巴胺（一种D-1激动剂）对尾状核结合位点的亲和力，但不降低SCH 23390（一种D-1拮抗剂）对尾状核结合位点的亲和力。碘化配体区分D-1和D-2多巴胺受体：大鼠脑垂体的神经中间叶，富含D-2多巴胺受体的组织，在尾状核中具有少于4%的特异性结合位点。由于[125 I]SCH 23982的比活度高于[3 H]SCH 23390（之前用于鉴别D-1受体的配体），并且由于碘化配体所得结果与[3 H]SCH 23390所得结果相似，因此[125 I]SCH 23982是鉴别D-1受体的首选配体。
[125I]SCH 23982, [125I]8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol, binds reversibly and with high affinity (Kd= 0.7 ± 0.05 nM) to specific binding sites (maximum binding = 108 ± 3.5 fmol/mg) in the caudate nucleus of the rat brain. The caudate binding site displays pharmacological properties similar to the D-1 receptor; furthermore, the site has a low affinity for drugs favoring the D-2 receptor. GTP diminishes the affinity of dopamine, a D-1 agonist, but not SCH 23390, a D-1 antagonist, for the caudate binding site. The iodinated ligand discriminates between the D-1 and the D-2 dopamine receptors: the neurointermediate lobe of the rat pituitary gland, a tissue rich in D-2 dopamine receptors, possesses less than 4% of the specific binding sites in the caudate. Because [125I]SCH 23982 exists at a higher specific activity than [3H]SCH 23390, a ligand used previously to identify the D-1 receptor, and because the results obtained with the iodinated ligand are otherwise similar to those obtained with the [3H]SCH 23390, [125I]SCH 23982 is the ligand of choice for identifying the D-1 receptor.
通过选择性 DA1 拮抗剂 SCH 23390 分离外周多巴胺受体。
DOI：
10.1161/01.hyp.6.2_pt_2.i25
发表时间：
1984
期刊：
Hypertension (Dallas, Tex. : 1979)
影响因子：
--
作者：
Goldberg,LI;Glock,D;Kohli,JD;Barnett,A
通讯作者：
Barnett,A