Wouters W, Van Dun J, Laduron P M
FEBS Lett. 1987 Mar 23;213(2):359-64. doi: 10.1016/0014-5793(87)81522-3.
7-Azido-8-[125I]ketanserin ([125I]AZIK) was characterized as a potent photoaffinity probe for serotonin-S2 receptors. In reversible binding experiments, [125I]AZIK bound with high affinity (Kd = 0.69 nM) to rat frontal cortex membranes. When incubation with [125I]AZIK was followed by UV irradiation, the binding was found to be irreversible. Protection experiments with various drugs demonstrated the serotonin-S2 nature of the photoaffinity labelling. SDS-polyacrylamide gel electrophoresis of the photolabelled membranes allowed one to identify the serotonin-S2 receptor ligand binding site as a single polypeptide with a molecular mass of approx. 67,500 Da. [125I]AZIK will be a valuable tool for the elucidation of the serotonin-S2 receptor structure.
7-叠氮基-8-[125I]酮色林（[125I]AZIK）被鉴定为一种有效的血清素-S2受体光亲和探针。在可逆结合实验中，[125I]AZIK以高亲和力（Kd = 0.69 nM）与大鼠额叶皮质膜结合。当用[125I]AZIK孵育后进行紫外线照射时，发现结合是不可逆的。用各种药物进行的保护实验证明了光亲和标记的血清素-S2性质。对光标记膜进行SDS-聚丙烯酰胺凝胶电泳，能够将血清素-S2受体配体结合位点鉴定为一条分子量约为67,500 Da的单一多肽。[125I]AZIK将成为阐明血清素-S2受体结构的有价值工具。
