Sadowski S, Huang R R, Fong T M, Marko O, Cascieri M A
Department of Molecular Pharmacology and Biochemistry, Merck Research Laboratories, Rahway, NJ 07065.
Neuropeptides. 1993 Jun;24(6):317-9. doi: 10.1016/0143-4179(93)90001-q.
We have characterized the binding of [125I-iodo-histidyl, methyl Phe7]neurokinin B (125I-NKB) to the human neurokinin-3 (NK3) receptor. 125I-NKB specifically binds to the NK3 receptor expressed in CHO cells with a Kd of 0.2 nM. The ligand displays little crossreactivity with the human NK1 and NK2 receptors. The binding of 125I-NKB to the human NK3 receptor and to rat cortex membranes is inhibited by neurokinin B with IC50 of 1.5 nM and 4 nM, respectively. In contrast, 350- to 500-fold higher concentrations of substance P and neurokinin A are required to inhibit binding to either receptor preparation. The data suggest that 125I-NKB is a high affinity, selective ligand for the human and rat NK3 receptor.
我们已经对[125I-碘组氨酰，甲基苯丙氨酸7]神经激肽B（125I-NKB）与人神经激肽-3（NK3）受体的结合进行了表征。125I-NKB以0.2 nM的解离常数（Kd）特异性结合于CHO细胞中表达的NK3受体。该配体与人NK1和NK2受体几乎没有交叉反应性。神经激肽B可抑制125I-NKB与人NK3受体及大鼠皮层膜的结合，其半数抑制浓度（IC50）分别为1.5 nM和4 nM。相比之下，需要高350至500倍浓度的P物质和神经激肽A才能抑制与这两种受体制剂的结合。这些数据表明，125I-NKB是人和大鼠NK3受体的高亲和力、选择性配体。
