Renzetti A R, Catalioto R M, Criscuoli M, Cucchi P, Lippi A, Guelfi M, Quartara L, Maggi C A
Department of Pharmacology, Menarini Ricerche S.p.A., Florence, Italy.
Biochem Biophys Res Commun. 1998 Jul 9;248(1):78-82. doi: 10.1006/bbrc.1998.8883.
[3H]MEN 11420, a radiolabeled glycosylated peptide antagonist of the tachykinin NK2 receptor, has been investigated in ligand-receptor binding assays using membranes of CHO cells transfected with the human tachykinin NK2 receptor. [3H]MEN 11420 bound to a single class of high affinity binding sites: its binding was inhibited by natural tachykinins (potency ranking: NKA >> SP > or = NKB), as well as by peptide (MEN 11420 > MEN 10376 >> R 396) and nonpeptide (SR 48968 > GR 159897) selective NK2 receptor antagonists. These data indicate that [3H]MEN 11420 is a potent radioligand for the human tachykinin NK2 receptor that may represent a useful tool for studying ligand-receptor interactions at the molecular level.
[3H]MEN 11420是速激肽NK2受体的一种放射性标记糖基化肽拮抗剂，已使用转染了人速激肽NK2受体的CHO细胞膜在配体-受体结合试验中进行了研究。[3H]MEN 11420与一类单一的高亲和力结合位点结合：其结合受到天然速激肽（效力排序：NKA >> SP >或= NKB）以及肽（MEN 11420 > MEN 10376 >> R 396）和非肽（SR 48968 > GR 159897）选择性NK2受体拮抗剂的抑制。这些数据表明，[3H]MEN 11420是一种用于人速激肽NK2受体的有效放射性配体，可能是在分子水平研究配体-受体相互作用的有用工具。
