[3H]去甘氨酰胺（9）-d（CH2）5[D-异亮氨酸2，异亮氨酸4]精氨酸加压素：一种精氨酸加压素V2受体拮抗剂放射性配体。

[3H]desGly-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP: an AVP V2 receptor antagonist radioligand.

作者信息

Trinder D, Stephenson J M, Gao X, Phillips P A, Risvanis J, Johnston C I

机构信息

University of Melbourne, Department of Medicine, Austin Hospital, Heidelberg, Victoria, Australia.

出版信息

Peptides. 1991 Nov-Dec;12(6):1195-200. doi: 10.1016/0196-9781(91)90194-t.

DOI:10.1016/0196-9781(91)90194-t

PMID:1815207

Abstract

Binding characteristics of the selective V2 antagonist radioligand [3H]desGly-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP to rat kidney were determined. Binding was specific, saturable and reversible. The peptide bound to a single class of high-affinity binding sites with Bmax 69.4 +/- 6.8 fmol/mg protein and KD 2.8 +/- 0.3 nM. AVP and other related peptides displaced [3H]desGly-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP binding. The order of potency of inhibition was desamino-D-AVP greater than AVP greater than d(CH2)5[D-Ileu2,Ileu4]AVP greater than oxytocin greater than d(CH2)5[Tyr(Me)2]AVP greater than d(CH2)5[sarcosine7]AVP, which is typical of a selective V2 radioligand. Autoradiographic localization of [3H]desGly-NH2(9)-d(CH2)5[D-Ileu2,Ileu4]AVP binding sites in kidney showed dense binding in the inner and outer medulla with less binding in the cortex, which is consistent with known renal V2 receptor distribution.

摘要

测定了选择性V2拮抗剂放射性配体[3H]去甘氨酰胺（9）-d（CH2）5[D-异亮氨酸2，异亮氨酸4]抗利尿激素（AVP）与大鼠肾脏的结合特性。结合是特异性的、可饱和的且可逆的。该肽与一类单一的高亲和力结合位点结合，Bmax为69.4±6.8 fmol/mg蛋白质，KD为2.8±0.3 nM。AVP和其他相关肽可取代[3H]去甘氨酰胺（9）-d（CH2）5[D-异亮氨酸2，异亮氨酸4]AVP的结合。抑制效力顺序为去氨基-D-AVP＞AVP＞d（CH2）5[D-异亮氨酸2，异亮氨酸4]AVP＞催产素＞d（CH2）5[酪氨酸（甲基）2]AVP＞d（CH2）5[肌氨酸7]AVP，这是选择性V2放射性配体的典型特征。肾脏中[3H]去甘氨酰胺（9）-d（CH2）5[D-异亮氨酸2，异亮氨酸4]AVP结合位点的放射自显影定位显示，内髓和外髓结合密集，皮质结合较少，这与已知的肾脏V2受体分布一致。