Cornett L E, Cate C M
Department of Physiology and Biophysics, University of Arkansas for Medical Sciences, Little Rock, Arkansas 72205.
J Recept Res. 1989;9(1):1-18. doi: 10.3109/10799898909066041.
We compared [3H] arginine8 vasopressin (AVP) and [3H] 1-beta-mercapto-beta, beta-cyclopentamethylene propionic acid, O-methyl tyrosine2, arginine8 vasopressin (d(CH2)5 Tyr(Me)AVP), a selective V1 receptor antagonist, as radioligands for the rat hepatocyte V1 receptor. Both radioligands bound with high affinity to a site in partially purified membranes prepared from Long Evans rat hepatocytes. The binding site concentrations obtained with either radioligand, 608 +/- 101 fmol/mg protein (n = 5) with [3H] AVP and 603 +/- 62 fmol/mg protein (n = 5) with [3H]d(CH2)5 Tyr(Me)AVP, were not significantly (p greater than 0.5) different. Furthermore, the rank order of potency of a series of synthetic vasopressin analogs and related peptides were identical in competition studies using either radioligand and were consistent with a V1 receptor interaction. Our results demonstrate that [3H] d(CH2)5 Tyr(Me)AVP is a suitable radioligand to study the V1 receptor subtype.
我们比较了[3H]精氨酸8血管加压素（AVP）和[3H]1-β-巯基-β，β-环亚戊基丙酸、O-甲基酪氨酸2、精氨酸8血管加压素（d(CH2)5Tyr(Me)AVP，一种选择性V1受体拮抗剂）作为大鼠肝细胞V1受体放射性配体的情况。两种放射性配体都以高亲和力结合到从Long Evans大鼠肝细胞制备的部分纯化膜中的一个位点。用[3H]AVP获得的结合位点浓度为608±101 fmol/mg蛋白（n = 5），用[3H]d(CH2)5Tyr(Me)AVP获得的结合位点浓度为603±62 fmol/mg蛋白（n = 5），两者无显著差异（p>0.5）。此外，在使用任一放射性配体的竞争研究中，一系列合成血管加压素类似物和相关肽的效价顺序相同，且与V1受体相互作用一致。我们的结果表明，[3H]d(CH2)5Tyr(Me)AVP是研究V1受体亚型的合适放射性配体。
