利用选择性配体[3H]森克肽对大鼠和豚鼠皮质膜中NK-3结合位点的表征。

Characterization of NK-3 binding sites in rat and guinea pig cortical membranes by the selective ligand [3H]Senktide.

作者信息

Renzetti A R, Barsacchi P, Criscuoli M, Lucacchini A

机构信息

Department of Pharmacology, Laboratori Guidotti S.p.A., Pisa, Italy.

出版信息

Neuropeptides. 1991 Mar;18(3):107-14. doi: 10.1016/0143-4179(91)90101-n.

DOI:10.1016/0143-4179(91)90101-n

PMID:1712430

Abstract

We have used [3H]Senktide, a selective Neurokinin B receptor ligand, for the characterization of NK-3 receptors in rat and guinea pig CNS membranes. Scatchard analysis of saturation binding studies in cerebral cortex membranes indicated that this ligand bound to a single site with apparent high affinity (KD = 4.6 +/- 1.6 and 3.1 +/- 0.37 nM, Bmax = 13.7 +/- 1.6 and 21.8 +/- 2.2 fmol/mg protein in rat and guinea pig membranes, respectively). However, in competition studies with a group of neurokinins and related peptides two different rank orders of affinities were obtained, as follows: NKB greater than [MePhe7]-NKB greater than or equal to Arg0-NKB greater than or equal to Senktide much greater than NKA greater than SP, in rat membranes, and [MePhe7]NKB greater than Senktide = NKB greater than Arg0-NKB much greater than SP greater than NKA, in guinea pig membranes.

摘要

我们使用了[3H]Senktide（一种选择性神经激肽B受体配体）来鉴定大鼠和豚鼠中枢神经系统膜中的NK-3受体。对大脑皮质膜饱和结合研究进行的Scatchard分析表明，该配体以明显的高亲和力与单一位点结合（大鼠和豚鼠膜中的KD分别为4.6±1.6和3.1±0.37 nM，Bmax分别为13.7±1.6和21.8±2.2 fmol/mg蛋白质）。然而，在与一组神经激肽和相关肽的竞争研究中，获得了两种不同的亲和力排序，如下：在大鼠膜中，NKB＞[MePhe7]-NKB≥Arg0-NKB≥Senktide＞＞NKA＞SP；在豚鼠膜中，[MePhe7]NKB＞Senktide = NKB＞Arg0-NKB＞＞SP＞NKA。