[125I][甲硫苯丙氨酸7]神经激肽B与速激肽NK3受体结合的特性：种间差异的证据。

Characterisation of [125I][MePhe7]neurokinin B binding to tachykinin NK3 receptors: evidence for interspecies variance.

作者信息

Suman-Chauhan N, Grimson P, Guard S, Madden Z, Chung F Z, Watling K, Pinnock R, Woodruff G

机构信息

Parke Davis Neuroscience Research Centre, Addenbrookes Hospital Site, Cambridge, UK.

出版信息

Eur J Pharmacol. 1994 Sep 15;269(1):65-72. doi: 10.1016/0922-4106(94)90027-2.

DOI:10.1016/0922-4106(94)90027-2

PMID:7530207

Abstract

Human tachykinin NK3 receptors expressed in Chinese hamster ovary (CHO-K1) cells were characterised using the novel radioligand [125I]iodohistidyl,[MePhe7]neurokinin B ([125I][MePhe7]neurokinin B). [125I][MePhe7]neurokinin B was shown to label human NK3 binding sites with high affinity in a saturable and reversible manner. The rank order of affinity of a range of tachykinin ligands confirmed that the tachykinin receptor expressed was the NK3 receptor type. An interspecies comparison of NK3 binding sites revealed pharmacological differences between human, guinea pig and rat tachykinin NK3 receptors. The NK2 selective antagonist SR 48968, inhibited binding of [125I][MePhe7]neurokinin B to NK3 binding sites with Ki values of 287 nM and 205 nM in human and guinea pig respectively, but was > 30-fold less active in the rat.

摘要

使用新型放射性配体[125I]碘组氨酰、[MePhe7]神经激肽B（[125I][MePhe7]神经激肽B）对在中国仓鼠卵巢（CHO-K1）细胞中表达的人速激肽NK3受体进行了表征。结果表明，[125I][MePhe7]神经激肽B能够以饱和且可逆的方式高亲和力标记人NK3结合位点。一系列速激肽配体的亲和力排序证实，所表达的速激肽受体为NK3受体类型。对NK3结合位点的种间比较揭示了人、豚鼠和大鼠速激肽NK3受体之间的药理学差异。NK2选择性拮抗剂SR 48968抑制[125I][MePhe7]神经激肽B与NK3结合位点的结合，在人和豚鼠中的Ki值分别为287 nM和205 nM，但在大鼠中的活性则低30倍以上。