Direct evidence for the interaction of neurokinin A with the tachykinin NK(1) receptor in tissue.
Direct evidence for the interaction of neurokinin A with the tachykinin NK(1) receptor in tissue.
复制标题
神经激肽 A 与组织中速激肽 NK(1) 受体相互作用的直接证据。
DOI：
10.1016/s0014-2999(01)01107-4
复制
发表时间：
2001
影响因子：
5
通讯作者：
Leeman,SE
中科院分区：
文献类型：
--
作者：
Bremer,AA;Tansky,MF;Wu,M;Boyd,ND;Leeman,SE
神经激肽A（NKA）是一种速激肽肽，与速激肽NK2受体有高亲和力结合。然而，最近的同源结合研究表明，神经激肽A也是速激肽NK1受体的高亲和力配体。在这份报告中，我们证明了光反应性神经激肽A类似物特异性标记大鼠下颌下腺膜中的NK1受体，并通过生物测定表明神经激肽A是唾液分泌的有效刺激物。通过在光标记和功能测定中使用特异性非肽拮抗剂，我们明确地证明了神经激肽A可以特异性地与NK1受体在体内相互作用，并引起NK1受体介导的生理反应。
Neurokinin A (NKA) is a tachykinin peptide that binds with high affinity to the tachykinin NK2receptor. Recent homologous binding studies, however, have shown that neurokinin A is also a high-affinity ligand for the tachykinin NK1receptor. In this report, we demonstrate that a photoreactive neurokinin A analogue specifically labels the NK1receptor in rat submandibular gland membranes and show via bioassay that neurokinin A is a potent stimulator of salivary secretion. Through the use of specific non-peptide antagonists in both photolabeling and functional assays, we unequivocally demonstrate that neurokinin A can specifically interact with the NK1receptor in vivo and elicit NK1receptor-mediated physiological responses.