Direct evidence for the interaction of neurokinin A with the tachykinin NK1 receptor in tissue

被引:8
作者
Bremer, AA [1 ]
Tansky, MF [1 ]
Wu, MY [1 ]
Boyd, ND [1 ]
Leeman, SE [1 ]
机构
[1] Boston Univ, Sch Med, Dept Pharmacol & Expt Therapeut, Boston, MA 02118 USA
关键词
neurokinin A; tachykinin NK1 receptor; photoaffinity labeling; bioassay;
D O I
10.1016/S0014-2999(01)01107-4
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Neurokinin A (NKA) is a tachykinin peptide that binds with high affinity to the tachykinin NK, receptor. Recent homologous binding studies, however, have shown that neurokinin A is also a high-affinity ligand for the tachykinin NK, receptor. In this report, we demonstrate that a photoreactive neurokinin A analogue specifically labels the NK, receptor 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 NK, receptor in vivo and elicit NK, receptor-mediated physiological responses. (C) 2001 Published by Elsevier Science B.V.
引用
收藏
页码:143 / 147
页数:5
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