介导多种物种离体气管制剂收缩的神经激肽受体的特性研究。

Characterisation of the neurokinin receptors mediating contraction of isolated tracheal preparations from a variety of species.

作者信息

Sheldrick R L, Ball D I, Coleman R A

机构信息

Peripheral Pharmacology Department, Glaxo Group Research Ltd., Ware, Herfordshire, U.K.

出版信息

Agents Actions Suppl. 1990;31:205-9. doi: 10.1007/978-3-0348-7379-6_25.

DOI:10.1007/978-3-0348-7379-6_25

PMID:1706905

Abstract

The effects of neurokinin (NK) agonists on isolated tracheal preparations from rat (RT), pig (PT), rabbit (RbT) and guinea-pig (GPT) have been investigated. None of the NKs contracted RT, suggesting that this preparation lacks NK receptors mediating contraction, whereas NKs caused concentration- related contractions of PT, RbT and GPT. In PT, NK1-receptors mediate contraction since only substance P (SP) and the NK1-receptor selective agonists, SP methylester (SPOMe) and GR73632 were highly potent. In contrast, in RbT, only NKA and the selective NK2-receptor agonist, GR64349 were potent, indicating the presence of NK2-receptors. However, in GPT both NK1- and NK2-receptors appear to mediate contraction to NKs since NKA, GR73632 and GR64349 were highly potent and SP and SPOMe moderately potent agonists. This study demonstrates apparent species differences in the NK-receptor populations present in tracheal smooth muscle.

摘要

研究了神经激肽（NK）激动剂对大鼠离体气管制备物（RT）、猪离体气管制备物（PT）、兔离体气管制备物（RbT）和豚鼠离体气管制备物（GPT）的作用。没有一种NK能使RT收缩，这表明该制备物缺乏介导收缩的NK受体，而NK能引起PT、RbT和GPT的浓度依赖性收缩。在PT中，NK1受体介导收缩，因为只有P物质（SP）以及NK1受体选择性激动剂SP甲酯（SPOMe）和GR73632具有高效能。相反，在RbT中，只有神经激肽A（NKA）和选择性NK2受体激动剂GR64349具有效能，表明存在NK2受体。然而，在GPT中，NK1和NK2受体似乎都介导对NK的收缩反应，因为NKA、GR73632和GR64349是高效能激动剂，而SP和SPOMe是中效能激动剂。本研究证明了气管平滑肌中存在的NK受体群体存在明显的种属差异。