环磷酸腺苷（cAMP）信号通路使非洲爪蟾卵母细胞及中国仓鼠卵巢（CHO）细胞中表达的香草酸受体1（VR1）变得敏感。

The cAMP pathway sensitizes VR1 expressed in oocytes from Xenopus laevis and in CHO cells.

作者信息

Vulcu Sebastian D, Rupp Johanna, Wiwie Caroline, Gillen Clemens, Jostock Ruth, Nawrath Hermann

机构信息

Department of Pharmacology, University of Mainz, Mainz, Germany.

出版信息

Pharmacology. 2003 Sep;69(1):38-43. doi: 10.1159/000071265.

DOI:10.1159/000071265

PMID:12886029

Abstract

The vanilloid receptor 1 (VR1) is a heat-activated cation channel which also responds to capsaicin and other chemical stimuli. Protein kinase C has a stimulatory effect on VR1 activity, either alone or after activation with capsaicin. The influence of the cAMP-signaling pathway on the effects of capsaicin is controversial. To clarify this, the actions of capsaicin and the modulatory effects of forskolin, pCPT-cAMP, and isobutylmethylxanthine were studied in Xenopus laevis oocytes expressing rat VR1 and in CHO cells expressing human VR1. Capsaicin activated the VR1 channel and increased the intracellular calcium concentration. The effects of capsaicin were enhanced by forskolin, pCPT-cAMP, and isobutylmethylxanthine. A modulatory function of the cAMP system on VR1 activation could, therefore, modulate heat sensation and pain.

摘要

香草酸受体1（VR1）是一种热激活阳离子通道，它也对辣椒素和其他化学刺激作出反应。蛋白激酶C对VR1活性具有刺激作用，无论是单独作用还是在用辣椒素激活后。环磷酸腺苷（cAMP）信号通路对辣椒素作用的影响存在争议。为了阐明这一点，在表达大鼠VR1的非洲爪蟾卵母细胞和表达人VR1的中国仓鼠卵巢（CHO）细胞中研究了辣椒素的作用以及福斯可林、对氯苯硫代环磷腺苷（pCPT-cAMP）和异丁基甲基黄嘌呤的调节作用。辣椒素激活了VR1通道并增加了细胞内钙浓度。福斯可林、pCPT-cAMP和异丁基甲基黄嘌呤增强了辣椒素的作用。因此，cAMP系统对VR1激活的调节功能可能会调节热感觉和疼痛。