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Guide to receptors and channels, 2nd edition.《受体与离子通道指南》第二版
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2
Molecular cloning, functional characterization of the porcine transient receptor potential V1 (pTRPV1) and pharmacological comparison with endogenous pTRPV1.猪瞬时受体电位香草酸亚型1（pTRPV1）的分子克隆、功能特性及与内源性pTRPV1的药理学比较
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Mechanisms involved in the nociception produced by peripheral protein kinase c activation in mice.小鼠外周蛋白激酶C激活产生伤害感受的相关机制。
Pain. 2005 Sep;117(1-2):171-81. doi: 10.1016/j.pain.2005.06.001.
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Pre- and postsynaptic localization of the 5-HT7 receptor in rat dorsal spinal cord: immunocytochemical evidence.5-羟色胺7受体在大鼠脊髓背角的突触前和突触后定位：免疫细胞化学证据
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P2X2 receptors are essential for [Ca2+]i increases in response to ATP in cultured rat myenteric neurons.P2X2受体对于培养的大鼠肠肌间神经元中因ATP刺激而引起的细胞内钙离子浓度（[Ca2+]i）升高至关重要。
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Peripheral inflammation selectively increases TRPV1 function in IB4-positive sensory neurons from adult mouse.外周炎症选择性地增强成年小鼠IB4阳性感觉神经元中TRPV1的功能。
Pain. 2005 May;115(1-2):37-49. doi: 10.1016/j.pain.2005.02.010.
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Sensitization of TRPV1 by EP1 and IP reveals peripheral nociceptive mechanism of prostaglandins.EP1和IP对TRPV1的致敏作用揭示了前列腺素的外周伤害感受机制。
Mol Pain. 2005 Jan 17;1:3. doi: 10.1186/1744-8069-1-3.
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TRPV1 function in mouse colon sensory neurons is enhanced by metabotropic 5-hydroxytryptamine receptor activation.代谢型5-羟色胺受体激活可增强小鼠结肠感觉神经元中的TRPV1功能。
J Neurosci. 2004 Oct 27;24(43):9521-30. doi: 10.1523/JNEUROSCI.2639-04.2004.
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Interaction between protein kinase Cmu and the vanilloid receptor type 1.蛋白激酶Cμ与1型香草酸受体之间的相互作用。
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10
Differential pH and capsaicin responses of Griffonia simplicifolia IB4 (IB4)-positive and IB4-negative small sensory neurons.简单叶豆（Griffonia simplicifolia）IB4（IB4）阳性和IB4阴性小感觉神经元的不同pH值和辣椒素反应
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代谢型5-羟色胺受体激活对大鼠初级感觉神经元中瞬时受体电位V1功能的增强作用

Potentiation of transient receptor potential V1 functions by the activation of metabotropic 5-HT receptors in rat primary sensory neurons.

作者信息

Ohta Toshio, Ikemi Yuki, Murakami Matsuka, Imagawa Toshiaki, Otsuguro Ken-Ichi, Ito Shigeo

机构信息

Laboratory of Pharmacology, Department of Biochemical Sciences, Graduate School of Veterinary Medicine, Hokkaido University, Sapporo 060-0818, Japan.

出版信息

J Physiol. 2006 Nov 1;576(Pt 3):809-22. doi: 10.1113/jphysiol.2006.112250. Epub 2006 Aug 10.

DOI:10.1113/jphysiol.2006.112250
PMID:16901936
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1890424/
Abstract

5-Hydroxytryptamine (5-HT) is one of the major chemical mediators released in injured and inflamed tissue and is capable of inducing hyperalgesia in vivo. However, the cellular mechanisms of 5-HT-induced hyperalgesia remain unclear. Transient receptor potential V1 (TRPV1) plays a pivotal role in nociceptive receptors. In the present study, we determined whether 5-HT changes TRPV1 functions in cultured dorsal root ganglion (DRG) neurons isolated from neonatal rats, using Ca(2+) imaging and whole-cell patch-clamp techniques. In more than 70% of DRG neurons, 5-HT potentiated the increases of Ca(2+) induced by capsaicin, protons and noxious heat. Capsaicin-induced current and depolarizing responses, and proton-induced currents were also augmented by 5-HT. RT-PCR analysis revealed the expression of 5-HT(2A) and 5-HT(7) receptors in rat DRG neurons. Agonists for 5-HT(2A) and 5-HT(7) receptors mimicked the potentiating effect of 5-HT, and their antagonists decreased it. In DRG ipsilateral to the complete Freund's adjuvant-injected inflammation side, expression levels of 5-HT(2A) and 5-HT(7) mRNAs increased, and the potentiating effect of 5-HT was more prominent than in the contralateral control side. These results suggest that the PKC- and PKA-mediated signalling pathways are involved in the potentiating effect of 5-HT on TRPV1 functions through the activation of 5-HT(2A) and 5-HT(7) receptors, respectively. Under inflammatory conditions, the increases of the biosynthesis of these 5-HT receptors may lead to further potentiation of TRPV1 functions, resulting in the generation of inflammatory hyperalgesia in vivo.

摘要

5-羟色胺（5-HT）是在受伤和发炎组织中释放的主要化学介质之一，能够在体内诱发痛觉过敏。然而，5-HT诱发痛觉过敏的细胞机制仍不清楚。瞬时受体电位V1（TRPV1）在伤害性感受器中起关键作用。在本研究中，我们使用Ca(2+)成像和全细胞膜片钳技术，确定5-HT是否会改变从新生大鼠分离的培养背根神经节（DRG）神经元中TRPV1的功能。在超过70%的DRG神经元中，5-HT增强了辣椒素、质子和有害热诱导的Ca(2+)增加。5-HT还增强了辣椒素诱导的电流和去极化反应以及质子诱导的电流。逆转录聚合酶链反应（RT-PCR）分析显示大鼠DRG神经元中5-HT(2A)和5-HT(7)受体的表达。5-HT(2A)和5-HT(7)受体激动剂模拟了5-HT的增强作用，而它们的拮抗剂则降低了这种作用。在完全弗氏佐剂注射炎症侧同侧的DRG中，5-HT(2A)和5-HT(7) mRNA的表达水平增加，5-HT的增强作用比 contralateral 对照侧更明显。这些结果表明，蛋白激酶C（PKC）和蛋白激酶A（PKA）介导的信号通路分别通过激活5-HT(2A)和5-HT(7)受体参与了5-HT对TRPV1功能的增强作用。在炎症条件下，这些5-HT受体生物合成的增加可能导致TRPV1功能的进一步增强，从而在体内产生炎症性痛觉过敏。