编辑“︁TRPV1”︁（章节）

== 临床意义 ==

针对多种动物的研究发现，阻止TRPV1发挥作用会导致体温上升，包括人类及鼠类。这一发现暗示该通道涉及生物体温调节过程<ref name="pmid17392452">{{cite journal en| author = Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, Juan T, Deng H, Han B, Klionsky L, Kuang R, Le A, Tamir R, Wang J, Youngblood B, Zhu D, Norman MH, Magal E, Treanor JJ, Louis JC | title = The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation | journal = J. Neurosci. | volume = 27 | issue = 13 | pages = 3366–74 | pmid = 17392452 | doi = 10.1523/JNEUROSCI.4833-06.2007 | url =https://archive.org/details/sim_journal-of-neuroscience_2007-03-28_27_13/page/3366|date=March 2007}}</ref>。 而最近，AMG517这种高度针对TRPV1的[[受体]][[拮抗剂]]已不再用于临床试验，这是因为它会导致体温升高至无法接受的水平<ref name="pmid18337008">{{cite journal en| author = Gavva NR, Treanor JJ, Garami A, Fang L, Surapaneni S, Akrami A, Alvarez F, Bak A, Darling M, Gore A, Jang GR, Kesslak JP, Ni L, Norman MH, Palluconi G, Rose MJ, Salfi M, Tan E, Romanovsky AA, Banfield C, Davar G | title = Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans | journal = Pain | volume = 136 | issue = 1-2 | pages = 202–10 | pmid = 18337008 | doi = 10.1016/j.pain.2008.01.024 | url =https://archive.org/details/sim_pain_2008-05_136_1-2/page/202|date=May 2008}}</ref>。近期因类似原因而停用的TRPV1受体拮抗剂还包括GRC 6211以及NGD 8243。另一种化合物SB-705498也被用于类似的临床试验，但其对体温的影响则没有相关报告<ref name="pmid17659837">{{cite journal en| author = Chizh BA, O'Donnell MB, Napolitano A, Wang J, Brooke AC, Aylott MC, Bullman JN, Gray EJ, Lai RY, Williams PM, Appleby JM | title = The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans | journal = Pain | volume = 132 | issue = 1-2 | pages = 132–41 | pmid = 17659837 | doi = 10.1016/j.pain.2007.06.006 | url =https://archive.org/details/sim_pain_2007-11_132_1-2/page/132|date=November 2007}}</ref>。 

TRPV1通道蛋白的后期[[磷酸化]]翻译修饰，对该通道能否发挥正常功能是至关重要的。近期[[美国]]卫生教育与福利部下的[[国家卫生研究所]]所发表的报告指出，Cdk5促使的磷酸化修饰，对该通道的配体驱动通道开启的敏感道来说是有重要關係的<ref name="pmid17194758">{{cite journal en| author = Pareek TK, Keller J, Kesavapany S, Agarwal N, Kuner R, Pant HC, Iadarola MJ, Brady RO, Kulkarni AB | title = Cyclin-dependent kinase 5 modulates nociceptive signaling through direct phosphorylation of transient receptor potential vanilloid 1 | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 104 | issue = 2 | pages = 660–5 | pmid = 17194758 | pmc = 1752192 | doi = 10.1073/pnas.0609916104 | url =  |date=January 2007}}</ref>。

=== 末梢神经系统 ===

在实验鼠上的试验表明，通过使用针对TRPV1的受体拮抗剂，可以明显减轻炎症反应及神经疼痛的伤害性<ref name="pmid16045489">{{cite journal en| author = Jhaveri MD, Elmes SJ, Kendall DA, Chapman V | title = Inhibition of peripheral vanilloid TRPV1 receptors reduces noxious heat-evoked responses of dorsal horn neurons in naïve, carrageenan-inflamed and neuropathic rats | journal = Eur. J. Neurosci. | volume = 22 | issue = 2 | pages = 361–70 | year = 2005 | pmid = 16045489 | doi = 10.1111/j.1460-9568.2005.04227.x }}</ref>。这一结果表明，TRPV1通道是能对[[辣椒素]]做出反应的唯一感受器<ref name="Story_2008">{{cite journal en | author = Story GM, Cruz-Orengo L | title = Feel the Burn | journal = American Scientist | volume = 95 | issue = 4 | pages = 326–333 | year = 2008 | pmid =  | doi =  | issn = 0003-0996 | url = http://www.americanscientist.org/template/AssetDetail/assetid/55542 | access-date = 2009-12-03 | archive-date = 2008-01-19 | archive-url = https://web.archive.org/web/20080119204957/http://www.americanscientist.org/template/AssetDetail/assetid/55542 | dead-url = no }}</ref>。

对于人类来说，作用在TRPV1感受器上的药物，应当能用于治疗与[[多发性硬化症]]、[[化疗]]或者[[截肢]]有关的神经性疼痛，也能缓解因组织损伤，如[[骨关节炎]]导致的[[炎症]]有关的疼痛<ref name="pmid18220816">{{cite journal en| author = Gunthorpe MJ, Szallasi A | title = Peripheral TRPV1 receptors as targets for drug development: new molecules and mechanisms | journal = Curr. Pharm. Des. | volume = 14 | issue = 1 | pages = 32–41 | year = 2008 | pmid = 18220816 | doi = 10.2174/138161208783330754| url = http://openurl.ingenta.com/content/nlm?genre=article&issn=1381-6128&volume=14&issue=1&spage=32&aulast=Gunthorpe }}</ref>。

最近几年，人们才意识到TRPV1通道是体温调节中的一个环节。这是因为人们发现一些针对TRPV1的选择性受体拮抗剂会导致体温升高（[[高温症]]），这说明在体内TRPV1通道通过告知大脑应当降温，来不间断的调节着体温<ref name="pmid17392452">{{cite journal en| author = Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, Juan T, Deng H, Han B, Klionsky L, Kuang R, Le A, Tamir R, Wang J, Youngblood B, Zhu D, Norman MH, Magal E, Treanor JJ, Louis JC | title = The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation | journal = J. Neurosci. | volume = 27 | issue = 13 | pages = 3366–74 | pmid = 17392452 | doi = 10.1523/JNEUROSCI.4833-06.2007 | url =https://archive.org/details/sim_journal-of-neuroscience_2007-03-28_27_13/page/3366|date=March 2007}}</ref> 。如果因某种原因导致TRPV1通道没有及时发出这种降温信号，则体温会不断上升。于此类似的，这也是为什么食用含有辣椒素（针对TRPV1的一种激动剂）的食物会导致流汗——大脑希望通过该方式来降低体温。最近的一个研究表明，在内脏中TRPV1通道也会持续的工作，通过发出降低体温的信号来不断调节体温<ref name="pmid17626206">{{cite journal en|author=Steiner AA, Turek VF, Almeida MC, Burmeister JJ, Oliveira DL, Roberts JL, Bannon AW, Norman MH, Louis JC, Treanor JJ, Gavva NR, Romanovsky AA | title = Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors | journal = J. Neurosci. | volume = 27 | issue = 28 | pages = 7459–68 | pmid = 17626206 | doi = 10.1523/JNEUROSCI.1483-07.2007 | url =https://archive.org/details/sim_journal-of-neuroscience_2007-07-11_27_28/page/7458|date=July 2007}}</ref>。因此，该通道的主要功能被认为是调节体温<ref name="pmid18805596"> {{cite journal en|author=Gavva NR | title = Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1 | journal = Trends Pharmacol Sci. | volume = 29 | pages = 550–557 | year = 2008 |issue=11 |doi=10.1016/j.tips.2008.08.003 }}</ref>。

=== 中枢神经系统 ===

TRPV1通道在高级的[[中枢神经系统]]中，也有相应的表达。该通道除了被认为可以用于治疗神经性疼痛之外，还可以治疗其它症状例如[[焦虑]]<ref name="pmid18220817">{{cite journal en| author = Di Marzo V, Starowicz K, Cristino L | title = TRPV1 receptors in the central nervous system: potential for previously unforeseen therapeutic applications | journal = Curr. Pharm. Des. | volume = 14 | issue = 1 | pages = 42–54 | year = 2008 | pmid = 18220817 | doi = 10.2174/138161208783330790| url = http://openurl.ingenta.com/content/nlm?genre=article&issn=1381-6128&volume=14&issue=1&spage=42&aulast=Starowicz }}</ref>。此外，该通道似乎还与[[海马区]]中的[[长时程抑制效应]]有关<ref name="pmid18341994">{{cite journal en| author = Gibson HE, Edwards JG, Page RS, Van Hook MJ, Kauer JA | title = TRPV1 Channels Mediate Long-Term Depression at Synapses on Hippocampal Interneurons | journal = Neuron | volume = 57 | issue = 5 | pages = 746–59 | year = 2008 | pmid = 18341994 | doi = 10.1016/j.neuron.2007.12.027 }}</ref>。而长时程抑制则会减弱形成新的记忆的能力，于此相反的[[长时程增强效应]]则会帮助形成记忆。在[[突触]]中形成的抑制与增强模式，则为形成记忆的方式提供了编码。长时程抑制效应及其导致突触链接剪枝的效果，对于形成记忆来说是很重要的。针对实验鼠大脑切片的研究发现，通过热或者辣椒素的刺激可以引发长时程抑制效应，而辣椒素受体阻断剂则能阻碍辣椒素所引起的抑制效应<ref name="pmid18341994"/>。因此，正如已经在末梢神经系统中应用TRPV1拮抗剂来缓解疼痛那样，也许将来有可能通过在中枢神经系统中使用这种拮抗剂来治疗一些疾病，例如[[癫痫]]。