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比較的最近遺伝子が単離されたカリウムチャネルであり、他のカリウムチャネルに比べると生理的な機能や構造活性相関の解析は進んでいない。電気生理学的特性から[[背景(漏洩)カリウム電流]]を担っていると考えられ静止膜電位の形成や膜抵抗の決定に関与していると考えられている。TREK1で形成されるイオンチャネルは最もよく研究されているK2Pチャネルであり、膜電位や細胞膜の[[ホスファチジルイノシトール#PI.284.2C5.29P2|ホスファチジルイノシトール-4,5-二リン酸]]との相互作用、[[リン酸化]]、pH、膜の伸展、熱などによる制御が示され、多様式polymodalな制御を受けるイオンチャネルであると知られてきている<ref><pubmed>17375039</pubmed></ref>。 | 比較的最近遺伝子が単離されたカリウムチャネルであり、他のカリウムチャネルに比べると生理的な機能や構造活性相関の解析は進んでいない。電気生理学的特性から[[背景(漏洩)カリウム電流]]を担っていると考えられ静止膜電位の形成や膜抵抗の決定に関与していると考えられている。TREK1で形成されるイオンチャネルは最もよく研究されているK2Pチャネルであり、膜電位や細胞膜の[[ホスファチジルイノシトール#PI.284.2C5.29P2|ホスファチジルイノシトール-4,5-二リン酸]]との相互作用、[[リン酸化]]、pH、膜の伸展、熱などによる制御が示され、多様式polymodalな制御を受けるイオンチャネルであると知られてきている<ref><pubmed>17375039</pubmed></ref>。 | ||
{| class="wikitable" | |||
|+Potassium channel classes, function, and pharmacology.<ref name=Rang60>{{cite book | author=Rang, HP | title = Pharmacology | publisher = Churchill Livingstone | location = Edinburgh | year = 2003 | isbn = 0-443-07145-4 | oclc = | doi = | page = 60 }}</ref> | |||
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|'''Class''' | |||
! Subclasses | |||
!Function | |||
!Blockers | |||
!Activators | |||
|- | |||
| [[Calcium-activated potassium channel|Calcium-activated]] <br /> 6[[transmembrane helix|T]] & 1[[pore-forming loop|P]] | |||
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* [[BK channel]] | |||
* [[SK channel]] | |||
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* inhibition following stimuli increasing intracellular calcium | |||
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* [[charybdotoxin]], [[iberiotoxin]] | |||
* [[apamin]] | |||
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* 1-EBIO | |||
* NS309 | |||
* CyPPA | |||
|- | |||
|rowspan=3 | [[Inward-rectifier potassium ion channel|Inwardly rectifying]] <br /> 2[[transmembrane helix|T]] & 1[[pore-forming loop|P]] | |||
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* [[ROMK]] (K<sub>ir</sub>1.1) | |||
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* recycling and secretion of potassium in [[nephron]]s | |||
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* Nonselective: Ba<sup>2+</sup>, Cs<sup>+</sup> | |||
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* none | |||
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* [[G protein-coupled inwardly-rectifying potassium channel|GPCR regulated]] (K<sub>ir</sub>3.x) | |||
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* mediate the inhibitory effect of many [[GPCR]]s | |||
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* [[GPCR]] antagonists | |||
* [[ifenprodil]]<ref name="pmid16123769"><pubmed>16123769</pubmed></ref> | |||
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* [[GPCR]] agonists | |||
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* [[ATP-sensitive K+ channels|ATP-sensitive]] (K<sub>ir</sub>6.x) | |||
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* close when [[adenosine triphosphate|ATP]] is high to promote [[insulin]] secretion | |||
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* [[glibenclamide]] | |||
* [[tolbutamide]] | |||
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* [[diazoxide]] | |||
* [[pinacidil]] | |||
|- | |||
| [[Tandem pore domain potassium channel|Tandem pore domain]] <br /> 4[[transmembrane helix|T]] & 2[[pore-forming loop|P]] | |||
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* TWIK ([[KCNK1|TWIK-1]], [[KCNK6|TWIK-2]], [[KCNK7]])<ref name="pmid20393194">{{cite journal | author = Enyedi P, Czirják G | title = Molecular background of leak K<sup>+</sup> currents: two-pore domain potassium channels | journal = Physiological Reviews | volume = 90 | issue = 2 | pages = 559–605 | year = 2010 | pmid = 20393194 | doi = 10.1152/physrev.00029.2009 }}</ref><ref name="pmid17652773">{{cite journal | author = Lotshaw DP | title = Biophysical, pharmacological, and functional characteristics of cloned and native mammalian two-pore domain K+ channels | journal = Cell Biochemistry and Biophysics | volume = 47 | issue = 2 | pages = 209–56 | year = 2007 | pmid = 17652773 | doi = 10.1007/s12013-007-0007-8 }}</ref> | |||
* TREK ([[KCNK2|TREK-1]], [[KCNK10|TREK-2]], [[KCNK4|TRAAK]]<ref name="pmid9628867">{{cite journal | author = Fink M, Lesage F, Duprat F, Heurteaux C, Reyes R, Fosset M, Lazdunski M | title = A neuronal two P domain K+ channel stimulated by arachidonic acid and polyunsaturated fatty acids | journal = The EMBO Journal | volume = 17 | issue = 12 | pages = 3297–308 | year = 1998 | pmid = 9628867 | pmc = 1170668 | doi = 10.1093/emboj/17.12.3297 }}</ref>)<ref name="pmid20393194"/><ref name="pmid17652773"/> | |||
* TASK ([[KCNK3|TASK-1]], [[KCNK9|TASK-3]], [[KCNK15|TASK-5]])<ref name="pmid20393194"/><ref name="pmid17652773"/> | |||
* TALK ([[KCNK5|TASK-2]],<ref name="pmid11256078">{{cite journal | author = Goldstein SA, Bockenhauer D, O'Kelly I, Zilberberg N | title = Potassium leak channels and the KCNK family of two-P-domain subunits | journal = Nature Reviews Neuroscience | volume = 2 | issue = 3 | pages = 175–84 | year = 2001 | pmid = 11256078 | doi = 10.1038/35058574 }}</ref> [[KCNK16|TALK-1]], [[KCNK17|TALK-2]])<ref name="pmid20393194"/><ref name="pmid17652773"/> | |||
* THIK ([[KCNK13|THIK-1]], [[KCNK12|THIK-2]])<ref name="pmid20393194"/><ref name="pmid17652773"/> | |||
* [[KCNK18|TRESK]]<ref name="pmid20393194"/><ref name="pmid17652773"/><ref name="pmid12754259">{{cite journal | author = Sano Y, Inamura K, Miyake A, Mochizuki S, Kitada C, Yokoi H, Nozawa K, Okada H, Matsushime H, Furuichi K | title = A novel two-pore domain K+ channel, TRESK, is localized in the spinal cord | journal = The Journal of Biological Chemistry | volume = 278 | issue = 30 | pages = 27406–12 | year = 2003 | pmid = 12754259 | doi = 10.1074/jbc.M206810200 }}</ref><ref name="pmid14981085">{{cite journal | author = Czirják G, Tóth ZE, Enyedi P | title = The two-pore domain K+ channel, TRESK, is activated by the cytoplasmic calcium signal through calcineurin | journal = The Journal of Biological Chemistry | volume = 279 | issue = 18 | pages = 18550–8 | year = 2004 | pmid = 14981085 | doi = 10.1074/jbc.M312229200 }}</ref> | |||
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* Contribute to [[resting potential]] | |||
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* [[bupivacaine]]<ref name="pmid10201682">{{cite journal | doi = 10.1097/00000542-199904000-00024 | author = Kindler CH, Yost CS, Gray AT | title = Local anesthetic inhibition of baseline potassium channels with two pore domains in tandem | journal = Anesthesiology | volume = 90 | issue = 4 | pages = 1092–102 | year = 1999 | pmid = 10201682 }}</ref><ref name="pmid11249964">{{cite journal | author = Meadows HJ, Randall AD | title = Functional characterisation of human TASK-3, an acid-sensitive two-pore domain potassium channel | journal = Neuropharmacology | volume = 40 | issue = 4 | pages = 551–9 | year = 2001 | pmid = 11249964 | doi = 10.1016/S0028-3908(00)00189-1 }}</ref><ref name="pmid12660311">{{cite journal | author = Kindler CH, Paul M, Zou H, Liu C, Winegar BD, Gray AT, Yost CS | title = Amide local anesthetics potently inhibit the human tandem pore domain background K+ channel TASK-2 (KCNK5) | journal = Journal of Pharmacology and Experimental Therapeutics | volume = 306 | issue = 1 | pages = 84–92 | year = 2003 | pmid = 12660311 | doi = 10.1124/jpet.103.049809 }}</ref><ref name="pmid12760993">{{cite journal | author = Punke MA, Licher T, Pongs O, Friederich P | title = Inhibition of human TREK-1 channels by bupivacaine | journal = Anesthesia & Analgesia | volume = 96 | issue = 6 | pages = 1665–73 | year = 2003 | pmid = 12760993 | doi = 10.1213/01.ANE.0000062524.90936.1F }}</ref> | |||
* [[quinidine]]<ref name="pmid11249964"/><ref name="pmid8605869">{{cite journal | author = Lesage F, Guillemare E, Fink M, Duprat F, Lazdunski M, Romey G, Barhanin J | title = TWIK-1, a ubiquitous human weakly inward rectifying K+ channel with a novel structure | journal = The EMBO Journal | volume = 15 | issue = 5 | pages = 1004–11 | year = 1996 | pmid = 8605869 | pmc = 449995 }}</ref><ref name="pmid9312005">{{cite journal | author = Duprat F, Lesage F, Fink M, Reyes R, Heurteaux C, Lazdunski M | title = TASK, a human background K+ channel to sense external pH variations near physiological pH | journal = The EMBO Journal | volume = 16 | issue = 17 | pages = 5464–71 | year = 1997 | pmid = 9312005 | pmc = 1170177 | doi = 10.1093/emboj/16.17.5464 }}</ref><ref name="pmid9812978">{{cite journal | author = Reyes R, Duprat F, Lesage F, Fink M, Salinas M, Farman N, Lazdunski M | title = Cloning and expression of a novel pH-sensitive two pore domain K+ channel from human kidney | journal = The Journal of Biological Chemistry | volume = 273 | issue = 47 | pages = 30863–9 | year = 1998 | pmid = 9812978 | doi = 10.1074/jbc.273.47.30863 }}</ref><ref name="pmid10784345">{{cite journal | author = Meadows HJ, Benham CD, Cairns W, Gloger I, Jennings C, Medhurst AD, Murdock P, Chapman CG | title = Cloning, localisation and functional expression of the human orthologue of the TREK-1 potassium channel | journal = Pflügers Archiv : European Journal of Physiology | volume = 439 | issue = 6 | pages = 714–22 | year = 2000 | pmid = 10784345 | doi = 10.1007/s004240050997 }}</ref> | |||
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* [[halothane]]<ref name="pmid11249964"/><ref name="pmid10321245">{{cite journal | author = Patel AJ, Honoré E, Lesage F, Fink M, Romey G, Lazdunski M| title = Inhalational anesthetics activate two-pore-domain background K+ channels | journal = Nature Neuroscience | volume = 2 | issue = 5 | pages = 422–6 | year = 1999 | pmid = 10321245 | doi = 10.1038/8084 }}</ref><ref name="pmid10839924">{{cite journal | doi = 10.1097/00000542-200006000-00032 | author = Gray AT, Zhao BB, Kindler CH, Winegar BD, Mazurek MJ, Xu J, Chavez RA, Forsayeth JR, Yost CS | title = Volatile anesthetics activate the human tandem pore domain baseline K+ channel KCNK5 | journal = Anesthesiology | volume = 92 | issue = 6 | pages = 1722–30 | year = 2000 | pmid = 10839924 }}</ref> | |||
|- | |||
| [[Voltage-gated potassium channel|Voltage-gated]] <br /> 6[[transmembrane helix|T]] & 1[[pore-forming loop|P]] | |||
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* [[hERG]] (K<sub>v</sub>11.1) | |||
* [[KvLQT1]] (K<sub>v</sub>7.1) | |||
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* [[action potential]] [[repolarization]] | |||
* limits frequency of action potentials (disturbances cause [[Cardiac dysrhythmia|dysrhythmia]]) | |||
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* [[tetraethylammonium]] | |||
* [[4-Aminopyridine|4-aminopyridine]] | |||
* [[dendrotoxin]]s (some types) | |||
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* [[retigabine]] (K<sub>v</sub>7)<ref name=Rogawski>{{cite journal |author=Rogawski MA, Bazil CW |title=New Molecular Targets for Antiepileptic Drugs: α2δ, SV2A, and Kv7/KCNQ/M Potassium Channels |journal=Curr Neurol Neurosci Rep |volume=8 |issue=4 |pages=345–52 |year=2008 |month=July |pmid=18590620 |pmc=2587091 |doi=10.1007/s11910-008-0053-7}}</ref> | |||
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== 神経細胞におけるカリウムチャネルの役割 == | == 神経細胞におけるカリウムチャネルの役割 == |