チャネル開口薬、チャネルオープナー

WordNet

without undue constriction as from e.g. tenseness or inhibition; "the clarity and resonance of an open tone"; "her natural and open response"
a clear or unobstructed space or expanse of land or water; "finally broke out of the forest into the open" (同)clear
information that has become public; "all the reports were out in the open"; "the facts had been brought to the surface" (同)surface
a tournament in which both professionals and amateurs may play
become available; "an opportunity opened up" (同)open_up
become open; "The door opened" (同)open_up
cause to open or to become open; "Mary opened the car door" (同)open_up
make available; "This opens up new possibilities" (同)open_up
start to operate or function or cause to start operating or functioning; "open a business" (同)open_up
not sealed or having been unsealed; "the letter was already open"; "the opened package lay on the table" (同)opened
used of mouth or eyes; "keep your eyes open"; "his mouth slightly opened" (同)opened
not brought to a conclusion; subject to further thought; "an open question"; "our position on this bill is still undecided"; "our lawsuit is still undetermined" (同)undecided, undetermined, unresolved
affording unobstructed entrance and exit; not shut or closed; "an open door"; "they left the door open" (同)unfastened
(set theory) of an interval that contains neither of its endpoints
accessible to all; "open season"; "an open economy"
affording free passage or access; "open drains"; "the road is open to traffic"; "open ranks"
begin or set in action, of meetings, speeches, recitals, etc.; "He opened the meeting with a long speech"
display the contents of a file or start an application as on a computer
have an opening or passage or outlet; "The bedrooms open into the hall"
having no protecting cover or enclosure; "an open boat"; "an open fire"; "open sports cars"
make the opening move; "Kasparov opened with a standard opening"
not having been filled; "the job is still open"
not requiring union membership; "an open shop employs nonunion workers"
open to or in view of all; "an open protest"; "an open letter to the editor"
ready for business; "the stores are open"
direct the flow of; "channel information towards a broad audience" (同)canalize, canalise
a television station and its programs; "a satellite TV channel"; "surfing through the channels"; "they offer more than one hundred channels" (同)television channel, TV channel
a passage for water (or other fluids) to flow through; "the fields were crossed with irrigation channels"; "gutters carried off the rainwater into a series of channels under the street"
(often plural) a means of communication or access; "it must go through official channels"; "lines of communication were set up between the two firms" (同)communication channel, line
a path over which electrical signals can pass; "a channel is typically what you rent from a telephone company" (同)transmission channel
a deep and relatively narrow body of water (as in a river or a harbor or a strait linking two larger bodies) that allows the best passage for vessels; "the ship went aground in the channel"
a hand tool used for opening sealed containers (bottles or cans)
the first event in a series; "she played Chopin for her opener"; "the seasons opener was a game against the Yankees"
official routes of communication; "you have to go through channels"

PrepTutorEJDIC

…‘を'『開く』,開ける;…‘の'ふた(おおい)をとる / …‘を'『切り開いて作る』,開拓する;…‘を'全開通させる《+『名』+『up,』+『名』+『up』》 / …‘を'『広げる』《+『up』+(『out』)+『名,』+『名』+『up』(『out』)》 / …‘を'『始める』 / …‘を'開業する,開店する,開場する / (人に)〈心など〉‘を'打ち明ける,〈秘密など〉‘を'漏らす《+『名』+『to』+『名』》 / (新思想などに)〈心・目〉‘を'開く《+『名』+『to』+『名』》 / 〈戸などが〉『開く』,あく / 〈花・つぼみが〉開く《+『out』》 / 〈学校などが〉『始まる』;〈店などが〉開く / 〈道路などが〉開通する / (…に)向かって開いている,(…に)通じている《+『out』『on』(『upon,to,onto』)+『名』》 / 《副詞[句]を伴って》〈風景などが〉広がる,ひらける / 本を開く;(…)ページを開く《+『to』(《英》『at』)+『名』》 / (窓・口などが)『開いた』,開いている;(包みなどが)広げられて / (花が)咲いた / (店などが)『開いている』,開業している;(催し物が)『公開の』,だれでも入れる / 《名詞の前にのみ用いて》ふたのしてない,屋根のない,おおいのない / 広く開いた,さえぎるものがない / 公然の / 率直な,遠慮しない / さらされている,無防備の / 《補語にのみ用いて》(職・地位などが)空位の;(時間などが)あいている / (問題・議事などが)未解決の / 凍結しない,雪や霜の降らない;温和な / (漁・猟が)解禁の / (音声が)開口音の;開音節の / 《the~》戸外,野外 / 空き地;(樹木のない)開けた場所,平野
〈C〉『水路』(川・湾・運河の船の通行ができる深い部分) / 〈U〉河床・川底 / 〈C〉『海峡』 / 〈C〉みぞ(groove),(道路の)水渠(すいきょ) / 《複数形で》(運搬・伝達の)正式の経路(手続き);(一般に)経路 / 〈C〉(テレビ・ラジオの)チャンネル / …‘に'水路を開く / …‘に'みぞを堀る / …'を'伝える,流す
開ける道具 / 開ける人 / (シリーズの)第1試合;(番組などの)最初の出しもの

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/01 13:50:17」(JST)

wiki en

A channel opener, also known as a channel activator, is a type of drug which facilitates ion flow through ion channels.

An example of a class of channel openers are potassium channel openers.

References

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 先天性ＱＴ延長症候群の予後およびマネージメント prognosis and management of congenital long qt syndrome
2. 低カリウム性周期性四肢麻痺 hypokalemic periodic paralysis
3. QT短縮症候群 short qt syndrome
4. 心臓の再灌流障害 reperfusion injury of the heart
5. 狭心症の新しい治療法 new therapies for angina pectoris

English Journal

Natriuretic peptides modulate ATP-sensitive K(+) channels in rat ventricular cardiomyocytes.

Burley DS, Cox CD, Zhang J, Wann KT, Baxter GF.Author information Cardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff, CF10 3NB, UK, burleyds@cardiff.ac.uk.AbstractB-type natriuretic peptide (BNP) and C-type natriuretic peptide (CNP), and (Cys-18)-atrial natriuretic factor (4-23) amide (C-ANF), are cytoprotective under conditions of ischemia-reperfusion, limiting infarct size. ATP-sensitive K(+) channel (KATP) opening is also cardioprotective, and although the KATP activation is implicated in the regulation of cardiac natriuretic peptide release, no studies have directly examined the effects of natriuretic peptides on cardiac KATP activity. Normoxic cardiomyocytes were patch clamped in the cell-attached configuration to examine sarcolemmal KATP (sKATP) activity. The KATP opener pinacidil (200 μM) increased the open probability of the patch (NPo; values normalized to control) at least twofold above basal value, and this effect was abolished by HMR1098 10 μM, a selective KATP blocker (5.23 ± 1.20 versus 0.89 ± 0.18; P < 0.001). We then examined the effects of BNP, CNP, C-ANF and 8Br-cGMP on the sKATP current. Bath application of BNP (≥10 nM) or CNP (≥0.01 nM) suppressed basal NPo (BNP: 1.00 versus 0.56 ± 0.09 at 10 nM, P < 0.001; CNP: 1.0 versus 0.45 ± 0.16, at 0.01 nM, P < 0.05) and also abolished the pinacidil-activated current at concentrations ≥10 nM. C-ANF (≥10 nM) enhanced KATP activity (1.00 versus 3.85 ± 1.13, at 100 nM, P < 0.05). The cGMP analog 8Br-cGMP 10 nM dampened the pinacidil-activated current (2.92 ± 0.60 versus 1.53 ± 0.32; P < 0.05). Natriuretic peptides modulate sKATP current in ventricular cardiomyocytes. This may be at least partially associated with their ability to augment intracellular cGMP concentrations via NPR-A/B, or their ability to bind NPR-C with high affinity. Although the mechanism of modulation requires elucidation, these preliminary data give new insights into the relationship between natriuretic peptide signaling and sKATP in the myocardium.
Basic research in cardiology.Basic Res Cardiol.2014 Mar;109(2):402. doi: 10.1007/s00395-014-0402-4. Epub 2014 Jan 30.
B-type natriuretic peptide (BNP) and C-type natriuretic peptide (CNP), and (Cys-18)-atrial natriuretic factor (4-23) amide (C-ANF), are cytoprotective under conditions of ischemia-reperfusion, limiting infarct size. ATP-sensitive K(+) channel (KATP) opening is also cardioprotective, and although the
PMID 24477916

Sevoflurane postconditioning against cerebral ischemic neuronal injury is abolished in diet-induced obesity: Role of brain mitochondrial KATP channels.

Yang Z, Chen Y, Zhang Y, Jiang Y, Fang X, Xu J.Author information Department of Surgery, Second Hospital, Jilin University, Changchun, Jilin 130041, P.R. China.AbstractObesity is associated with increased infarct volumes and adverse outcomes following ischemic stroke. However, its effect on anesthetic postconditioning‑induced neuroprotection has not been investigated. The present study examined the effect of sevoflurane postconditioning on focal ischemic brain injury in diet‑induced obesity. Sprague‑Dawley rats were fed a high‑fat diet (HF; 45% kcal as fat) for 12 weeks to develop obesity syndrome. Rats fed a low‑fat diet (LF; 10% kcal as fat) served as controls. The HF or LF‑fed rats were subjected to focal cerebral ischemia for 60 min, followed by 24 h of reperfusion. Postconditioning was performed by exposure to sevoflurane for 15 min immediately at the onset of reperfusion. The involvement of the mitochondrial KATP (mitoKATP) channel was analyzed by the administration of a selective inhibitor of 5‑hydroxydecanoate (5‑HD) prior to sevoflurane postconditioning or by administration of diazoxide (DZX), a mitoKATP channel opener, instead of sevoflurane. The cerebral infarct volume, neurological score and motor coordination were evaluated 24 h after reperfusion. The HF‑fed rats had larger infarct volumes, and lower neurological scores than the LF‑fed rats and also failed to respond to neuroprotection by sevoflurane or DZX. By contrast, sevoflurane and DZX reduced the infarct volumes and improved the neurological scores and motor coordination in the LF‑fed rats. Pretreatment with 5‑HD inhibited sevoflurane‑induced neuroprotection in the LF‑fed rats, whereas it had no effect in the HF‑fed rats. Molecular studies demonstrated that the expression of Kir6.2, a significant mitoKATP channel component, was reduced in the brains of the HF‑fed rats compared with the LF‑fed rats. The results of this study indicate that diet‑induced obesity eliminates the ability of anesthetic sevoflurane postconditioning to protect the brain against cerebral ischemic neuronal injury, most likely due to an impaired brain mitoKATP channel.
Molecular medicine reports.Mol Med Rep.2014 Mar;9(3):843-50. doi: 10.3892/mmr.2014.1912. Epub 2014 Jan 22.
Obesity is associated with increased infarct volumes and adverse outcomes following ischemic stroke. However, its effect on anesthetic postconditioning‑induced neuroprotection has not been investigated. The present study examined the effect of sevoflurane postconditioning on focal ischemic brain i
PMID 24452205

BKCa channels expressed in sensory neurons modulate inflammatory pain in mice.

Lu R1, Lukowski R2, Sausbier M2, Zhang DD1, Sisignano M1, Schuh CD1, Kuner R3, Ruth P2, Geisslinger G1, Schmidtko A4.Author information 1Pharmazentrum Frankfurt/ZAFES, Institut für Klinische Pharmakologie, Klinikum der Johann Wolfgang Goethe-Universität, Frankfurt am Main, Germany.2Pharmakologie, Toxikologie und Klinische Pharmazie, Institut für Pharmazie, Tübingen, Germany.3Pharmakologisches Institut, Universität Heidelberg, Heidelberg, Germany.4Pharmazentrum Frankfurt/ZAFES, Institut für Klinische Pharmakologie, Klinikum der Johann Wolfgang Goethe-Universität, Frankfurt am Main, Germany. Electronic address: achim.schmidtko@uni-wh.de.AbstractLarge conductance calcium-activated potassium (BKCa) channels are important regulators of neuronal excitability. Although there is electrophysiological evidence for BKCa channel expression in sensory neurons, their in vivo functions in pain processing have not been fully defined. Using a specific antibody, we demonstrate here that BKCa channels are expressed in subpopulations of peptidergic and nonpeptidergic nociceptors. To test a functional association of BKCa channel activity in sensory neurons with particular pain modalities, we generated mice in which BKCa channels are ablated specifically from sensory neurons and analyzed their behavior in various models of pain. Mutant mice showed increased nociceptive behavior in models of persistent inflammatory pain. However, their behavior in models of neuropathic or acute nociceptive pain was normal. Moreover, systemic administration of the BKCa channel opener, NS1619, inhibited persistent inflammatory pain. Our investigations provide in vivo evidence that BKCa channels expressed in sensory neurons exert inhibitory control on sensory input in inflammatory pain states.
Pain.Pain.2014 Mar;155(3):556-65. doi: 10.1016/j.pain.2013.12.005. Epub 2013 Dec 11.
Large conductance calcium-activated potassium (BKCa) channels are important regulators of neuronal excitability. Although there is electrophysiological evidence for BKCa channel expression in sensory neurons, their in vivo functions in pain processing have not been fully defined. Using a specific an
PMID 24333777