ωコノトキシン
- 関
- omega-CgTX
WordNet
- the ending of a series or sequence; "the Alpha and the Omega, the first and the last, the beginning and the end"--Revelation (同)Z
- the last (24th) letter of the Greek alphabet
PrepTutorEJDIC
- 〈C〉オメガ(ギリシャ語アルアァベット24文字の最後の字Ω,ω;英語のO,oの長音に相当) / 〈U〉(一連のものの)最後,終り(end)
UpToDate Contents
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English Journal
- Challenging the catechism of therapeutics for chronic neuropathic pain: Targeting CaV2.2 interactions with CRMP2 peptides.
- Feldman P, Khanna R.Author information Sophia Therapeutics LLC, 351 West 10th Street, Indianapolis, IN 46202, USA.AbstractChronic neuropathic pain management is a worldwide concern. Pharmaceutical companies globally have historically targeted ion channels as the therapeutic catechism with many blockbuster successes. Remarkably, no new pain therapeutic has been approved by European or American regulatory agencies over the last decade. This article will provide an overview of an alternative approach to ion channel drug discovery: targeting regulators of ion channels, specifically focusing on voltage-gated calcium channels. We will highlight the discovery of an anti-nociceptive peptide derived from a novel calcium channel interacting partner - the collapsin response mediator protein 2 (CRMP2). In vivo administration of this peptide reduces pain behavior in a number of models of neuropathic pain without affecting sympathetic-associated cardiovascular activity, memory retrieval, sensorimotor function, or depression. A CRMP2-derived peptide analgesic, with restricted access to the CNS, represents a completely novel approach to the treatment of severe pain with an improved safety profile. As peptides now represent one of the fastest growing classes of new drugs, it is expected that peptide targeting of protein interactions within the calcium channel complex may be a paradigm shift in ion channel drug discovery.
- Neuroscience letters.Neurosci Lett.2013 Dec 17;557 Pt A:27-36. doi: 10.1016/j.neulet.2013.06.057. Epub 2013 Jul 3.
- Chronic neuropathic pain management is a worldwide concern. Pharmaceutical companies globally have historically targeted ion channels as the therapeutic catechism with many blockbuster successes. Remarkably, no new pain therapeutic has been approved by European or American regulatory agencies over t
- PMID 23831344
- Expression and motor functional roles of voltage-dependent type 7 K(+) channels in the human taenia coli.
- Adduci A, Martire M, Taglialatela M, Arena V, Rizzo G, Coco C, Currò D.Author information Institute of Pharmacology, School of Medicine, Catholic University of the Sacred Heart, L.go F. Vito 1, 00168 Rome, Italy.AbstractVoltage-dependent type 7 K(+) (KV7 or KCNQ) channels modulate the excitability of neurons and muscle cells. The aims of the present study were to investigate the motor effects of KV7 channel modulators and the expression of KV7 channels in the human taenia coli. The effects of KV7 channel modulators on the muscle tone of human taenia coli strips were investigated under nonadrenergic non-nitrergic conditions by organ bath studies. Gene expression and tissue localisation of channels were studied by real-time PCR and immunohistochemistry, respectively. Under basal conditions, the KV7 channel blocker XE-991 induced concentration-dependent contractions, with mean EC50 and Emax of 18.7μM and 30.5% respectively of the maximal bethanechol-induced contraction, respectively. The KV7 channel activators retigabine and flupirtine concentration-dependently relaxed the taenia coli, with mean EC50s of 19.2μM and 29.9μM, respectively. Retigabine also relaxed bethanechol-precontracted strips, with maximal relaxations of 79.2% of the bethanecol-induced precontraction. The motor effects induced by the KV7 channel modulators were not affected by tetrodotoxin or ω-conotoxin GVIA. XE-991 greatly reduced retigabine- and flupirtine-induced relaxations. Transcripts encoded by all KCNQ genes were detected in the taenia coli, with KCNQ4 showing the highest expression levels. KV7.4 channels were clearly visualised by immunohistochemistry in colonic epithelium, circular muscle layer and taenia coli. KV7 channels appear to contribute to the resting muscle tone of the human taenia coli. In addition, KV7 channel activators significantly relax the taenia coli. Thus, they could be useful therapeutic relaxant agents for colonic motor disorders.
- European journal of pharmacology.Eur J Pharmacol.2013 Dec 5;721(1-3):12-20. doi: 10.1016/j.ejphar.2013.09.061. Epub 2013 Oct 10.
- Voltage-dependent type 7 K(+) (KV7 or KCNQ) channels modulate the excitability of neurons and muscle cells. The aims of the present study were to investigate the motor effects of KV7 channel modulators and the expression of KV7 channels in the human taenia coli. The effects of KV7 channel modulators
- PMID 24120659
- Dominance of P/Q-type calcium channels in depolarization-induced presynaptic FM dye release in cultured hippocampal neurons.
- Nimmervoll B, Flucher BE, Obermair GJ.Author information Division of Physiology, Medical University Innsbruck, Fritz-Pregl-Str. 3, 6020 Innsbruck, Austria.AbstractNeurotransmitter release probability is related by high power to the local concentration of calcium in presynaptic terminals, which in turn is controlled by voltage-gated calcium channels. P/Q- and N-type channels trigger synaptic transmission in the majority of neurons of the central nervous system. However, whether and under which conditions both channel types act cooperatively or independently is still insufficiently understood. Previous studies suggested either a dominance of N- or P/Q-type channels, or a synergistic action of both channels, depending on the experimental paradigms. Thus, to provide insight into the properties of neurotransmitter release in cultured mouse hippocampal neurons, we used quantitative analysis of FM dye release from presynaptic boutons induced by high potassium membrane depolarization. Increasing extracellular potassium concentrations revealed a sigmoid dependence of FM dye release to the stimulation strength. Individual and combined application of the P/Q- and N-type channel-specific blockers ω-agatoxin-IVA and ω-conotoxin-GVIA, respectively, allowed us to specifically isolate the contribution of both channel types to release triggered with 40 mM KCl. Analysis of the release kinetics and the fractional release amplitude demonstrate that, whereas in only 15% of the synapses release depended exclusively on P/Q-type channels, the majority of synapses (85%) contained both N- and P/Q-type channels. Nevertheless, the kinetics of FM dye release in synapses containing both channel types was determined by the P/Q-type channels. Together, our data suggest a more direct coupling of P/Q-type channels to synaptic release compared to N-type channels, which may explain the high prevalence of neurological P/Q-type channelopathies.
- Neuroscience.Neuroscience.2013 Dec 3;253:330-40. doi: 10.1016/j.neuroscience.2013.08.052. Epub 2013 Sep 5.
- Neurotransmitter release probability is related by high power to the local concentration of calcium in presynaptic terminals, which in turn is controlled by voltage-gated calcium channels. P/Q- and N-type channels trigger synaptic transmission in the majority of neurons of the central nervous system
- PMID 24012836
Japanese Journal
- Vasodilatory Effect of Cilnidipine, an L-type and N-type Calcium Channel Blocker, on Rat Kidney Glomerular Arterioles
- Konno Yuusuke,Kimura Kenjiro
- International Heart Journal 49(6), 723-732, 2008
- … This efferent arteriolar dilating action of cilnidipine was abolished after pretreatment with ω-conotoxin, a selective N-type calcium channel blocker. …
- NAID 130000069124
- Characterization of intracellular free Ca2+ movements in neural progenitor cells derived from ES cells transfected with MASH 1 transcription factor gene
- IDE Michiko,UEDA Yuji,WATANABE Kenji,S. KUROKAWA Manae,YOSHIKAWA Hideshi,SAKAIBARA Manabu,HASHIMOTO Takuo,SUZUKI Noboru
- 炎症・再生 : 日本炎症・再生医学会雑誌 = Inflammation and regeneration 25(5), 452-460, 2005-09-25
- … A L-type channel inhibitor, nifedipine, but not a N-type channel inhibitor, omega-conotoxin GVIA, reduced the increase of fluorescence intensity upon depolarization. …
- NAID 10026499202
Related Links
- Omega, delta and kappa families of conotoxins have a knottin or inhibitor cysteine knot scaffold. The knottin scaffold is a very special disulfide-through- disulfide knot, in which the III-VI ...
Related Pictures
★リンクテーブル★
[★]
- 英
- omega-conotoxin、omega-CgTX
- 関
- ωコノトキシン、ω-コノトキシンGVIA
[★]
- 関
- omega-CgTX GVIA、omega-conotoxin、omega-conotoxin GVIA
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- 英
- omega-conotoxin、omega-CgTX
- 関
- ω-コノトキシン
[★]
ωコノトキシンGVIA
- 関
- omega-CgTX、omega-CgTX GVIA
[★]
ωコノトキシンMVIIA
- 関
- ziconotide
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コノトキシン
- 関
- alpha-conotoxin、conopeptide
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ω、オメガ