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Page 1
Showing results for class opener
Your search for clasp opener retrieved no results
The cis-Regulatory Atlas of the Mouse Immune System.
Yoshida H, Lareau CA, Ramirez RN, Rose SA, Maier B, Wroblewska A, Desland F, Chudnovskiy A, Mortha A, Dominguez C, Tellier J, Kim E, Dwyer D, Shinton S, Nabekura T, Qi Y, Yu B, Robinette M, Kim KW, Wagers A, Rhoads A, Nutt SL, Brown BD, Mostafavi S, Buenrostro JD, Benoist C; Immunological Genome Project. Yoshida H, et al. Cell. 2019 Feb 7;176(4):897-912.e20. doi: 10.1016/j.cell.2018.12.036. Epub 2019 Jan 24. Cell. 2019. PMID: 30686579 Free PMC article.
This breadth of data enable variance components analysis that suggests that genes fall into two distinct classes, controlled by either enhancer- or promoter-driven logic, and multiple regression that connects genes to the enhancers that regulate them. Relating transcriptio …
This breadth of data enable variance components analysis that suggests that genes fall into two distinct classes, controlled by eithe …
The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy.
Gunthorpe MJ, Large CH, Sankar R. Gunthorpe MJ, et al. Epilepsia. 2012 Mar;53(3):412-24. doi: 10.1111/j.1528-1167.2011.03365.x. Epub 2012 Jan 5. Epilepsia. 2012. PMID: 22220513 Free article. Review.
Its primary mechanism of action (MoA) as a positive allosteric modulator of KCNQ2-5 (K(v) 7.2-7.5) ion channels defines RTG/EZG as the first neuronal potassium (K(+)) channel opener for the treatment of epilepsy. KCNQ2-5 channels are predominantly expressed in neurons and …
Its primary mechanism of action (MoA) as a positive allosteric modulator of KCNQ2-5 (K(v) 7.2-7.5) ion channels defines RTG/EZG as the first …
Alternative Targets for Modulators of Mitochondrial Potassium Channels.
Wrzosek A, Gałecka S, Żochowska M, Olszewska A, Kulawiak B. Wrzosek A, et al. Molecules. 2022 Jan 4;27(1):299. doi: 10.3390/molecules27010299. Molecules. 2022. PMID: 35011530 Free PMC article. Review.
This may result in unexpected or unwanted effects induced by these compounds. In our review, we briefly present the various classes of mitochondrial potassium (mitoK) channels and describe the chemical compounds that modulate their activity. ...
This may result in unexpected or unwanted effects induced by these compounds. In our review, we briefly present the various classes o …
ATP sensitive potassium channel openers: A new class of ocular hypotensive agents.
Roy Chowdhury U, Dosa PI, Fautsch MP. Roy Chowdhury U, et al. Exp Eye Res. 2017 May;158:85-93. doi: 10.1016/j.exer.2016.04.020. Epub 2016 Apr 26. Exp Eye Res. 2017. PMID: 27130546 Free PMC article. Review.
Additionally, when used in conjunction with known intraocular pressure lowering drugs, an additive effect on IOP reduction was observed. These K(ATP) channel openers have also been reported to protect the retinal ganglion cells during ischemic stress and glutamate induced …
Additionally, when used in conjunction with known intraocular pressure lowering drugs, an additive effect on IOP reduction was observed. The …
New drugs for asthma.
Barnes PJ. Barnes PJ. Eur Respir J. 1992 Oct;5(9):1126-36. Eur Respir J. 1992. PMID: 1358672 Review.
Several new drugs are now under development for the treatment of asthma, either as improvements to existing classes of therapy or as novel agents. Amongst bronchodilators, long-acting inhaled beta 2-agonists (salmeterol and formoterol) look very promising and there is also …
Several new drugs are now under development for the treatment of asthma, either as improvements to existing classes of therapy or as …
KCNQ3 is the principal target of retigabine in CA1 and subicular excitatory neurons.
Varghese N, Lauritano A, Taglialatela M, Tzingounis AV. Varghese N, et al. J Neurophysiol. 2021 Apr 1;125(4):1440-1449. doi: 10.1152/jn.00564.2020. Epub 2021 Mar 17. J Neurophysiol. 2021. PMID: 33729829 Free PMC article.
Retigabine is a first-in-class potassium channel opener approved for patients with epilepsy. ...Our work provides new insight into the action of retigabine in forebrain neurons, clarifying retigabine's action in the nervous system.NEW & NOTEWORTHY Retigabine has …
Retigabine is a first-in-class potassium channel opener approved for patients with epilepsy. ...Our work provides new insight …
Pharmacologic profile of the selective mitochondrial-K(ATP) opener BMS-191095 for treatment of acute myocardial ischemia.
Grover GJ, Atwal KS. Grover GJ, et al. Cardiovasc Drug Rev. 2002 Summer;20(2):121-36. doi: 10.1111/j.1527-3466.2002.tb00187.x. Cardiovasc Drug Rev. 2002. PMID: 12177690 Review.
ATP-sensitive potassium channel (K(ATP)) openers as a class protect ischemic myocardium. The protective effects are independent of vasodilator activity and effects on action potential shortening, actions typically associated with sarcolemmal K(ATP) activation. BMS-1 …
ATP-sensitive potassium channel (K(ATP)) openers as a class protect ischemic myocardium. The protective effects are independen …
New Insights on KCa3.1 Channel Modulation.
Manfroni G, Ragonese F, Monarca L, Astolfi A, Mancinelli L, Iannitti RG, Bastioli F, Barreca ML, Cecchetti V, Fioretti B. Manfroni G, et al. Curr Pharm Des. 2020;26(18):2096-2101. doi: 10.2174/1381612826666200316152645. Curr Pharm Des. 2020. PMID: 32175839
The KCa3.1 channel has a very rich pharmacological profile with several classes of molecules that selectively interact with different binding sites of the channel. Among them, benzo imidazolones can be openers (positive modulators such as 1-EBIO, DC-EBIO) or blocker …
The KCa3.1 channel has a very rich pharmacological profile with several classes of molecules that selectively interact with different …
A profile of azetukalner for the treatment of epilepsy: from pharmacology to potential for therapy.
Lattanzi S, Trinka E, Meletti S, Striano P, Matricardi S, Silvestrini M, Brigo F. Lattanzi S, et al. Expert Rev Clin Pharmacol. 2024 Apr 3:1-10. doi: 10.1080/17512433.2024.2337012. Online ahead of print. Expert Rev Clin Pharmacol. 2024. PMID: 38571335 Review.
AREAS COVERED: A literature review on the pharmacology, efficacy, tolerability, and safety of azetukalner (XEN1101), a second-generation opener of neuronal potassium channels currently in Phase 3 development as ASM. ...Structurally distinct from currently marketed ASMs, az …
AREAS COVERED: A literature review on the pharmacology, efficacy, tolerability, and safety of azetukalner (XEN1101), a second-generation …
The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles.
Turner SC, Carroll WA, White TK, Gopalakrishnan M, Coghlan MJ, Shieh CC, Zhang XF, Parihar AS, Buckner SA, Milicic I, Sullivan JP. Turner SC, et al. Bioorg Med Chem Lett. 2003 Jun 16;13(12):2003-7. doi: 10.1016/s0960-894x(03)00324-x. Bioorg Med Chem Lett. 2003. PMID: 12781183
2-Amino-4-azaindoles have been identified as a structurally novel class of BK(Ca) channel openers. Their synthesis from 2-chloro-3-nitropyridine is described together with their in vitro properties assessed by 86Rb(+) efflux and whole-cell patch-clamp assays using H …
2-Amino-4-azaindoles have been identified as a structurally novel class of BK(Ca) channel openers. Their synthesis from 2-chlo …
232 results