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Automated planar electrode electrophysiology in drug discovery: examples of the use of QPatch in basic characterization and high content screening on Na(v), K(Ca)2.3, and K(v)11.1 channels.
Korsgaard MP, Strøbaek D, Christophersen P. Korsgaard MP, et al. Comb Chem High Throughput Screen. 2009 Jan;12(1):51-63. doi: 10.2174/138620709787048037. Comb Chem High Throughput Screen. 2009. PMID: 19149491 Review.
Kv7 channels as targets for anti-epileptic and psychiatric drug-development.
Grunnet M, Strøbæk D, Hougaard C, Christophersen P. Grunnet M, et al. Among authors: strobaek d. Eur J Pharmacol. 2014 Mar 5;726:133-7. doi: 10.1016/j.ejphar.2014.01.017. Epub 2014 Jan 20. Eur J Pharmacol. 2014. PMID: 24457124 Review.
Characterization of a novel high-potency positive modulator of K(v)7 channels.
Dalby-Brown W, Jessen C, Hougaard C, Jensen ML, Jacobsen TA, Nielsen KS, Erichsen HK, Grunnet M, Ahring PK, Christophersen P, Strøbæk D, Jørgensen S. Dalby-Brown W, et al. Among authors: strobaek d. Eur J Pharmacol. 2013 Jun 5;709(1-3):52-63. doi: 10.1016/j.ejphar.2013.03.039. Epub 2013 Apr 3. Eur J Pharmacol. 2013. PMID: 23562623
Evidence for a common pharmacological interaction site on K(Ca)2 channels providing both selective activation and selective inhibition of the human K(Ca)2.1 subtype.
Hougaard C, Hammami S, Eriksen BL, Sørensen US, Jensen ML, Strøbæk D, Christophersen P. Hougaard C, et al. Mol Pharmacol. 2012 Feb;81(2):210-9. doi: 10.1124/mol.111.074252. Epub 2011 Nov 1. Mol Pharmacol. 2012. PMID: 22046005
Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons.
Strøbaek D, Hougaard C, Johansen TH, Sørensen US, Nielsen EØ, Nielsen KS, Taylor RD, Pedarzani P, Christophersen P. Strøbaek D, et al. Mol Pharmacol. 2006 Nov;70(5):1771-82. doi: 10.1124/mol.106.027110. Epub 2006 Aug 22. Mol Pharmacol. 2006. PMID: 16926279
NS8593 inhibited all the SK1-3 subtypes Ca(2+)-dependently (K(d) = 0.42, 0.60, and 0.73 microM, respectively, at 0.5 microM Ca(2+)), whereas the compound did not affect the Ca(2+)-activated K(+) channels of intermediate and large conductance (hIK and hBK channels, respecti …
NS8593 inhibited all the SK1-3 subtypes Ca(2+)-dependently (K(d) = 0.42, 0.60, and 0.73 microM, respectively, at 0.5 microM Ca(2+)), …
NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
Nausch B, Rode F, Jørgensen S, Nardi A, Korsgaard MP, Hougaard C, Bonev AD, Brown WD, Dyhring T, Strøbæk D, Olesen SP, Christophersen P, Grunnet M, Nelson MT, Rønn LC. Nausch B, et al. Among authors: strobaek d. J Pharmacol Exp Ther. 2014 Sep;350(3):520-30. doi: 10.1124/jpet.113.212662. Epub 2014 Jun 20. J Pharmacol Exp Ther. 2014. PMID: 24951278 Free PMC article.
Biophysical and pharmacological characterization of α6-containing nicotinic acetylcholine receptors expressed in HEK293 cells.
Rasmussen AH, Strøbæk D, Dyhring T, Jensen ML, Peters D, Grunnet M, Timmermann DB, Ahring PK. Rasmussen AH, et al. Among authors: strobaek d. Brain Res. 2014 Jan 13;1542:1-11. doi: 10.1016/j.brainres.2013.10.024. Epub 2013 Oct 21. Brain Res. 2014. PMID: 24157862
A high-throughput screening campaign for detection of ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay.
Jørgensen S, Dyhring T, Brown DT, Strøbæk D, Christophersen P, Demnitz J. Jørgensen S, et al. Among authors: strobaek d. Assay Drug Dev Technol. 2013 Apr;11(3):163-72. doi: 10.1089/adt.2012.479. Epub 2012 Nov 30. Assay Drug Dev Technol. 2013. PMID: 23198866
Selective activation of the SK1 subtype of human small-conductance Ca2+-activated K+ channels by 4-(2-methoxyphenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester (GW542573X) is dependent on serine 293 in the S5 segment.
Hougaard C, Jensen ML, Dale TJ, Miller DD, Davies DJ, Eriksen BL, Strøbaek D, Trezise DJ, Christophersen P. Hougaard C, et al. Mol Pharmacol. 2009 Sep;76(3):569-78. doi: 10.1124/mol.109.056663. Epub 2009 Jun 10. Mol Pharmacol. 2009. PMID: 19515965
Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators ofsmall conductance Ca2+-activated K+ channels.
Sørensen US, Strøbaek D, Christophersen P, Hougaard C, Jensen ML, Nielsen EØ, Peters D, Teuber L. Sørensen US, et al. J Med Chem. 2008 Dec 11;51(23):7625-34. doi: 10.1021/jm800809f. J Med Chem. 2008. PMID: 18998663
The first described compound in this class is NS8593 (14), and the most potent analogue identified in this study is the racemic compound 39 (NS11757), which reversibly inhibits SK3-mediated currents with a K(d) value of 9 nM....
The first described compound in this class is NS8593 (14), and the most potent analogue identified in this study is the racemic compound 39 …
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