Ion channels & transporters research and screening are areas that benefit the most from the FDSS kinetic plate imager’s high throughput feature. The FDSS can be equipped with 96-, 384- (FDSS/μCELL and FDSS-GX) and 1536- (FDSS-GX) manifold pipettors to add ligands / compounds into all wells simultaneously, and it images the whole plate so all wells are read at the same time, resulting in no time lag among wells while the reactions of cells occur. Ion channels are a class of transmembrane proteins that allow for certain ions to pass through the cell membrane (in and / or out of the cell). These proteins regulate cellular functions and are involved in the development of cardiovascular, neurologic, and metabolic disease solutions. Applications (and accompanying resources) include:
|Kawamoto T, Kimura H, Kusumoto K, Fukumoto S, Shiraishi M, Watanabe T, Sawada H.||Potent and selective inhibition of the human Na+/H+ exchanger isoform NHE1 by a novel aminoguanidine derivative T-162559||Eur J Pharmacol. 2001 May 18;420(1):1-8.|
|McNamara CR, Mandel-Brehm J, Bautista DM, Siemens J, Deranian KL, Zhao M, Hayward NJ, Chong JA, Julius D, Moran MM, Fanger CM.||TRPA1 mediates formalin-induced pain||Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13525-30. Epub 2007 Aug 8.|
|Ayala JE, Niswender CM, Luo Q, Banko JL, Conn PJ.||Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated||Neuropharmacology. 2008 Apr;54(5):804-14. Epub 2007 Dec 24.|
|Niswender CM, Johnson KA, Luo Q, Ayala JE, Kim C, Conn PJ, Weaver CD.||A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors||Mol Pharmacol. 2008 Apr;73(4):1213-24. Epub 2008 Jan 2.|
|Kobayashi K, Nishizawa Y, Sawada K, Ogura H, Miyabe M.||K(+)-channel openers suppress epileptiform activities induced by 4-aminopyridine in cultured rat hippocampal neurons||J Pharmacol Sci. 2008 Dec;108(4):517-28. Epub 2008 Dec 11.|
|Delpire E, Days E, Lewis LM, Mi D, Kim K, Lindsley CW, Weaver CD.||Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2||Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5383-8. Epub 2009 Mar 11.|
|Kim Y, Kang S, Lee JY, Rhim H.||High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1||Mol Pharmacol. 2009 Nov;76(5):1094-103. Epub 2009 Aug 25.|
|Kim Y, Kang S, Lee JY, Rhim H.||High throughput screening assay of alpha(1G) T-type Ca2+ channels and comparison with patch-clamp studies||Comb Chem High Throughput Screen. 2009 Mar;12(3):296-302.|
|Titus SA, Beacham D, Shahane SA, Southall N, Xia M, Huang R, Hooten E, Zhao Y, Shou L, Austin CP, Zheng W.||A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel||Anal Biochem. 2009 Nov 1;394(1):30-8. Epub 2009 Jul 5.|
|Jinliang Sui, Shakira Cotard, Jennifer Andersen, Ping Zhu, Jane Staunton, Margaret Lee, and Stephen Lin||Optimization of a Yellow Fluorescent Protein-Based Iodide Influx High-Throughput Screening Assay for Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Modulators||ASSAY and Drug Development Technologies. December 2010, 8(6): 656-668. doi:10.1089/adt.2010.0312.|
|C. David Weaver||Triple-Addition Assay Protocols for Detecting and Characterizing Modulators of Seven-Transmembrane Receptors||Current Protocols in Chemical Biology. 3:119–140.|
|App. Note N°.||Title|
|FDSS Application Note N°. 16||FDSS Application Note No.16 FluxORTM Differentially Identifies K+ Channel Antagonists Using FDSS6000 [0.1MB/PDF]|
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