Development and validation of a secondary screening assay for TRPM8 antagonists using QPatch HT

Assay and Drug Development Technologies

Volumn 8, Issue 1, 2010, Pages 63-72

  Beck, Edward J ^a   Hutchinson, Tasha L ^a   Qin, Ning ^a   Flores, Christopher M ^a   Liu, Yi ^a  

^a LLC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMICAL COMPOUND; ION CHANNEL; MENTHOL; TRANSIENT RECEPTOR POTENTIAL CHANNEL M; TRANSIENT RECEPTOR POTENTIAL CHANNEL M 8 ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BIOASSAY; CONTROLLED STUDY; ELECTROPHYSIOLOGY; HUMAN; HUMAN CELL; INHIBITION KINETICS; NONHUMAN; PATCH CLAMP; QPATCH HT; SCREENING; STEADY STATE; VALIDATION PROCESS;

CELLS, CULTURED; DRUG EVALUATION, PRECLINICAL; HUMANS; PATCH-CLAMP TECHNIQUES; TRPM CATION CHANNELS;

EID: 77649174506     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2009.0214     Document Type: Article

References (14)

1. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ: Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 1981;391:85-100.
2. Dunlop J, Bowlby M, Peri R, Vasilyev D, Arias R: High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiology. Nat Rev Drug Discov 2008;7:358-368.
3. Mathes C: QPatch: the past, present and future of automated patch clamp. Expert Opin Ther Targets 2006;10:319-327.
4. Korsgaard MP, Strøbaek D, Christophersen P: 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. Comb Chem High Throughput Screen 2009;12:51-63.
5. Kutchinsky J, Friis S, Asmild M, Taboryski R, Pedersen S, Vestergaard RK, et al.: Characterization of potassium channel modulators with QPatch automated patch-clamp technology: system characteristics and performance. Assay Drug Dev Technol 2003;1:685-693.
6. Schrøder RL, Friis S, Sunesen M, Mathes C, Willumsen NJ: Automated patchclamp technique: increased throughput in functional characterization and in pharmacological screening of small-conductance Ca2+ release-activated Ca2+ channels. J Biomol Screen 2008;13:638-647.
7. Friis S, Mathes C, Sunesen M, Bowlby MR, Dunlop J: Characterization of compounds on nicotinic acetylcholine receptor alpha7 channels using higher throughput electrophysiology. J Neurosci Methods 2009;177:142-148.
8. Mathes C, Friis S, Finley M, Liu Y: QPatch: the missing link between HTS and ion channel drug discovery. Comb Chem High Throughput Screen 2009;12: 78-95.
9. Colburn RW, Lubin ML, Stone DJ, Jr, Wang Y, Lawrence D, D'Andrea MR, et al.: Attenuated cold sensitivity in TRPM8 null mice. Neuron 2007;54:379-386.
10. Liu Y, Lubin ML, Reitz TL, Wang Y, Colburn RW, Flores CM, et al.: Molecular identification and functional characterization of a temperature-sensitive transient receptor potential channel (TRPM8) from canine. Eur J Pharmacol 2006;530:23-32.
11. Behrendt HJ, Germann T, Gillen C, Hatt H, Jostock R: Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br J Pharmacol 2004;141:737-745.
12. Weil A, Moore SE, Waite NJ, Randall A, Gunthorpe MJ: Conservation of functional and pharmacological properties in the distantly related temperature sensors TRVP1 and TRPM8. Mol Pharmacol 2005;68:518-527.
13. Mälkiä A, Madrid R, Meseguer V, de la Peña E, Valero M, Belmonte C, et al.: Bidirectional shifts of TRPM8 channel gating by temperature and chemical agents modulate the cold sensitivity of mammalian thermoreceptors. J Physiol (Lond) 2007;581:155-174.
14. Lampe T, Alonso-Alija C, Stelte-Ludwig B, Sandner P, Bauser M, Beck H, et al.: Substituted 4-benzyloxy-phenylmethylamide derivatives as cold menthol receptor-1 (CMR-1) antagonists for the treatment of urological disorder. 2006;WO2006040136 A1.