title: Ca2+ mobilization assays in GPCR drug discovery.
abstract: Intracellular calcium mobilization can be measured using several methods varying in indicator dyes and devices used. In this chapter, we describe the fluorescence-based method (FLIPR Calcium 4 Assay) developed by Molecular Devices for a FlexStation and routinely used in our laboratory for detecting intracellular calcium changes. The assay is designed to study calcium mobilization induced by majority of GPCRs and calcium channels and allows for simultaneous concentration-dependent analysis of several receptor agonists and antagonists, useful in receptor characterization and drug discovery projects.
authors.affiliation: Division of Asthma, Allergy and Lung Biology, King's College London, 5th Floor, Tower Wing, Guy's Hospital, London, SE1 9RT, UK, grzegorz.woszczek@kcl.ac.uk.
authors.forename: Grzegorz
authors.initials: G
authors.lastname: Woszczek
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Fuerst
mesh_terms: D001681:Biological Assay; D001920:Bradykinin / Q000494:pharmacology; D000001:Calcimycin / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism*; D061207:Calcium Ionophores / Q000494:pharmacology; D020013:Calcium Signaling; D055808:Drug Discovery; D005456:Fluorescent Dyes; D057166:High-Throughput Screening Assays; D006632:Histamine / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D008246:Lysophospholipids / Q000494:pharmacology; D032389:Myocytes, Smooth Muscle / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D061251:Primary Cell Culture; D011933:Reagent Kits, Diagnostic; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D012137:Respiratory System / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D013110:Sphingosine / Q000031:analogs & derivatives / Q000494:pharmacology
chemical_list: D061207:Calcium Ionophores; D005456:Fluorescent Dyes; D008246:Lysophospholipids; D011933:Reagent Kits, Diagnostic; D043562:Receptors, G-Protein-Coupled; C060506:sphingosine 1-phosphate; D000001:Calcimycin; D006632:Histamine; D013110:Sphingosine; D001920:Bradykinin; D002118:Calcium