WGA-coated yttrium oxide beads enable an imaging-based adenosine 2a receptor binding scintillation proximity assay suitable for high throughput screening

Assay and Drug Development Technologies

Volumn 2, Issue 3, 2004, Pages 290-299

  Bryant, Robert ^a,c   McGuinness, Debra ^a   Turek Etienne, Tammy ^a   Guyer, Deborah ^b   Yu, Liming ^b   Howells, Leighton ^b   Caravano, Joseph ^a,d   Zhai, Ying ^a   Lachowicz, Jean ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Amersham Biosciences   (United States)

^c Linguagen Corp   (United States)

^d UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,3 DIETHYL 8 PHENYLXANTHINE; 1,3 DIPROPYL 8 (4 SULFOPHENYL)XANTHINE; 2 ANILINOADENOSINE; 5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; 8 (3 CHLOROSTYRYL)CAFFEINE; 8 CYCLOPENTYL 1,3 DIPROPYLXANTHINE; 8 CYCLOPENTYLTHEOPHYLLINE; 8 [4 (2 AMINOETHYLCARBAMOYL)METHOXYPHENYL] 1,3 DIPROPYLXANTHINE; 9 CHLORO 2 (2 FURYL) 5,6 DIHYDRO 5 IMINO 1,2,4 TRIAZOLO[2,3 C]QUINAZOLINE; ADENOSINE 5' (N CYCLOPROPYLCARBOXAMIDE); ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A2A RECEPTOR; ADENOSINE A2A RECEPTOR AGONIST; ADENOSINE A2A RECEPTOR ANTAGONIST; ADENOSINE RECEPTOR; DIADENOSINE TETRAPHOSPHATE; DIMETHYL SULFOXIDE; G PROTEIN COUPLED RECEPTOR; ISOPRENALINE; N METHYLHISTAMINE; PHENYLBUTAZONE; POLYVINYL DERIVATIVE; RADIOLIGAND; TETRACAINE; TOLUENE DERIVATIVE; TRACAZOLATE; TRITIUM; UNINDEXED DRUG; WHEAT GERM AGGLUTININ; YTTRIUM;

ARTICLE; AUTOMATION; BINDING ASSAY; CELL LINE; CELL MEMBRANE; CONTROLLED STUDY; DRUG STRUCTURE; FILTRATION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; IMAGING SYSTEM; INTERMETHOD COMPARISON; LIGAND BINDING; MATERIAL COATING; PROTEIN FAMILY; RADIOASSAY; RECEPTOR BINDING; SCINTILLATION COUNTING; SIGNAL TRANSDUCTION;

EID: 4043121932     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/1540658041410713     Document Type: Article

References (17)

1. Dohlman HG, Caron MG, Lefkowitz RJ: Structure and function of the beta 2-adrenergic receptor - homology with rhodopsin. Kidney Int Suppl 1987;23:S2-S13.
2. Chern Y, King K, Lai HL, Lai HT: Molecular cloning of a novel adenosine receptor gene from rat brain. Biochem Biophys Res Commun 1992;185:304-309.
3. Fink JS, Weaver DR, Rivkees SA, Peterfreund RA, Pollack AE, Adler EM, Reppert SM: Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. Brain Res Mol Brain Res 1992;14:186-195.
4. Dixon AK, Gubitz AK, Sirinathsinghji DJ, Richardson PJ, Freeman TC: Tissue distribution of adenosine receptor mRNAs in the rat. Br J Pharmacol 1996;118:1461-1468.
5. Ledent C, Vaugeois JM, Schiffmann SN, Pedrazzini T, El Yacoubi M, Vanderhaeghen JJ, Costentin J, Heath JK, Vassart G, Parmentier M: Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2a receptor. Nature 1997;388:674-678.
6. Kanda T, Jackson MJ, Smith LA, Pearce RK, Nakamura J, Kase H, Kuwana Y, Jenner P: Adenosine A2A antagonist: a novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeys. Ann Neurol 1998;43:507-513.
7. Klotz KN: Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch Pharmacol 2000;362:382-391.
8. 3H]-SCH 58261. Br J Pharmacol 1997;121:353-360.
9. Turek-Etienne TC, Small EC, Soh SC, Xin TA, Gaitonde PV, Barrabee EB, Hart RF, Bryant RW: Evaluation of fluorescent compound interference in 4 fluorescence polarization assays: 2 kinases, 1 protease, and 1 phosphatase. J Biomol Screen 2003;8:176-184.
10. 2 receptor selective antagonist. Life Sci 1999;64:535-539.
11. Cook L, Pak R, Graves R, Cook J, Manly S, Padmanabha R: Benefits from using imaging based detection (LEADseeker) and red-shifted emission for radiometric proximity assay screening. Poster presented at the Society for Biomolecular Screening, 7th Annual Conference, Baltimore, MD, September 10-13, 2001.
12. Lowitz K, Prescott G, Guyer D, Dunst R: Comparison of human ghrelin receptor binding assays using SPA and the LEADseeker multimodality imaging system. Poster presented at the Society for Biomolecular Screening, 9th Annual Conference, Portland, OR, September 21-25, 2003.
13. 50) of an enzymatic reaction. Biochem Pharmacol 1973;22:413-424.
14. Liu J, Feldman PA, Lippy JS, Bobkova E, Kurilla MG, Chung TD: A scintillation proximity assay for rna detection. Anal Biochem 2001;289:239-245.
15. Gobel J, Saussy DL, Goetz AS: Development of scintillation-proximity assays for alpha adrenoceptors. J Pharmacol Toxicol Methods 1999;42:237-244.
16. Sorg G, Schubert HD, Buttner FH, Heilker R: Automated high throughput screening for serine kinase inhibitors using a LEADseeker scintillation proximity assay in the 1536-well format. J Biomol Screen 2002;7:11-19.
17. Friedman JE, Scott Bowes S, Serene J: Development of PVT SPA assays for adenosine receptors. Poster presented at the IBC 6th Annual Conference on Assay Development, San Diego, CA, October 16-18, 2002.