An offline-addition format for identifying GPCR modulators by screening 384-well mixed compounds in the FLIPR

Journal of Biomolecular Screening

Volumn 10, Issue 1, 2005, Pages 46-55

  Gopalakrishnan, Sujatha M ^a   Mammen, Betsy ^a   Schmidt, Martin ^b   Otterstaetter, Bernd ^b   Amberg, Willi ^b   Wernet, Wolfgang ^b   Kofron, James L ^a   Burns, David J ^a   Warrior, Usha ^a  

^a ABBOTT LABORATORIES   (United States)

^b ABBOTT GMBH AND CO KG   (Germany)

Author keywords

FLIPR; G protein coupled receptor; High throughput screening; Intracellular calcium release; Neurokinin

Indexed keywords

17ALPHA ETHYNYL 17BETA HYDROXY 5ALPHA ANDROSTANO[3,2 B]PYRIMIDO[1,2 A]BENZIMIDAZOLE; 17BETA HYDROXY 17ALPHA ETHYNYL DELTA4 ANDROSTANO[3,2 B]PYRIMIDO[1,2 A]BENZIMIDAZOLE; 2 BENZHYDRYL 3 (2 IODOBENZYLAMINO)QUINUCLIDINE; 3 [3,5 BIS(TRIFLUOROMETHYL)BENZYLOXY] 2 PHENYLPIPERIDINE; G PROTEIN COUPLED RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; SUBSTANCE P; UNCLASSIFIED DRUG; WIN 62577;

ANALYTIC METHOD; ARTICLE; ASTROCYTOMA; CALCIUM CELL LEVEL; FLUORESCENCE IMAGING PLATE READER; HIGH THROUGHPUT SCREENING; PRIORITY JOURNAL;

CELL LINE, TUMOR; DRUG EVALUATION, PRECLINICAL; FLUORESCENT DYES; HUMANS; INHIBITORY CONCENTRATION 50; KINETICS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NEUROKININ-1;

EID: 17044423277     PISSN: 10870571     EISSN: None     Source Type: Journal    
DOI: 10.1177/1087057104270017     Document Type: Article

References (15)

1. Schroeder KS, Neagle BD: FLIPR: a new instrument for accurate, high throughput optical screening. J Biomol Screen 1996;1:75-80.
2. Krahn T, Paffhausen W, Andreas S, Bechem M, Schmidt D: Masking background fluorescence and luminescence in optical analysis of biomedical assays. US Patent 1998;6, 420.
3. Humphrey JM: Medicinal chemistry of selective neurokinin-1 antagonists. Curr Top Med Chem 2003;3:1423-1435.
4. Kawaja AM, Rogers DF: Tachykinins to effector. J Biochem Cell Bio 1996;28:721-738.
5. Cascieri MA, Ber E, Fong TM, et al: Characterization of the binding of a potent, selective, radioiodinated antagonist to the human neurokinin-1 receptor. Mol Pharmacol 1992;42:458-463.
6. 50) of an enzymatic reaction. Biochem Pharmacol 1973;22:3099-3108.
7. Craig D: The Cheng-Prusoff relationship: something lost in the translation. Trends Pharmacol Sci 1993;14:89-91.
8. 2+]I mobilization, cardiovascular and dural extravasation assays. Eur J Pharmacol 1996;317:129-135.
9. Parsons AM, el-Fakahany EE, Seybold VS: Tachykinins alter inositol phosphate formation, but not cyclic AMP levels, in primary cultures of neonatal rat spinal neurons through activation of neurokinin receptors. Neuroscience 1995;68:855-865.
10. Sachais BS, Krause JE: Both extracellular and transmembrane residues contribute to the species selectivity of the neurokinin-1 receptor antagonist WIN 51708. Mol Pharmacol 1994;46:122-128.
11. Appell KC, Fragale BJ, Loscig J, Singh S, Tomczuk BE: Antagonists that demonstrate species differences in neurokinin-1 receptors. Mol Pharmacol 1992;41:772-775.
12. Hann M, Hudson B, Lewell X, Lifely R, Miller L, Ramsden N: Strategic pooling of compounds for high-throughput screening. J Chem Inf Comput Sci 1999;39:897-902.
13. Hodder P, Cassaday J, Peltier R, et al: Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system. Anal Biochem 2003;313:246-254.
14. Garland AM, Grady EF, Lovett M, et al: Mechanisms of desensitization and resensitization of G protein-coupled neurokinin 1 and neurokinin 2 receptors. Mol Pharmacol 1996;438:46.
15. Hedley L, Phagoo SB, James IF: Measurement of intracellular calcium in cell populations loaded with aequorin: neurokinin-1 responses in U373MG cells. Anal Biochem 1996;236:270-274.