A robust homogeneous binding assay for α4β2 nicotinic acetylcholine receptor

Acta Pharmacologica Sinica

Volumn 26, Issue 10, 2005, Pages 1175-1180

  Hui, Xin ^a   Gao, Jie ^a   Xie, Xin ^a   Suto, Naoki ^b   Ogiku, Tsuyoshi ^b   Wang, Ming Wei ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

Author keywords

High throughput screening; Nicotinic acetylcholine receptor; Scintillation proximity assay

Indexed keywords

5 (2 AZETIDINYLMETHOXY) 2 CHLOROPYRIDINE; CALCIUM; CYSTEINE; EPIBATIDINE; ION CHANNEL; MEMBRANE RECEPTOR; N METHYL 4 (3 PYRIDINYL) 3 BUTENAMINE; NC 00074281; NC 00077510; NC 00077640; NC 00078111; NC 00078246; NC 00085558; NC 00085845; NC 00088249; NC 00088584; NC 00090476; NC 00095121; NC 00095315; NC 00096768; NC 00097744; NC 00098179; NC 00102353; NICOTINIC AGENT; NICOTINIC RECEPTOR; NICOTINIC RECEPTOR ALPHA4BETA2; UNCLASSIFIED DRUG; WHEAT GERM AGGLUTININ;

ARTICLE; ASSAY; AUTOMATION; BIOTECHNOLOGY; CALCIUM CELL LEVEL; CALCIUM MOBILIZATION; CELL MEMBRANE; CELL STRAIN HEK293; CONTROLLED STUDY; DRUG RECEPTOR BINDING; EMBRYO; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; NUCLEOTIDE SEQUENCE; PROTEIN EXPRESSION; SCINTILLATION;

ALKALOIDS; AZETIDINES; AZOCINES; BICYCLO COMPOUNDS, HETEROCYCLIC; CALCIUM; CELL LINE; DRUG EVALUATION, PRECLINICAL; EMBRYO; EMBRYO, MAMMALIAN; HUMANS; KIDNEY; NICOTINE; NICOTINIC AGONISTS; NICOTINIC ANTAGONISTS; PROTEIN BINDING; PYRIDINES; QUINOLIZINES; RECEPTORS, NICOTINIC; SCINTILLATION COUNTING;

EID: 26044480949     PISSN: 16714083     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1745-7254.2005.00202.x     Document Type: Article

References (17)

1. Lukas RJ, Changeux JP, Novere N, Albuquerque EX, Balfour DJ, Berg DK, et al. International Union of Pharmacology. XX. Current status of the nomenclature for nicotinic acetylcholine receptors and their subunits. Pharmacol Rev 1999; 51: 397-401.
2. Albuquerque EX, Alkondon M, Pereira EF, Castro NG, Schrattenholz A, Barbosa CT, et al. Properties of neuronal nicotinic acetylcholine receptors: pharmacological characterization and modulation of synaptic function. J Pharmacol Exp Ther 1997; 280: 1117-36.
3. Cordero-Erausquin M, Marubio LM, Klink R, Changeux JP. Nicotinic receptor function: new perspectives from knockout mice. Trends Pharmacol Sci 2000; 21: 211-7.
4. Kesingland AC, Gentry CT, Panesar MS, Bowes MA, Vernier JM, Cube R, et al. Analgesic profile of the nicotinic acetylcholine receptor agonists, (+)-epibatidine and ABT-594 in models of persistent inflammatory and neuropathic pain. Pain 2000; 86: 113-8.
5. Boyce S, Webb JK, Shepheard SL, Russell MG, Hill RG, Rupniak NM. Analgesic and toxic effects of ABT-594 resemble epibatidine and nicotine in rats. Pain 2000; 85: 443-50.
6. Carpenter JW, Laethem C, Hubbard FR, Eckols TK, Baez M, McClure D, et al. Configuring radioligand receptor binding assays for HTS using scintillation proximity assay technology. Methods Mol Biol 2002; 190: 31-49.
7. Chavez-Noriega LE, Gillespie A, Stauderman KA, Crona JH, Claeps BO, Elliott KJ, et al. Characterization of the recombinant human neuronal nicotinic acetylcholine receptors α3β2 and α4β2 stably expressed in HEK293 cells. Neuropharmacology 2000; 39: 2543-60.
8. Donnelly-Roberts DL, Puttfarcken PS, Kuntzweiler TA, Briggs CA, Anderson DJ, Campbell JE, et al. ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: In vitro characterization. J Pharmacol Exp Ther 1998; 285: 777-86.
9. Qian J, Voorbach MJ, Huth JR, Coen ML, Zhang HC, Ng SC, et al. Discovery of novel inhibitors of Bcl-xL using multiple high-throughput screening platforms. Anal Biochem 2004; 328: 131-8.
10. 50) of an enzymatic reaction. Biochem Pharmacol 1973; 22: 3099-108.
11. Khan IM, Yaksh TL, Taylor P. Ligand specificity of nicotinic acetylcholine receptors in rat spinal cord: studies with nicotine and cytisine. J Pharmacol Exp Ther 1994; 270: 159-66.
12. Wu B, Gao J, Wang M-W. Development of a complex scintillation proximity assay for high-throughput screening of PPARγ modulators. Acta Pharmacol Sin 2005; 26: 339-44.
13. Crane K, Shin DT. Development of a homogeneous binding assay for histamine receptors. Anal Biochem 2004; 335: 42-9.
14. Gobel J, Saussy DL, Goetz AS. Development of scintillation-proximity assays for alpha adrenoceptors. J Pharmacol Toxicol Methods 1999; 42: 237-44.
15. Rodgers G, Hubert C, McKinzie J, Suter T, Statnick M, Emmerson P, et al. Development of displacement binding and GTPγS scintillation proximity assays for the identification of antagonists of the micro-opioid receptor. Assay Drug Dev Technol 2003; 1: 627-36.
16. Xiao Y, Baydyuk M, Wang HP, Davis HE, Kellar KJ. Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. Bioorg Med Chem Lett 2004; 14: 1845-8.
17. Zhang JH, Chung TD, Oldenburg KR. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999; 4: 67-73.