Immobilized nicotinic receptor stationary phases: going with the flow in high-throughput screening and pharmacological studies

被引:40
作者
Moaddel, R [1 ]
Wainer, IW [1 ]
机构
[1] NIA, Gerontol Res Ctr, NIH, Baltimore, MD 21224 USA
关键词
nicotinic agonists; nicotinic antagonists; non-competitive inhibitors; affinity chromatography; immobilized receptors;
D O I
10.1016/S0731-7085(02)00513-7
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
The nicotinic acetylcholine receptor (nAChR) subtypes alpha3beta4-nAChR and alpha4beta2-nAChR have been immobilized and the resulting stationary phases used to determine binding affinities. The alpha3beta4-nAUR column was coupled to a C-18 column and a mixture of 18 compounds was sorted into ligands and non-ligands for the alpha3beta4-nAUR. The results demonstrate that the nAChR stationary phases can be used for on-line high-throughput screening (HTS). Published by Elsevier Science B.V.
引用
收藏
页码:1715 / 1724
页数:10
相关论文
共 22 条
[1]   Multidimensional on-line screening for ligands to the α3β4 neuronal nicotinic acetylcholine receptor using an immobilized nicotinic receptor liquid chromatographic stationary phase [J].
Baynham, MT ;
Patel, S ;
Moaddel, R ;
Wainer, IW .
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 2002, 772 (01) :155-161
[2]   Development of an immobilized brain glutamine synthetase liquid chromatographic stationary phase for on-line biochemical studies [J].
Cloix, JF ;
Wainer, IW .
JOURNAL OF CHROMATOGRAPHY A, 2001, 913 (1-2) :133-140
[3]   In vitro enzyme evolution:: the screening challenge of isolating the one in a million [J].
Cohen, N ;
Abramov, S ;
Dror, Y ;
Freeman, A .
TRENDS IN BIOTECHNOLOGY, 2001, 19 (12) :507-510
[4]  
Fryer JD, 1999, J PHARMACOL EXP THER, V288, P88
[5]   High-performance affinity chromatography and immobilized serum albumin as probes for drug- and hormone-protein binding [J].
Hage, DS ;
Austin, J .
JOURNAL OF CHROMATOGRAPHY B, 2000, 739 (01) :39-54
[6]  
Hernandez SC, 2000, J PHARMACOL EXP THER, V293, P962
[7]   Neuronal nicotinic acetylcholine receptors as targets for drug discovery [J].
Holladay, MW ;
Dart, MJ ;
Lynch, JK .
JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (26) :4169-4194
[8]   The emerging three-dimensional structure of a receptor - The nicotinic acetylcholine receptor [J].
Hucho, F ;
Tsetlin, VI ;
Machold, J .
EUROPEAN JOURNAL OF BIOCHEMISTRY, 1996, 239 (03) :539-557
[9]  
KALISZAN R, 1997, CHROMATOGRAPHIC SEPA, P273
[10]  
Lloyd GK, 2000, J PHARMACOL EXP THER, V292, P461