Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors

被引：90
作者：
Strange, Philip G. [1 ]
机构：
[1] Univ Reading, Sch Pharm, Reading RG6 6UB, Berks, England
来源：
BRITISH JOURNAL OF PHARMACOLOGY | 2010年 / 161卷 / 06期
基金：
英国生物技术与生命科学研究理事会; 英国惠康基金;
关键词：
agonist; antagonist; inverse agonist; functional assay; GTP gamma S binding assay; efficacy; drug screening; SCINTILLATION PROXIMITY ASSAY; UNDERLYING AGONIST EFFICACY; HUMAN DOPAMINE-D-2 RECEPTOR; M-3 MUSCARINIC RECEPTORS; PHARMACOLOGICAL CHARACTERIZATION; CHO-CELLS; INVERSE AGONIST; RAT THALAMUS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); GUANINE-NUCLEOTIDES;
D O I：
10.1111/j.1476-5381.2010.00963.x
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
LINKED ARTICLES This article is part of a themed section on Analytical Receptor Pharmacology in Drug Discovery. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2010.161.issue-6.
引用
收藏
页码：1238 / 1249
页数：12
相关论文
共 74 条
  • [71] TIAN WN, 1994, MOL PHARMACOL, V45, P524
  • [72] ANALYSIS OF RECEPTOR-G PROTEIN INTERACTIONS IN PERMEABILIZED CELLS
    WIELAND, T
    LIEDEL, K
    KALDENBERGSTASCH, S
    HERINGDORF, DM
    SCHMIDT, M
    JAKOBS, KH
    [J]. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1995, 351 (04) : 329 - 336
  • [73] Comparative analysis of the efficacy of A1 adenosine receptor activation of Gi/oα G proteins following coexpression of receptor and c protein and expression of A1 adenosine receptor-Gi/oα fusion proteins
    Wise, A
    Sheehan, M
    Rees, S
    Lee, M
    Milligan, G
    [J]. BIOCHEMISTRY, 1999, 38 (08) : 2272 - 2278
  • [74] Aripiprazole and its human metabolite are partial agonists at the human dopamine D2 receptor, but the rodent metabolite displays antagonist properties
    Wood, Martyn D.
    Scott, Claire
    Clarke, Kirsten
    Westaway, Julie
    Davies, Ceri H.
    Reavill, Charlie
    Hill, Mark
    Rourke, Claire
    Newson, Michael
    Jones, Declan N. C.
    Forbes, Ian T.
    Gribble, Andrew
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 2006, 546 (1-3) : 88 - 94
12345678