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 50 条
  • [31] Analysis of G protein activation in Sf9 and mammalian cells by agonist-promoted [35S]GTPγS binding
    Windh, RT
    Manning, DR
    G PROTEIN PATHWAYS PART B: G PROTEINS AND THEIR REGULATORS, 2002, 344 : 3 - 14
  • [32] Visualization of Functional Neuropeptide Y Receptors in the Mouse Hippocampus and Neocortex Using [35S]GTPγS Binding
    Heidi Elbrønd-Bek
    Casper R. Gøtzsche
    Mette Skinbjerg
    Ditte Z. Christensen
    Per Plenge
    David P. D. Woldbye
    International Journal of Peptide Research and Therapeutics, 2015, 21 : 269 - 278
  • [33] Visualization of Functional Neuropeptide Y Receptors in the Mouse Hippocampus and Neocortex Using [35S]GTPγS Binding
    Elbrond-Bek, Heidi
    Gotzsche, Casper R.
    Skinbjerg, Mette
    Christensen, Ditte Z.
    Plenge, Per
    Woldbye, David P. D.
    INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS, 2015, 21 (03) : 269 - 278
  • [34] Functional coupling between adenosine A1 receptors and G-proteins in rat and postmortem human brain membranes determined with conventional guanosine-5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding or [35S]GTPγS/immunoprecipitation assay
    Odagaki, Yuji
    Kinoshita, Masakazu
    Ota, Toshio
    Meana, J. Javier
    Callado, Luis F.
    Matsuoka, Isao
    Garcia-Sevilla, Jesus A.
    PURINERGIC SIGNALLING, 2018, 14 (02) : 177 - 190
  • [35] In vitro visualization of 5-HT receptors in rat brain using [35S]GTPγS binding
    Beer, MS
    Stanton, JA
    ADVANCES IN SEROTONIN RECEPTOR RESEARCH: MOLECULAR BIOLOGY, SIGNAL TRANSDUCTION, AND THERAPEUTICS, 1998, 861 : 265 - 265
  • [36] Functional coupling between adenosine A1 receptors and G-proteins in rat and postmortem human brain membranes determined with conventional guanosine-5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding or [35S]GTPγS/immunoprecipitation assay
    Yuji Odagaki
    Masakazu Kinoshita
    Toshio Ota
    J. Javier Meana
    Luis F. Callado
    Isao Matsuoka
    Jesús A. García-Sevilla
    Purinergic Signalling, 2018, 14 : 177 - 190
  • [37] Autoradiographic analysis of dopamine receptor-stimulated [35S]GTPγS binding in rat striatum
    He, L
    Di Monte, DA
    Langston, JW
    Quik, M
    BRAIN RESEARCH, 2000, 885 (01) : 133 - 136
  • [38] Mechanisms of GDP regulation of cannabinoid receptor agonist efficacy in stimulating [35S]GTPγS binding.
    Childers, SR
    Breivogel, CS
    FASEB JOURNAL, 1998, 12 (04): : A152 - A152
  • [39] Functional activation of Gαq coupled with serotonin receptors in cerebral cortical membranes determined by antibody-capture scintillation proximity assay/[35S]GTPγS binding
    Odagaki, Yuji
    Toyoshima, Ryoichi
    JOURNAL OF PHARMACOLOGICAL SCIENCES, 2012, 118 : 179P - 179P
  • [40] Agonist-stimulated [35S]GTPγS binding in brain -: Modulation by endogenous adenosine
    Moore, RJ
    Xiao, RY
    Sim-Selley, LJ
    Childers, SR
    NEUROPHARMACOLOGY, 2000, 39 (02) : 282 - 289
12345