Binding of (-)-[3H]-CGP12177 at two sites in recombinant human beta 1-adrenoceptors and interaction with beta-blockers.
about
A full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptorsThe Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptorsIdentification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human β1-adrenoceptorIdentification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activitiesHuman atrial β(1L)-adrenoceptor but not β₃-adrenoceptor activation increases force and Ca(2+) current at physiological temperature.Agonist binding by the β2-adrenergic receptor: an effect of receptor conformation on ligand association-dissociation characteristicsThe design, synthesis and pharmacological characterization of novel β₂-adrenoceptor antagonists.Thermodynamics and docking of agonists to the β(2)-adrenoceptor determined using [(3)H](R,R')-4-methoxyfenoterol as the marker ligand.beta3-adrenergic receptor activation increases human atrial tissue contractility and stimulates the L-type Ca2+ currentMultiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates.Human heart beta-adrenoceptors: beta1-adrenoceptor diversification through 'affinity states' and polymorphism.Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation.Chronic activation of the low affinity site of β1-adrenoceptors stimulates haemodynamics but exacerbates pressure-overload cardiac remodelling.On and off-target effects of telomere uncapping G-quadruplex selective ligands based on pentacyclic acridinium saltsPhosphodiesterase PDE3 blunts the positive inotropic and cyclic AMP enhancing effects of CGP12177 but not of noradrenaline in rat ventricleUse of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells.Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.Positive inotropic and lusitropic effects mediated via the low-affinity state of beta1-adrenoceptors in pithed rats.Markedly reduced effects of (-)-isoprenaline but not of (-)-CGP12177 and unchanged affinity of beta-blockers at Gly389-beta1-adrenoceptors compared to Arg389-beta1-adrenoceptors.
P2860
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P2860
Binding of (-)-[3H]-CGP12177 at two sites in recombinant human beta 1-adrenoceptors and interaction with beta-blockers.
description
2004 nî lūn-bûn
@nan
2004年の論文
@ja
2004年学术文章
@wuu
2004年学术文章
@zh
2004年学术文章
@zh-cn
2004年学术文章
@zh-hans
2004年学术文章
@zh-my
2004年学术文章
@zh-sg
2004年學術文章
@yue
2004年學術文章
@zh-hant
name
Binding of (-)-[3H]-CGP12177 a ...... nteraction with beta-blockers.
@en
type
label
Binding of (-)-[3H]-CGP12177 a ...... nteraction with beta-blockers.
@en
prefLabel
Binding of (-)-[3H]-CGP12177 a ...... nteraction with beta-blockers.
@en
P2093
P1476
Binding of (-)-[3H]-CGP12177 a ...... nteraction with beta-blockers.
@en
P2093
Alberto J Kaumann
James A Lynham
Shirin S Joseph
P2888
P304
P356
10.1007/S00210-004-0884-Y
P577
2004-04-02T00:00:00Z