Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery.
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The chemokine receptor CCR1 is constitutively active, which leads to G protein-independent, β-arrestin-mediated internalizationAPD125, a selective serotonin 5-HT(2A) receptor inverse agonist, significantly improves sleep maintenance in primary insomniaEnhanced spontaneous activity of the mu opioid receptor by cysteine mutations: characterization of a tool for inverse agonist screeningA constitutively active G protein-coupled acetylcholine receptor regulates motility of larval Schistosoma mansoniPhasic and Tonic mGlu7 Receptor Activity Modulates the Thalamocortical NetworkHypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidenceReal-time analysis of dopamine: antagonist interactions at recombinant human D2long receptor upon modulation of its activation stateStructural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-protein-coupled receptorsCharacterization of beta(1)-selectivity, adrenoceptor-G(s)-protein interaction and inverse agonism of nebivolol in human myocardiumMacMARCKS interacts with the metabotropic glutamate receptor type 7 and modulates G protein-mediated constitutive inhibition of calcium channels.Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons.NaV1.5 sodium channel window currents contribute to spontaneous firing in olfactory sensory neurons.Bidirectional scaling of astrocytic metabotropic glutamate receptor signaling following long-term changes in neuronal firing rates.Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonismThe 5-HT3B subunit confers spontaneous channel opening and altered ligand properties of the 5-HT3 receptor.PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity.The significance of G protein-coupled receptor crystallography for drug discovery.A pharmacological analysis of an associative learning task: 5-HT(1) to 5-HT(7) receptor subtypes function on a pavlovian/instrumental autoshaped memory.Honey Bee Allatostatins Target Galanin/Somatostatin-Like Receptors and Modulate Learning: A Conserved Function?Evidence for constitutively-active adenosine receptors at mammalian motor nerve endingsCentral kappa-opioid receptor-mediated antidepressant-like effects of nor-Binaltorphimine: behavioral and BDNF mRNA expression studies.Maturational alterations in constitutive activity of medial prefrontal cortex kappa-opioid receptors in Wistar ratsAn intracellular loop (IL2) residue confers different basal constitutive activities to the human lutropin receptor and human thyrotropin receptor through structural communication between IL2 and helix 6, via helix 3.Cucurbitacin B inhibits the stemness and metastatic abilities of NSCLC via downregulation of canonical Wnt/β-catenin signaling axis.Heterotrimeric g proteins: insights into the neurobiology of mood disorders.Label-free optical biosensor: a tool for G protein-coupled receptors pharmacology profiling and inverse agonists identification.Inverse agonism at beta-adrenergic receptors: therapeutic implications.Pharmacology and structure of isolated conformations of the adenosine A₂A receptor define ligand efficacy.Characterization of human and rodent native and recombinant adenosine A(2B) receptors by radioligand binding studies.Constitutive activity modulation of human metabotropic glutamate 5a receptors in HEK293 cells: a role for key amino-terminal cysteine residues.The temporal hormesis of drug therapiesRegulation of ethanol-related behavior and ethanol metabolism by the Corazonin neurons and Corazonin receptor in Drosophila melanogaster.C-terminal truncated cannabinoid receptor 1 coexpressed with G protein trimer in Sf9 cells exists in a precoupled state and shows constitutive activity.Inducing plasticity of astrocytic receptors by manipulation of neuronal firing rates.Alpha-1 adrenoceptor up-regulation induced by prazosin but not KMD-3213 or reserpine in rats.Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors.h5-HT(1B) receptor-mediated constitutive Galphai3-protein activation in stably transfected Chinese hamster ovary cells: an antibody capture assay reveals protean efficacy of 5-HT17Beta-estradiol modulates hMT1 melatonin receptor function.Aberrant ligand-induced activation of G protein-coupled estrogen receptor 1 (GPER) results in developmental malformations during vertebrate embryogenesis.
P2860
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P2860
Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery.
description
2000 nî lūn-bûn
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2000 թուականի Մայիսին հրատարակուած գիտական յօդուած
@hyw
2000 թվականի մայիսին հրատարակված գիտական հոդված
@hy
2000年の論文
@ja
2000年論文
@yue
2000年論文
@zh-hant
2000年論文
@zh-hk
2000年論文
@zh-mo
2000年論文
@zh-tw
2000年论文
@wuu
name
Inverse agonism at G protein-c ...... plications for drug discovery.
@ast
Inverse agonism at G protein-c ...... plications for drug discovery.
@en
type
label
Inverse agonism at G protein-c ...... plications for drug discovery.
@ast
Inverse agonism at G protein-c ...... plications for drug discovery.
@en
prefLabel
Inverse agonism at G protein-c ...... plications for drug discovery.
@ast
Inverse agonism at G protein-c ...... plications for drug discovery.
@en
P2093
P2860
P356
P1476
Inverse agonism at G protein-c ...... plications for drug discovery.
@en
P2093
A P IJzerman
A P Kourounakis
R A de Ligt
P2860
P356
10.1038/SJ.BJP.0703311
P407
P577
2000-05-01T00:00:00Z