Literature DB >> 10780991

Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery.

R A de Ligt1, A P Kourounakis, A P IJzerman.   

Abstract

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Year:  2000        PMID: 10780991      PMCID: PMC1572052          DOI: 10.1038/sj.bjp.0703311

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


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  82 in total

1.  ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL.

Authors:  J MONOD; J WYMAN; J P CHANGEUX
Journal:  J Mol Biol       Date:  1965-05       Impact factor: 5.469

2.  Interaction at end-plate receptors between different choline derivatives.

Authors:  J DEL CASTILLO; B KATZ
Journal:  Proc R Soc Lond B Biol Sci       Date:  1957-05-07

Review 3.  Effects of drugs on beta-adrenergic receptors on human lymphocytes.

Authors:  P B Molinoff; R D Aarons
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4.  Histamine H1-receptor binding sites in guinea pig brain membranes: regulation of agonist interactions by guanine nucleotides and cations.

Authors:  R S Chang; S H Synder
Journal:  J Neurochem       Date:  1980-04       Impact factor: 5.372

5.  A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

Authors:  A De Lean; J M Stadel; R J Lefkowitz
Journal:  J Biol Chem       Date:  1980-08-10       Impact factor: 5.157

6.  Ligand-induced overexpression of a constitutively active beta2-adrenergic receptor: pharmacological creation of a phenotype in transgenic mice.

Authors:  P Samama; R A Bond; H A Rockman; C A Milano; R J Lefkowitz
Journal:  Proc Natl Acad Sci U S A       Date:  1997-01-07       Impact factor: 11.205

7.  Two affinity states of Ri adenosine receptors in brain membranes. Analysis of guanine nucleotide and temperature effects on radioligand binding.

Authors:  M J Lohse; V Lenschow; U Schwabe
Journal:  Mol Pharmacol       Date:  1984-07       Impact factor: 4.436

8.  Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide.

Authors:  E Burgisser; A De Lean; R J Lefkowitz
Journal:  Proc Natl Acad Sci U S A       Date:  1982-03       Impact factor: 11.205

9.  The ternary complex model. Its properties and application to ligand interactions with the D2-dopamine receptor of the anterior pituitary gland.

Authors:  K A Wreggett; A De Léan
Journal:  Mol Pharmacol       Date:  1984-09       Impact factor: 4.436

10.  Interaction of convulsive ligands with benzodiazepine receptors.

Authors:  C Braestrup; R Schmiechen; G Neef; M Nielsen; E N Petersen
Journal:  Science       Date:  1982-06-11       Impact factor: 47.728

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  43 in total

Review 1.  The significance of G protein-coupled receptor crystallography for drug discovery.

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2.  Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors.

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3.  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-HT.

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4.  Characterization of beta(1)-selectivity, adrenoceptor-G(s)-protein interaction and inverse agonism of nebivolol in human myocardium.

Authors:  C Maack; S Tyroller; P Schnabel; B Cremers; E Dabew; M Südkamp; M Böhm
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5.  NaV1.5 sodium channel window currents contribute to spontaneous firing in olfactory sensory neurons.

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6.  The chemokine receptor CCR1 is constitutively active, which leads to G protein-independent, β-arrestin-mediated internalization.

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7.  Real-time analysis of dopamine: antagonist interactions at recombinant human D2long receptor upon modulation of its activation state.

Authors:  P J Pauwels; S Tardif; T Wurch; F C Colpaert
Journal:  Br J Pharmacol       Date:  2001-09       Impact factor: 8.739

Review 8.  A pharmacological analysis of an associative learning task: 5-HT(1) to 5-HT(7) receptor subtypes function on a pavlovian/instrumental autoshaped memory.

Authors:  Alfredo Meneses
Journal:  Learn Mem       Date:  2003 Sep-Oct       Impact factor: 2.460

9.  Maturational alterations in constitutive activity of medial prefrontal cortex kappa-opioid receptors in Wistar rats.

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Journal:  J Neurochem       Date:  2015-09-11       Impact factor: 5.372

10.  APD125, a selective serotonin 5-HT(2A) receptor inverse agonist, significantly improves sleep maintenance in primary insomnia.

Authors:  Russell Rosenberg; David J Seiden; Steven G Hull; Milton Erman; Howard Schwartz; Christen Anderson; Warren Prosser; William Shanahan; Matilde Sanchez; Emil Chuang; Thomas Roth
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