Published in J Pharmacol Exp Ther on January 27, 2004
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov (2009) 6.69
The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors. Br J Pharmacol (2013) 5.74
Metabotropic glutamate receptors: physiology, pharmacology, and disease. Annu Rev Pharmacol Toxicol (2010) 4.77
Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends Pharmacol Sci (2008) 3.22
Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther (2008) 2.29
Ionotropic and metabotropic glutamate receptor structure and pharmacology. Psychopharmacology (Berl) (2005) 2.25
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. J Med Chem (2012) 2.10
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol (2008) 1.94
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol Pharmacol (2010) 1.93
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology. Biochemistry (2011) 1.89
mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology (2009) 1.80
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. Bioorg Med Chem Lett (2008) 1.78
Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity. Mol Pharmacol (2008) 1.68
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Mol Pharmacol (2011) 1.46
Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). ACS Chem Neurosci (2011) 1.44
Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential. Neuropharmacology (2010) 1.30
Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273. ChemMedChem (2009) 1.29
Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks. Curr Top Med Chem (2013) 1.28
Positive allosteric modulation of metabotropic glutamate 5 (mGlu5) receptors reverses N-Methyl-D-aspartate antagonist-induced alteration of neuronal firing in prefrontal cortex. Biol Psychiatry (2007) 1.28
Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci (2010) 1.24
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. Bioorg Med Chem Lett (2008) 1.19
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. Bioorg Med Chem Lett (2008) 1.16
Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening. ACS Chem Neurosci (2010) 1.16
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. Mol Pharmacol (2012) 1.15
Cognitive effects of Group I metabotropic glutamate receptor ligands in the context of drug addiction. Eur J Pharmacol (2010) 1.12
Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents. Neuron (2015) 1.10
Metabotropic glutamate receptors as therapeutic targets for schizophrenia. Neuropharmacology (2011) 1.10
Preferential binding of allosteric modulators to active and inactive conformational states of metabotropic glutamate receptors. BMC Bioinformatics (2008) 1.06
Targeting glutamate synapses in schizophrenia. Trends Mol Med (2011) 1.06
Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology. Mol Pharmacol (2013) 1.05
Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. ACS Med Chem Lett (2010) 1.04
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. Bioorg Med Chem Lett (2011) 1.04
A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling. Mol Pharmacol (2013) 1.04
Novel Allosteric Modulators of G Protein-coupled Receptors. J Biol Chem (2015) 1.02
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Bioorg Med Chem Lett (2009) 0.99
Positive allosteric modulators of type 5 metabotropic glutamate receptors (mGluR5) and their therapeutic potential for the treatment of CNS disorders. Molecules (2011) 0.99
Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors. Chem Rev (2016) 0.97
Glutamatergic targets for enhancing extinction learning in drug addiction. Curr Neuropharmacol (2010) 0.95
Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). Bioorg Med Chem Lett (2009) 0.95
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. Bioorg Med Chem Lett (2012) 0.94
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett (2015) 0.92
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅). J Med Chem (2014) 0.92
Attenuation of ketamine-evoked behavioral responses by mGluR5 positive modulators in mice. Psychopharmacology (Berl) (2008) 0.91
Allosteric modulation of metabotropic glutamate receptors. Adv Pharmacol (2011) 0.91
Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias. Br J Pharmacol (2015) 0.88
Quantitative analysis reveals multiple mechanisms of allosteric modulation of the mGlu5 receptor in rat astroglia. Mol Pharmacol (2011) 0.85
mGluR5 positive modulators both potentiate activation and restore inhibition in NMDA receptors by PKC dependent pathway. J Biomed Sci (2011) 0.83
Disruption of the Na+ ion binding site as a mechanism for positive allosteric modulation of the mu-opioid receptor. Proc Natl Acad Sci U S A (2014) 0.83
Allosteric modulators for mGlu receptors. Curr Neuropharmacol (2007) 0.83
2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites. J Med Chem (2014) 0.83
Effects of positive allosteric modulators on single-cell oscillatory Ca2+ signaling initiated by the type 5 metabotropic glutamate receptor. Mol Pharmacol (2009) 0.83
Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation. Mol Pharmacol (2015) 0.83
Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. Bioorg Med Chem Lett (2012) 0.82
Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications. Cell Signal (2014) 0.81
Functional selectivity induced by mGlu₄ receptor positive allosteric modulation and concomitant activation of Gq coupled receptors. Neuropharmacology (2012) 0.80
Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5. Bioorg Med Chem (2015) 0.79
Metabotropic glutamate receptors: potential drug targets for psychiatric disorders. Open Med Chem J (2010) 0.79
Rethinking metabotropic glutamate receptor 5 pathological findings in psychiatric disorders: implications for the future of novel therapeutics. BMC Psychiatry (2014) 0.78
VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy. J Pharmacol Exp Ther (2015) 0.77
Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorg Med Chem Lett (2015) 0.77
Metabotropic glutamate receptor 5 - a promising target in drug development and neuroimaging. Eur J Nucl Med Mol Imaging (2016) 0.76
Targeting metabotropic glutamate receptors for novel treatments of schizophrenia. Mol Brain (2017) 0.75
Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACS Med Chem Lett (2016) 0.75
Metabotropic glutamate receptor 5 as a potential target for smoking cessation. Psychopharmacology (Berl) (2016) 0.75
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov (2009) 6.69
Syk-dependent cytokine induction by Dectin-1 reveals a novel pattern recognition pathway for C type lectins. Immunity (2005) 6.21
The genome of the blood fluke Schistosoma mansoni. Nature (2009) 5.94
Dectin-1 mediates the biological effects of beta-glucans. J Exp Med (2003) 5.82
Human dectin-1 deficiency and mucocutaneous fungal infections. N Engl J Med (2009) 5.27
Dectin-1 is a major beta-glucan receptor on macrophages. J Exp Med (2002) 4.87
Metabotropic glutamate receptors: physiology, pharmacology, and disease. Annu Rev Pharmacol Toxicol (2010) 4.77
Immune sensing of Candida albicans requires cooperative recognition of mannans and glucans by lectin and Toll-like receptors. J Clin Invest (2006) 4.45
The top prescription drugs of 2009 in the US: CNS therapeutics rank among highest grossing. ACS Chem Neurosci (2010) 4.20
Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation (2007) 3.65
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett (2005) 3.50
The Akt/PKB pathway: molecular target for cancer drug discovery. Oncogene (2005) 3.42
Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends Pharmacol Sci (2008) 3.22
The beta-glucan receptor dectin-1 recognizes specific morphologies of Aspergillus fumigatus. PLoS Pathog (2005) 3.13
The macrophage mannose receptor induces IL-17 in response to Candida albicans. Cell Host Microbe (2009) 3.07
International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences. Pharmacol Rev (2005) 2.98
Identification of oxadiazoles as new drug leads for the control of schistosomiasis. Nat Med (2008) 2.90
Enhanced learning and memory and altered GABAergic synaptic transmission in mice lacking the alpha 5 subunit of the GABAA receptor. J Neurosci (2002) 2.87
Dectin-1 uses novel mechanisms for yeast phagocytosis in macrophages. Blood (2004) 2.84
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J Pharmacol Exp Ther (2004) 2.83
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol (2009) 2.72
Application of combinatorial chemistry science on modern drug discovery. J Comb Chem (2008) 2.64
Syk kinase is required for collaborative cytokine production induced through Dectin-1 and Toll-like receptors. Eur J Immunol (2008) 2.62
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J Med Chem (2004) 2.46
Thioredoxin glutathione reductase from Schistosoma mansoni: an essential parasite enzyme and a key drug target. PLoS Med (2007) 2.39
Dectin-1 expression and function are enhanced on alternatively activated and GM-CSF-treated macrophages and are negatively regulated by IL-10, dexamethasone, and lipopolysaccharide. J Immunol (2003) 2.38
Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol Sci (2009) 2.38
Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci (2008) 2.34
Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther (2008) 2.29
In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem Biol (2010) 2.29
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol (2003) 2.27
Reduced cardiac hypertrophy in toll-like receptor 4-deficient mice following pressure overload. Cardiovasc Res (2005) 2.24
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol Cancer Ther (2005) 2.23
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorg Med Chem Lett (2006) 2.17
The top prescription drugs of 2010 in the United States: antipsychotics show strong growth. ACS Chem Neurosci (2011) 2.16
A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Mol Pharmacol (2008) 2.12
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. J Med Chem (2012) 2.10
A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol Pharmacol (2005) 2.03
Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment. Proc Natl Acad Sci U S A (2003) 1.98
Sedation and anesthesia mediated by distinct GABA(A) receptor isoforms. J Neurosci (2003) 1.97
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc Natl Acad Sci U S A (2003) 1.96
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol (2008) 1.94
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol Pharmacol (2010) 1.93
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology. Biochemistry (2011) 1.89
Covalent modifiers: an orthogonal approach to drug design. J Med Chem (2009) 1.87
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proc Natl Acad Sci U S A (2009) 1.87
Loss of Phosphatase and Tensin homologue deleted on chromosome 10 engages ErbB3 and insulin-like growth factor-I receptor signaling to promote antiestrogen resistance in breast cancer. Cancer Res (2009) 1.84
Activation of Toll-like receptor 4 signaling contributes to hippocampal neuronal death following global cerebral ischemia/reperfusion. J Neuroimmunol (2007) 1.84
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat Chem Biol (2007) 1.83
The role of SIGNR1 and the beta-glucan receptor (dectin-1) in the nonopsonic recognition of yeast by specific macrophages. J Immunol (2004) 1.82
Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science (2014) 1.81
mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology (2009) 1.80
Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. Curr Opin Pharmacol (2005) 1.80
The human beta-glucan receptor is widely expressed and functionally equivalent to murine Dectin-1 on primary cells. Eur J Immunol (2005) 1.80
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. Bioorg Med Chem Lett (2008) 1.78
Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia. Curr Top Med Chem (2006) 1.77