Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
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Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disordersDiscovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptorSynthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273Drugs for allosteric sites on receptorsA novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptorsSubstituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction.N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addictionDiscovery 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.Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening.Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moietiesSynthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 53-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.Allosteric modulation of the M₃ muscarinic receptor by amiodarone and N-ethylamiodarone: application of the four-ligand allosteric two-state model.Recent advances in the design and development of novel negative allosteric modulators of mGlu(5)Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discoveryProgress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signalingPractical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsAllosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.Approaches for probing allosteric interactions at 7 transmembrane spanning receptors.Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders.Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTSDiscovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB1.Overview of Critical Parameters for the Design and Execution of a High-Throughput Screen for Allosteric Ligands.Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold.Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs.Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.
P2860
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P2860
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.
description
2008 nî lūn-bûn
@nan
2008 թուականի Մայիսին հրատարակուած գիտական յօդուած
@hyw
2008 թվականի մայիսին հրատարակված գիտական հոդված
@hy
2008年の論文
@ja
2008年論文
@yue
2008年論文
@zh-hant
2008年論文
@zh-hk
2008年論文
@zh-mo
2008年論文
@zh-tw
2008年论文
@wuu
name
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@ast
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@en
type
label
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@ast
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@en
prefLabel
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@ast
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@en
P2860
P1476
Synthesis and SAR of a mGluR5 ...... ylethynyl)pyrimidine scaffold.
@en
P2093
Alice L Rodriguez
Sameer Sharma
P2860
P304
P356
10.1016/J.BMCL.2008.05.091
P407
P577
2008-05-29T00:00:00Z