Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.
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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule ProbesThe Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's diseaseTargeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptorsDevelopment of allosteric modulators of GPCRs for treatment of CNS disordersDiscovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)Muscarinic Acetylcholine Receptor Subtypes as Potential Drug Targets for the Treatment of Schizophrenia, Drug Abuse and Parkinson's DiseaseAllosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discoveryDevelopment of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficitsSynthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.Cholinergic modulation of amyloid precursor protein processing with emphasis on M1 muscarinic receptor: perspectives and challenges in treatment of Alzheimer's disease.Novel M(1) allosteric ligands: a patent review.Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer's disease and schizophreniaDevelopment of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetrationDevelopment of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe moleculeMuscarinic M1 receptor agonists: can they improve cognitive performance?Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.Acute Effects of Muscarinic M1 Receptor Modulation on AβPP Metabolism and Amyloid-β Levels in vivo: A Microdialysis Study.The muscarinic M1 receptor positive allosteric modulator PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque.Therapeutics of Neurotransmitters in Alzheimer's Disease.M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease
P2860
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P2860
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.
description
2010 nî lūn-bûn
@nan
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
2010年论文
@zh
2010年论文
@zh-cn
name
Discovery and optimization of ...... ment of ML169, an MLPCN probe.
@en
type
label
Discovery and optimization of ...... ment of ML169, an MLPCN probe.
@en
prefLabel
Discovery and optimization of ...... ment of ML169, an MLPCN probe.
@en
P2093
P2860
P50
P1476
Discovery and optimization of ...... ment of ML169, an MLPCN probe.
@en
P2093
C David Weaver
Carrie K Jones
Douglas J Sheffler
Emily Days
Hyekyung P Cho
J Scott Daniels
L Michelle Lewis
Michael R Wood
Paul R Reid
Thomas M Bridges
P2860
P304
P356
10.1016/J.BMCL.2010.12.015
P407
P577
2010-12-09T00:00:00Z