Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)
about
Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probeDevelopment of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)Current approaches for the discovery of drugs that deter substance and drug abuse.Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.Structural features embedded in G protein-coupled receptor co-crystal structures are key to their success in virtual screening.Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate ReceptorsMolecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats.Muscarinic M5 receptors modulate ethanol seeking in rats.Prediction of consensus binding mode geometries for related chemical series of positive allosteric modulators of adenosine and muscarinic acetylcholine receptors.
P2860
Q28237300-8287B400-6039-476C-BC94-FC96C5AF8895Q28246512-BA616ACF-94F6-43B4-A0CE-82B60EA06510Q28973615-6E73F7F8-B71C-497C-A64D-58411F7E87DFQ35534556-02F24FAE-F316-4B8D-9E60-1A6358883FC2Q36336103-963D4488-A881-4634-8E94-D39339F459DCQ37183072-224BAB31-9047-41C2-B854-B6960DD885EAQ38755530-A5288550-1C70-4ECA-ABF9-309BBDCF166CQ48167663-B27895C2-6601-4B35-8D30-75544272A13BQ52684297-FA2EC637-9909-4299-A6CF-DE9ACB60250BQ52737158-395424EF-0A37-4ED4-B08D-18DEB44154D1
P2860
Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)
description
2013 nî lūn-bûn
@nan
2013 թուականի Նոյեմբերին հրատարակուած գիտական յօդուած
@hyw
2013 թվականի նոյեմբերին հրատարակված գիտական հոդված
@hy
2013年の論文
@ja
2013年論文
@yue
2013年論文
@zh-hant
2013年論文
@zh-hk
2013年論文
@zh-mo
2013年論文
@zh-tw
2013年论文
@wuu
name
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@ast
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@en
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@nl
type
label
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@ast
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@en
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@nl
prefLabel
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@ast
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@en
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@nl
P2093
P2860
P50
P356
P1476
Discovery of the first M5-sele ...... -a]isoindol-5(9bH)-one (ML375)
@en
P2093
Emery Smith
Hyekyung P Cho
J Scott Daniels
Joel M Harp
Masaya Kokubo
Michael R Wood
Nathan R Kett
Patrick R Gentry
Peter Chase
Peter S Hodder
P2860
P304
P356
10.1021/JM4013246
P407
P577
2013-11-27T00:00:00Z