Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004.
ACS Chem Neurosci
; 6(6): 838-44, 2015 Jun 17.
Article
em En
| MEDLINE
| ID: mdl-25857219
ABSTRACT
The M4 mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh may be exploited for selective receptor targeting. We report the synthesis of a focused library of putative M4 PAMs derived from VU10004. These compounds investigate the pharmacological effects of target thieno[2,3-b]pyridines assembled from primary cycloalkanamines and cyclic secondary amines providing useful estimates of affinity (KB), cooperativity (αß), and direct agonist properties (τB).
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Agonistas Colinérgicos
/
Receptor Muscarínico M4
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Tienopiridinas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
ACS Chem Neurosci
Ano de publicação:
2015
Tipo de documento:
Article