Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
Bioorg Med Chem Lett
; 22(7): 2380-4, 2012 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-22410083
ABSTRACT
A series of ligands based on SEN12333, containing either contracted or elongated alkyl chains, were synthesized and evaluated in molecular docking studies against a homology model of the α7 nicotinic acetylcholine receptor (nAChR) subtype. The predicted binding of all ligands was highly similar, with the exception of the analog containing a 5 methylene unit spacer. However, in vitro competition binding assays revealed that the ligands possessed dissimilar binding affinities, with a K(i) range of more than an order of magnitude (K(i)=0.50 to >10 µM), and only SEN12333 itself exhibited functional activity at the α7 nAChR.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Morfolinas
/
Agonistas Nicotínicos
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article