Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Bioorg Med Chem Lett
; 19(15): 4359-63, 2009 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-19560354
ABSTRACT
Direct comparison of pyridine versus pyrimidine substituents on a small but diverse set of ligands indicates that the pyrimidine substitution has the potential to enhance affinity and/or functional activity at alpha6 subunit-containing neuronal nicotinic receptors (NNRs) and decrease activation of ganglionic nicotinic receptors, depending on the scaffold. The ramifications of this structure-activity relationship are discussed in the context of the design of small molecules targeting smoking cessation.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Química Farmacêutica
/
Receptores Nicotínicos
/
Abandono do Hábito de Fumar
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Estados Unidos