1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.
Bioorg Med Chem Lett
; 13(17): 2921-4, 2003 Sep 01.
Article
em En
| MEDLINE
| ID: mdl-14611858
ABSTRACT
A series of novel 1H-pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes was prepared and screened at selected dopamine receptor subtypes. Compound 4 (NGB 4420) displayed high affinity and selectivity (>100-fold) for the D(4) over D(2) and other CNS receptors. This compound was identified as a D(4) antagonist via its attenuation of dopamine agonist-induced GTPgamma(35)S binding at D(4) receptor.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiofenos
/
Receptores de Dopamina D2
Limite:
Humans
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article