[3H]MFZ 2-12: a novel radioligand for the dopamine transporter.
Bioorg Med Chem Lett
; 11(13): 1659-61, 2001 Jul 09.
Article
em En
| MEDLINE
| ID: mdl-11425531
ABSTRACT
In an effort to develop a tritiated dopamine transporter radioligand with higher affinity than the widely used [(3)H]WIN 35,428, we have synthesized [(3)H]2beta-carbomethoxy-3beta-(3',4'-dichlorophenyl)tropane ([(3)H]MFZ 2-12). Unlabeled MFZ 2-12 and the N-demethylated intermediate (MFZ 2-13) inhibited dopamine uptake by the human dopamine transporter with IC(50)'s of 1.1 and 1.4nM, respectively. The N-nor-intermediate (MFZ 2-13) was treated with CT(3)I resulting in [(3)H]MFZ 2-12; S.A.=80 Ci/mmol). [(3)H]MFZ 2-12 reversibly bound with a K(D) of 2.8nM to human dopamine transporter expressed heterologously in EM4 cells.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteínas de Membrana Transportadoras
/
Tropanos
/
Glicoproteínas de Membrana
/
Proteínas de Transporte
/
Proteínas do Tecido Nervoso
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2001
Tipo de documento:
Article