Synthesis of dopamine transporter selective 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes.
Bioorg Med Chem Lett
; 13(4): 629-32, 2003 Feb 24.
Article
in En
| MEDLINE
| ID: mdl-12639545
ABSTRACT
A series of 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes was synthesized and the binding affinities of the compounds were determined at the dopamine and serotonin transporters. The 8-phenylpropyl analogues 8a (K(i)=4.1 nM) and 8b (K(i)=3.7 nM) were the most potent compounds of the series with binding affinities 3 times greater than GBR-12909. In addition, 8a (SERT/DAT=327) was over 300-fold more selective for the dopamine transporter than the serotonin transporter.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Membrane Transport Proteins
/
Membrane Glycoproteins
/
Bridged Bicyclo Compounds, Heterocyclic
/
Membrane Transport Modulators
/
Nerve Tissue Proteins
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2003
Document type:
Article
Affiliation country: