TY  - JOUR
A1  - Attia, Mohamed I.
A1  - Herdeis, Claus
A1  - Bräuner-Osborne, Hans
T1  - GABA(B)-Agonistic Activity of Certain Baclofen Homologues
JF  - Molecules
N2  - Baclofen (1) is a potent and selective agonist for bicuculline-insensitive GABAB receptors and is used clinically as an antispastic and muscle relaxant agent. In the search for new bioactive chemical entities that bind specifically to GABAB receptors, we report here the synthesis of certain baclofen homologues, namely (R,S)-5-amino-3-arylpentanoic acid hydrochlorides (R,S)-1a–h as well as (R,S)-5-amino-3-methylpentanoic acid [(RS)-1i] to be evaluated as GABABR agonists. Compound 1a is an agonist to GABAB receptors with an EC50 value of 46 μM on tsA201 cells transfected with GABAB1b/GABAB2/Gqz5, being the most active congener among all the synthesized compounds.
KW  - pharmacological evaluation
KW  - synthesis
KW  - GABA
KW  - baclofen homologues
KW  - GABAB receptor agonists
Y1  - 2013
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-129690
VL  - 18
IS  - 9
ER  -