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GABAB-Agonistic Activity of Certain Baclofen Homologues
AbstractBaclofen (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.
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Attia, M.I.; Herdeis, C.; Bräuner-Osborne, H. GABAB-Agonistic Activity of Certain Baclofen Homologues. Molecules 2013, 18, 10266-10284.View more citation formats
Attia MI, Herdeis C, Bräuner-Osborne H. GABAB-Agonistic Activity of Certain Baclofen Homologues. Molecules. 2013; 18(9):10266-10284.Chicago/Turabian Style
Attia, Mohamed I.; Herdeis, Claus; Bräuner-Osborne, Hans. 2013. "GABAB-Agonistic Activity of Certain Baclofen Homologues." Molecules 18, no. 9: 10266-10284.