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Molecules 2013, 18(9), 10266-10284; doi:10.3390/molecules180910266

GABAB-Agonistic Activity of Certain Baclofen Homologues

1,2,* , 2,*  and 3
1 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2 Department of Pharmaceutical Chemistry, Institute of Pharmacy and Food Chemistry, Würzburg University, Am Hubland, Würzburg 97074, Germany 3 Department of Drug Design and Pharmacology, Faculty of Heath and Medical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen DK-2100, Denmark
* Authors to whom correspondence should be addressed.
Received: 12 July 2013 / Revised: 13 August 2013 / Accepted: 15 August 2013 / Published: 22 August 2013
(This article belongs to the Section Medicinal Chemistry)
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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)-1ah 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.
Keywords: GABA; synthesis; baclofen homologues; GABAB receptor agonists; pharmacological evaluation GABA; synthesis; baclofen homologues; GABAB receptor agonists; pharmacological evaluation
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Attia, M.I.; Herdeis, C.; Bräuner-Osborne, H. GABAB-Agonistic Activity of Certain Baclofen Homologues. Molecules 2013, 18, 10266-10284.

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