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

GABAB-Agonistic Activity of Certain Baclofen Homologues

1,2,* , 2,*  and 3
Received: 12 July 2013; in revised form: 13 August 2013 / Accepted: 15 August 2013 / Published: 22 August 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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

AMA Style

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.



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