GABA(B)-Agonistic Activity of Certain Baclofen Homologues

Please always quote using this URN: urn:nbn:de:bvb:20-opus-129690
  • 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 onBaclofen (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.show moreshow less

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Metadaten
Author: Mohamed I. Attia, Claus Herdeis, Hans Bräuner-Osborne
URN:urn:nbn:de:bvb:20-opus-129690
Document Type:Journal article
Faculties:Fakultät für Chemie und Pharmazie / Institut für Pharmazie und Lebensmittelchemie
Language:English
Parent Title (English):Molecules
Year of Completion:2013
Volume:18
Issue:9
Pagenumber:10266-10284
Source:Molecules 2013, 18, 10266-10284; doi:10.3390/molecules180910266
DOI:https://doi.org/10.3390/molecules180910266
Dewey Decimal Classification:6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 615 Pharmakologie, Therapeutik
Tag:GABA; GABAB receptor agonists; baclofen homologues; pharmacological evaluation; synthesis
Release Date:2016/06/27
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung