GABAB-Agonistic Activity of Certain Baclofen Homologues
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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2013-08-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/18/9/10266 |
| _version_ | 1818163343992553472 |
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| author | Mohamed I. Attia Hans Bräuner-Osborne Claus Herdeis |
| author_facet | Mohamed I. Attia Hans Bräuner-Osborne Claus Herdeis |
| author_sort | Mohamed I. Attia |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-11T16:48:04Z |
| format | Article |
| id | doaj.art-ca9a2303d9204625a7215a754d843045 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-11T16:48:04Z |
| publishDate | 2013-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-ca9a2303d9204625a7215a754d8430452022-12-22T00:58:10ZengMDPI AGMolecules1420-30492013-08-01189102661028410.3390/molecules180910266GABAB-Agonistic Activity of Certain Baclofen HomologuesMohamed I. AttiaHans Bräuner-OsborneClaus HerdeisBaclofen (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.http://www.mdpi.com/1420-3049/18/9/10266GABAsynthesisbaclofen homologuesGABAB receptor agonistspharmacological evaluation |
| spellingShingle | Mohamed I. Attia Hans Bräuner-Osborne Claus Herdeis GABAB-Agonistic Activity of Certain Baclofen Homologues Molecules GABA synthesis baclofen homologues GABAB receptor agonists pharmacological evaluation |
| title | GABAB-Agonistic Activity of Certain Baclofen Homologues |
| title_full | GABAB-Agonistic Activity of Certain Baclofen Homologues |
| title_fullStr | GABAB-Agonistic Activity of Certain Baclofen Homologues |
| title_full_unstemmed | GABAB-Agonistic Activity of Certain Baclofen Homologues |
| title_short | GABAB-Agonistic Activity of Certain Baclofen Homologues |
| title_sort | gabab agonistic activity of certain baclofen homologues |
| topic | GABA synthesis baclofen homologues GABAB receptor agonists pharmacological evaluation |
| url | http://www.mdpi.com/1420-3049/18/9/10266 |
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