GABA-B-agonistic activity of certain baclofen homologues

Mohamed Attia; Claus Herdeis; Hans Bräuner-Osborne

doi:10.3390/molecules180910266

GABA-B-agonistic activity of certain baclofen homologues

Mohamed Attia, Claus Herdeis, Hans Bräuner-Osborne

9 Citations (Scopus)

Abstract

Baclofen (1) is a potent and selective agonist for bicuculline-insensitive GABA_B receptors and is used clinically as an antispastic and muscle relaxant agent. In the search for new bioactive chemical entities that bind specifically to GABA_B 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 GABA_BR agonists. Compound 1a is an agonist to GABA_B receptors with an EC₅₀ value of 46 μM on tsA201 cells transfected with GABA_B1b/GABA_B2/Gqz5, being the most active congener among all the synthesized compounds.

Original language	English
Journal	Molecules
Volume	18
Issue number	9
Pages (from-to)	10266-10284
ISSN	1420-3049
DOIs	https://doi.org/10.3390/molecules180910266
Publication status	Published - Sept 2013

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title = "GABA-B-agonistic activity of certain baclofen homologues",

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)-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.",

author = "Mohamed Attia and Claus Herdeis and Hans Br{\"a}uner-Osborne",

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T1 - GABA-B-agonistic activity of certain baclofen homologues

AU - Attia, Mohamed

AU - Herdeis, Claus

AU - Bräuner-Osborne, Hans

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Y1 - 2013/9

N2 - 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.

AB - 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.

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DO - 10.3390/molecules180910266

M3 - Journal article

C2 - 23973998

SN - 1420-3049

VL - 18

SP - 10266

EP - 10284

JO - Molecules

JF - Molecules

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ER -

GABA-B-agonistic activity of certain baclofen homologues

Abstract

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