Synthesis and pharmacological characterization of certain baclofen analogues

M.I. Attia; C. Herdeis; Hans Bräuner-Osborne

Synthesis and pharmacological characterization of certain baclofen analogues

M.I. Attia, C. Herdeis, Hans Bräuner-Osborne

1 Citationer (Scopus)

Abstract

(RS)-4-Amino-3-(4-chlorophenyl)butanoic acid (baclofen, 2) is the prototypic selective GABA_BR agonist and is used clinically for the treatment of spasticity associated with brain and spinal cord injuries. Synthesis and GABA_B receptor agonist activity of certain amino acids structurally related to baclofen (2) are reported. (RS)-4-amino-3-(4- ethynylphenyl)butanoic acid hydrochloride (1b) showed GABA_B receptor agonist activity with EC₅₀ = 240 μM whereas (RS)-4-amino-3-(4-iodophenyl)butanoic acid hydrochloride (1c) emerged as the best GABAB receptor agonist congener in the synthesized compounds with ED₅₀ = 32 μM.

Originalsprog	Engelsk
Tidsskrift	Digest Journal of Nanomaterials and Biostructures
Vol/bind	8
Udgave nummer	1
Sider (fra-til)	139-149
ISSN	1842-3582
Status	Udgivet - 2012

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Citationsformater

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abstract = "(RS)-4-Amino-3-(4-chlorophenyl)butanoic acid (baclofen, 2) is the prototypic selective GABABR agonist and is used clinically for the treatment of spasticity associated with brain and spinal cord injuries. Synthesis and GABAB receptor agonist activity of certain amino acids structurally related to baclofen (2) are reported. (RS)-4-amino-3-(4- ethynylphenyl)butanoic acid hydrochloride (1b) showed GABAB receptor agonist activity with EC50 = 240 μM whereas (RS)-4-amino-3-(4-iodophenyl)butanoic acid hydrochloride (1c) emerged as the best GABAB receptor agonist congener in the synthesized compounds with ED50 = 32 μM.",

author = "M.I. Attia and C. Herdeis and Hans Br{\"a}uner-Osborne",

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T1 - Synthesis and pharmacological characterization of certain baclofen analogues

AU - Attia, M.I.

AU - Herdeis, C.

AU - Bräuner-Osborne, Hans

PY - 2012

Y1 - 2012

N2 - (RS)-4-Amino-3-(4-chlorophenyl)butanoic acid (baclofen, 2) is the prototypic selective GABABR agonist and is used clinically for the treatment of spasticity associated with brain and spinal cord injuries. Synthesis and GABAB receptor agonist activity of certain amino acids structurally related to baclofen (2) are reported. (RS)-4-amino-3-(4- ethynylphenyl)butanoic acid hydrochloride (1b) showed GABAB receptor agonist activity with EC50 = 240 μM whereas (RS)-4-amino-3-(4-iodophenyl)butanoic acid hydrochloride (1c) emerged as the best GABAB receptor agonist congener in the synthesized compounds with ED50 = 32 μM.

AB - (RS)-4-Amino-3-(4-chlorophenyl)butanoic acid (baclofen, 2) is the prototypic selective GABABR agonist and is used clinically for the treatment of spasticity associated with brain and spinal cord injuries. Synthesis and GABAB receptor agonist activity of certain amino acids structurally related to baclofen (2) are reported. (RS)-4-amino-3-(4- ethynylphenyl)butanoic acid hydrochloride (1b) showed GABAB receptor agonist activity with EC50 = 240 μM whereas (RS)-4-amino-3-(4-iodophenyl)butanoic acid hydrochloride (1c) emerged as the best GABAB receptor agonist congener in the synthesized compounds with ED50 = 32 μM.

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M3 - Journal article

AN - SCOPUS:84871637222

SN - 1842-3582

VL - 8

SP - 139

EP - 149

JO - Digest Journal of Nanomaterials and Biostructures

JF - Digest Journal of Nanomaterials and Biostructures

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Synthesis and pharmacological characterization of certain baclofen analogues

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