GABAB-Agonistic Activity of Certain Baclofen Homologues
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چکیده
منابع مشابه
GABA(B)-agonistic activity of certain baclofen homologues.
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 (...
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The role of GABA(B) receptors in sleep is still poorly understood. GHB (γ-hydroxybutyric acid) targets these receptors and is the only drug approved to treat the sleep disorder narcolepsy. GABA(B) receptors are obligate dimers comprised of the GABA(B2) subunit and either one of the two GABA(B1) subunit isoforms, GABA(B1a) and GABA(B1b). To better understand the role of GABA(B) receptors in slee...
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MOHAMED I. ATTIA, CLAUS HERDEIS, HANS BRÄUNER-OSBORNE Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia Department of Pharmaceutical Chemistry, Institute of Pharmacy and Food Chemistry, Würzburg University, Am Hubland, 97074, Würzburg, Germany Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhag...
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Baclofen is a GABAB receptor agonist commonly used to relief spasticity related to motor disorders. The effects of baclofen on voluntary motor output are limited and not yet understood. Using noninvasive transcranial magnetic and electrical stimulation techniques, we examined electrophysiological measures probably involving GABAB (long-interval intracortical inhibition and the cortical silent p...
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CXCR4, a receptor for the chemokine CXCL12 (stromal-cell derived factor-1α), is a G-protein-coupled receptor (GPCR), expressed in the immune and CNS and integrally involved in various neurological disorders. The GABAB receptor is also a GPCR that mediates metabotropic action of the inhibitory neurotransmitter GABA and is located on neurons and immune cells as well. Using diverse approaches, we ...
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ژورنال
عنوان ژورنال: Molecules
سال: 2013
ISSN: 1420-3049
DOI: 10.3390/molecules180910266