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• W2038091402 abstract "γ-aminobutyric acid (GABA) plays important roles in the central nervous system, acting as a neurotransmitter on both ionotropic ligand-gated Cl--channels, and metabotropic G-protein coupled receptors (GPCRs). These two types of receptors called GABAA (and C) and GABAB are the targets of major therapeutic drugs such as the anxiolytic benzodiazepines, and antispastic drug baclofen (lioresal®), respectively. Although the multiplicity of GABAA receptors offer a number of possibilities to discover new and more selective drugs, the molecular characterization of the GABAB receptor revealed a unique, though complex, heterodimeric GPCR. High throughput screening strategies carried out in pharmaceutical industries, helped identifying new compounds positively modulating the activity of the GABAB receptor. These molecules, almost devoid of apparent activity when applied alone, greatly enhance both the potency and efficacy of GABAB agonists. As such, in contrast to baclofen that constantly activates the receptor everywhere in the brain, these positive allosteric modulators induce a large increase in GABAB-mediated responses only WHERE and WHEN physiologically needed. Such compounds are then well adapted to help GABA to activate its GABAB receptors, like benzodiazepines favor GABAA receptor activation. In this review, the way of action of these molecules will be presented in light of our actual knowledge of the activation mechanism of the GABAB receptor. We will then show that, as expected, these molecules have more pronounced in vivo responses and less side effects than pure agonists, offering new potential therapeutic applications for this new class of GABAB ligands. Keywords: Baclofen, anxiety, drug addiction, allosteric modulators, class C GPCRs" @default.
• W2038091402 created "2016-06-24" @default.
• W2038091402 creator A5019678940 @default.
• W2038091402 creator A5035290703 @default.
• W2038091402 date "2007-09-01" @default.
• W2038091402 modified "2023-10-18" @default.
• W2038091402 title "Allosteric Modulators of GABAB Receptors: Mechanism of Action and Therapeutic Perspective" @default.
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• W2038091402 doi "https://doi.org/10.2174/157015907781695919" @default.
• W2038091402 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2656813" @default.
• W2038091402 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19305802" @default.
• W2038091402 hasPublicationYear "2007" @default.
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