{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,14]],"date-time":"2026-10-14T04:06:36Z","timestamp":1791950796488,"version":"4.3.4"},"reference-count":115,"publisher":"MDPI AG","issue":"13","license":[{"start":{"date-parts":[[2020,7,7]],"date-time":"2020-07-07T00:00:00Z","timestamp":1594080000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"the Polish-Norwegian Research Program","award":["Pol-Nor\/198887\/73\/2013"],"award-info":[{"award-number":["Pol-Nor\/198887\/73\/2013"]}]},{"name":"HelseNord","award":["HNF1426-18"],"award-info":[{"award-number":["HNF1426-18"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>The \u03b3-aminobutyric acid (GABA) type B receptor (GABAB-R) belongs to class C of the G-protein coupled receptors (GPCRs). Together with the GABAA receptor, the receptor mediates the neurotransmission of GABA, the main inhibitory neurotransmitter in the central nervous system (CNS). In recent decades, the receptor has been extensively studied with the intention being to understand pathophysiological roles, structural mechanisms and develop drugs. The dysfunction of the receptor is linked to a broad variety of disorders, including anxiety, depression, alcohol addiction, memory and cancer. Despite extensive efforts, few compounds are known to target the receptor, and only the agonist baclofen is approved for clinical use. The receptor is a mandatory heterodimer of the GABAB1 and GABAB2 subunits, and each subunit is composed of an extracellular Venus Flytrap domain (VFT) and a transmembrane domain of seven \u03b1-helices (7TM domain). In this review, we briefly present the existing knowledge about the receptor structure, activation and compounds targeting the receptor, emphasizing the role of the receptor in previous and future drug design and discovery efforts.<\/jats:p>","DOI":"10.3390\/molecules25133093","type":"journal-article","created":{"date-parts":[[2020,7,7]],"date-time":"2020-07-07T10:41:09Z","timestamp":1594118469000},"page":"3093","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":114,"title":["The GABAB Receptor\u2014Structure, Ligand Binding and Drug Development"],"prefix":"10.3390","volume":"25","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8004-6671","authenticated-orcid":false,"given":"Linn Samira Mari","family":"Evenseth","sequence":"first","affiliation":[{"name":"Molecular Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Sciences, UiT The Arctic University of Norway, NO-9037 Troms\u00f8, Norway"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3898-1193","authenticated-orcid":false,"given":"Mari","family":"Gabrielsen","sequence":"additional","affiliation":[{"name":"Molecular Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Sciences, UiT The Arctic University of Norway, NO-9037 Troms\u00f8, Norway"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3290-3736","authenticated-orcid":false,"given":"Ingebrigt","family":"Sylte","sequence":"additional","affiliation":[{"name":"Molecular Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Sciences, UiT The Arctic University of Norway, NO-9037 Troms\u00f8, Norway"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2020,7,7]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"149","DOI":"10.1038\/290149a0","article-title":"3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain","volume":"290","author":"Hill","year":"1981","journal-title":"Nature"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"92","DOI":"10.1038\/283092a0","article-title":"(\u2013)Baclofen decreases neurotransmitter release in the mammalian CNS by an action at a novel GABA receptor","volume":"283","author":"Bowery","year":"1980","journal-title":"Nature"},{"key":"ref_3","first-page":"444","article-title":"Baclofen: A selective agonist for a novel type of GABA receptor proceedings","volume":"67","author":"Bowery","year":"1979","journal-title":"Br. 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