The receptors were first named in 1981 when their distribution in the CNS was determined, which was determined byNorman Bowery and his team using radioactively labelledbaclofen.[3]
GABAB receptors are involved in behavioral actions ofethanol,[5][6]gamma-hydroxybutyric acid (GHB),[7] and possibly in pain.[8] Recent research suggests that these receptors may play an important developmental role.[9]
Receptor dimer, inactive apo state, cartoon representation
GABAB Receptors are similar in structure to and in the same receptor family withmetabotropic glutamate receptors.[10] There are two subunits of the receptor,GABAB1 andGABAB2,[11] and these appear to assemble as obligateheterodimers in neuronal membranes by linking up by their intracellularC termini.[10] In the mammalian brain, two predominant, differentially expressedisoforms of the GABAB1 are transcribed from the Gabbr1 gene, GABAB(1a) and GABAB(1b), which are conserved in different species including humans.[12] This might potentially offer more complexity in terms of the function due to different composition of the receptor.[12]Cryo-electron microscopy structures of the full length GABAB receptor in different conformational states from inactiveapo to fully active have been obtained. Unlike Class A and B GPCRs, phospholipids bind within the transmembrane bundles and allosteric modulators bind at the interface ofGABAB1 andGABAB2 subunits.[13][14][15][16][17][18][19]
^Chen K, Li HZ, Ye N, Zhang J, Wang JJ (October 2005). "Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro".Brain Research Bulletin.67 (4):310–8.doi:10.1016/j.brainresbull.2005.07.004.PMID16182939.S2CID6433030.
^Dimitrijevic N, Dzitoyeva S, Satta R, Imbesi M, Yildiz S, Manev H (September 2005). "Drosophila GABA(B) receptors are involved in behavioral effects of gamma-hydroxybutyric acid (GHB)".European Journal of Pharmacology.519 (3):246–52.doi:10.1016/j.ejphar.2005.07.016.PMID16129424.
^Manev H, Dimitrijevic N (May 2004). "Drosophila model for in vivo pharmacological analgesia research".European Journal of Pharmacology.491 (2–3):207–8.doi:10.1016/j.ejphar.2004.03.030.PMID15140638.
^Dzitoyeva S, Gutnov A, Imbesi M, Dimitrijevic N, Manev H (August 2005). "Developmental role of GABAB(1) receptors in Drosophila".Brain Research. Developmental Brain Research.158 (1–2):111–4.doi:10.1016/j.devbrainres.2005.06.005.PMID16054235.
^Kimura T, Saunders PA, Kim HS, Rheu HM, Oh KW, Ho IK (January 1994). "Interactions of ginsenosides with ligand-bindings of GABA(A) and GABA(B) receptors".General Pharmacology.25 (1):193–9.doi:10.1016/0306-3623(94)90032-9.PMID8026706.
^Froestl W, Gallagher M, Jenkins H, Madrid A, Melcher T, Teichman S, et al. (October 2004). "SGS742: the first GABA(B) receptor antagonist in clinical trials".Biochemical Pharmacology.68 (8):1479–87.doi:10.1016/j.bcp.2004.07.030.PMID15451390.
^Bullock R (January 2005). "SGS-742 Novartis".Current Opinion in Investigational Drugs.6 (1):108–13.PMID15675610.
