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Gene Review

GABBR1  -  gamma-aminobutyric acid (GABA) B receptor, 1

Homo sapiens

Synonyms: GABA-B receptor 1, GABA-B-R1, GABA-BR1, GABABR1, GABBR1-3, ...
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Disease relevance of GABBR1


Psychiatry related information on GABBR1


High impact information on GABBR1


Chemical compound and disease context of GABBR1


Biological context of GABBR1


Anatomical context of GABBR1


Associations of GABBR1 with chemical compounds

  • Baclofen action is inhibited by the GABABR antagonist, 2-hydroxysaclofen [23].
  • The effect of a maximally effective concentration of FF (30%, vol/vol) was significantly suppressed by bicuculline, a GABAA receptor antagonist, and saclofen, a GABAB receptor antagonist, added concomitantly [25].
  • It has recently been demonstrated that GABABR indeed modulates alpha amino-3-hydroxy-5-methyl-4-isoxalone propionate-type ionotropic glutamate receptor (AMPAR)-mediated and type-1 metabotropic glutamate receptor (mGluR1)-mediated signaling [26].
  • Importantly, GABABR2 receptors can form a heteromeric assembly with GABABR1 proteins to operate as a heterodimer that displays robust coupling to inward-rectifying K+ channels, as well as inhibition of forskolin-stimulated adenylate cyclase activity [7].
  • On the other hand, application of 500 microM muscimol or 1 mM baclofen, GABAA and GABAB receptor agonists, respectively, were completely without effect [27].

Physical interactions of GABBR1


Other interactions of GABBR1


Analytical, diagnostic and therapeutic context of GABBR1


  1. The GABBR1 locus and the G1465A variant is not associated with temporal lobe epilepsy preceded by febrile seizures. Ma, S., Abou-Khalil, B., Sutcliffe, J.S., Haines, J.L., Hedera, P. BMC Med. Genet. (2005) [Pubmed]
  2. Human gamma-aminobutyric acid type B receptors are differentially expressed and regulate inwardly rectifying K+ channels. Kaupmann, K., Schuler, V., Mosbacher, J., Bischoff, S., Bittiger, H., Heid, J., Froestl, W., Leonhard, S., Pfaff, T., Karschin, A., Bettler, B. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  3. Heterodimerization of a functional GABAB receptor is mediated by parallel coiled-coil alpha-helices. Kammerer, R.A., Frank, S., Schulthess, T., Landwehr, R., Lustig, A., Engel, J. Biochemistry (1999) [Pubmed]
  4. Mapping, genomic structure, and polymorphisms of the human GABABR1 receptor gene: evaluation of its involvement in idiopathic generalized epilepsy. Peters, H.C., Kämmer, G., Volz, A., Kaupmann, K., Ziegler, A., Bettler, B., Epplen, J.T., Sander, T., Riess, O. Neurogenetics (1998) [Pubmed]
  5. Evidence for the gamma-amino-butyric acid type B receptor 1 (GABBR1) gene as a susceptibility factor in obsessive-compulsive disorder. Zai, G., Arnold, P., Burroughs, E., Barr, C.L., Richter, M.A., Kennedy, J.L. Am. J. Med. Genet. B Neuropsychiatr. Genet. (2005) [Pubmed]
  6. Human GABA(B) receptor 1 gene: eight novel sequence variants. Hisama, F.M., Gruen, J.R., Choi, J., Huseinovic, M., Grigorenko, E.L., Pauls, D., Mattson, R.H., Gelernter, J., Wood, F.B., Goei, V.L. Hum. Mutat. (2001) [Pubmed]
  7. Recent advances in GABAB receptors: from pharmacology to molecular biology. Ong, J., Kerr, D.I. Acta Pharmacol. Sin. (2000) [Pubmed]
  8. The spinal GABA system modulates burst frequency and intersegmental coordination in the lamprey: differential effects of GABAA and GABAB receptors. Tegnér, J., Matsushima, T., el Manira, A., Grillner, S. J. Neurophysiol. (1993) [Pubmed]
  9. Baclofen administration for the treatment of affective disorders in alcoholic patients. Krupitsky, E.M., Burakov, A.M., Ivanov, V.B., Krandashova, G.F., Lapin, I.P., Grinenko AJa, n.u.l.l., Borodkin YuS, n.u.l.l. Drug and alcohol dependence. (1993) [Pubmed]
  10. Pharmacologic rescue of lethal seizures in mice deficient in succinate semialdehyde dehydrogenase. Hogema, B.M., Gupta, M., Senephansiri, H., Burlingame, T.G., Taylor, M., Jakobs, C., Schutgens, R.B., Froestl, W., Snead, O.C., Diaz-Arrastia, R., Bottiglieri, T., Grompe, M., Gibson, K.M. Nat. Genet. (2001) [Pubmed]
  11. Heterodimerization is required for the formation of a functional GABA(B) receptor. White, J.H., Wise, A., Main, M.J., Green, A., Fraser, N.J., Disney, G.H., Barnes, A.A., Emson, P., Foord, S.M., Marshall, F.H. Nature (1998) [Pubmed]
  12. Facilitation of the induction of long-term potentiation by GABAB receptors. Mott, D.D., Lewis, D.V. Science (1991) [Pubmed]
  13. Electrophysiology of GABAA and GABAB receptor subtypes. Bormann, J. Trends Neurosci. (1988) [Pubmed]
  14. Omega-conotoxin sensitivity and presynaptic inhibition of glutamatergic sensory neurotransmission in vitro. Gruner, W., Silva, L.R. J. Neurosci. (1994) [Pubmed]
  15. Mechanism of action of gamma-aminobutyric acid on frog melanotrophs. Desrues, L., Vaudry, H., Lamacz, M., Tonon, M.C. J. Mol. Endocrinol. (1995) [Pubmed]
  16. Comparative protective effects of vinconate, baclofen, and pentobarbital against neuronal damage following repeated brief cerebral ischemia in the gerbil brain. Araki, T., Kato, H., Kogure, K. Research in experimental medicine. Zeitschrift für die gesamte experimentelle Medizin einschliesslich experimenteller Chirurgie. (1991) [Pubmed]
  17. The gene encoding GABBR1 is not associated with childhood absence epilepsy in the Chinese Han population. Lu, J., Chen, Y., Pan, H., Zhang, Y., Wu, H., Xu, K., Liu, X., Jiang, Y., Bao, X., Shen, Y., Wu, X. Neurosci. Lett. (2003) [Pubmed]
  18. Lack of association between a GABA receptor 1 gene polymorphism and temporal lobe epilepsy. Stogmann, E., Zimprich, A., Baumgartner, C., Gleiss, A., Zimprich, F. Epilepsia (2006) [Pubmed]
  19. Delineating a Ca2+ binding pocket within the venus flytrap module of the human calcium-sensing receptor. Silve, C., Petrel, C., Leroy, C., Bruel, H., Mallet, E., Rognan, D., Ruat, M. J. Biol. Chem. (2005) [Pubmed]
  20. Phosphorylation and chronic agonist treatment atypically modulate GABAB receptor cell surface stability. Fairfax, B.P., Pitcher, J.A., Scott, M.G., Calver, A.R., Pangalos, M.N., Moss, S.J., Couve, A. J. Biol. Chem. (2004) [Pubmed]
  21. Gamma-hydroxybutyrate reduces mitogen-activated protein kinase phosphorylation via GABA B receptor activation in mouse frontal cortex and hippocampus. Ren, X., Mody, I. J. Biol. Chem. (2003) [Pubmed]
  22. Identification of a GABAB receptor subunit, gb2, required for functional GABAB receptor activity. Ng, G.Y., Clark, J., Coulombe, N., Ethier, N., Hebert, T.E., Sullivan, R., Kargman, S., Chateauneuf, A., Tsukamoto, N., McDonald, T., Whiting, P., Mezey, E., Johnson, M.P., Liu, Q., Kolakowski, L.F., Evans, J.F., Bonner, T.I., O'Neill, G.P. J. Biol. Chem. (1999) [Pubmed]
  23. Molecular identification of the human GABABR2: cell surface expression and coupling to adenylyl cyclase in the absence of GABABR1. Martin, S.C., Russek, S.J., Farb, D.H. Mol. Cell. Neurosci. (1999) [Pubmed]
  24. Comparative cellular distribution of GABAA and GABAB receptors in the human basal ganglia: immunohistochemical colocalization of the alpha 1 subunit of the GABAA receptor, and the GABABR1 and GABABR2 receptor subunits. Waldvogel, H.J., Billinton, A., White, J.H., Emson, P.C., Faull, R.L. J. Comp. Neurol. (2004) [Pubmed]
  25. Human follicular fluid stimulates the sperm acrosome reaction by interacting with the gamma-aminobutyric acid receptors. Burrello, N., Vicari, E., D'Amico, L., Satta, A., D'Agata, R., Calogero, A.E. Fertil. Steril. (2004) [Pubmed]
  26. GABA(B) receptor-mediated modulation of glutamate signaling in cerebellar Purkinje cells. Tabata, T., Kano, M. Cerebellum (2006) [Pubmed]
  27. Effects of gamma-aminobutyric acid on skate retinal horizontal cells: evidence for an electrogenic uptake mechanism. Malchow, R.P., Ripps, H. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
  28. Assembly-dependent surface targeting of the heterodimeric GABAB Receptor is controlled by COPI but not 14-3-3. Brock, C., Boudier, L., Maurel, D., Blahos, J., Pin, J.P. Mol. Biol. Cell (2005) [Pubmed]
  29. A novel locus for autosomal dominant non-syndromic hearing loss, DFNA31, maps to chromosome 6p21.3. Snoeckx, R.L., Kremer, H., Ensink, R.J., Flothmann, K., de Brouwer, A., Smith, R.J., Cremers, C.W., Van Camp, G. J. Med. Genet. (2004) [Pubmed]
  30. GABA (gamma-amino-butyric acid) neurotransmission: identification and fine mapping of the human GABAB receptor gene. Grifa, A., Totaro, A., Rommens, J.M., Carella, M., Roetto, A., Borgato, L., Zelante, L., Gasparini, P. Biochem. Biophys. Res. Commun. (1998) [Pubmed]
  31. Molecular cloning of human GABABR1 and its tissue distribution. Makoff, A. Brain Res. Mol. Brain Res. (1999) [Pubmed]
  32. Association analysis of exonic variants of the gene encoding the GABAB receptor and idiopathic generalized epilepsy. Sander, T., Peters, C., Kämmer, G., Samochowiec, J., Zirra, M., Mischke, D., Ziegler, A., Kaupmann, K., Bettler, B., Epplen, J.T., Riess, O. Am. J. Med. Genet. (1999) [Pubmed]
  33. Gamma-hydroxybutyrate: an overview of the pros and cons for it being a neurotransmitter and/or a useful therapeutic agent. Cash, C.D. Neuroscience and biobehavioral reviews. (1994) [Pubmed]
  34. Developmental changes of agonist affinity at GABABR1 receptor variants in rat brain. Malitschek, B., Rüegg, D., Heid, J., Kaupmann, K., Bittiger, H., Fröstl, W., Bettler, B., Kuhn, R. Mol. Cell. Neurosci. (1998) [Pubmed]
  35. Repeated administration of the GABAB receptor agonist CGP44532 decreased nicotine self-administration, and acute administration decreased cue-induced reinstatement of nicotine-seeking in rats. Paterson, N.E., Froestl, W., Markou, A. Neuropsychopharmacology (2005) [Pubmed]
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