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14-September-2008 18:02:42 - GABAB receptor gamma-aminobutyric acid GABA B receptor, 1 Identifiers Symbol GABBR1 Entrez 2550 HUGO 4070 OMIM 603540 RefSeq NM_021905 UniProt Q9UBS5 Other data Locus Chr. 6 p21.3 gamma-aminobutyric acid GABA B receptor, 2 Identifiers Symbol GABBR2 Alt. Symbols GPR51 Entrez 9568 HUGO 4507 OMIM 607340 RefSeq NM_005458 UniProt O75899 Other data Locus Chr. 9 q22.1-22.3 The correct title of this article is GABAB receptor. It features superscript or subscript characters that are substituted or omitted because of technical limitations. GABAB receptors GABABR are metabotropic transmembrane receptors for gamma-aminobutyric acid GABA that are linked via G-proteins to potassium channels.1 These receptors are found in the central and peripheral autonomic nervous system.2 Contents 1 Functions 2 Structure 3 Agonists and antagonists 4 See also 5 References 6 External links Functions They can stimulate the opening of K+ channels which brings the neuron closer to the equilibrium potential of K+, hyperpolarising the neuron. This prevents sodium channels from opening, action potentials from firing, and VDCCs from opening, and so stops neurotransmitter release. Thus GABAB receptors are considered inhibitory receptors. GABAB receptors can also reduce the activity of adenylyl cyclase and decrease the cell's conductance to Ca2+.2 GABAB receptors are involved in behavioral actions of ethanol, 3 gamma-Hydroxybutyric acid GHB,4 and possibly in pain.5 Recent research suggests that these receptors may play an important developmental role. 6 Structure GABABRs are similar in structure to and in the same receptor family with metabotropic glutamate receptors.7 There are two subtypes of the receptor, GABAB1 and GABAB2,82 and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini.27 It is speculated that binding of GABA causes the subunits to swing shut around the agonist like a venus fly trap.2 Agonists and antagonists GABA GABA Baclofen Baclofen Baclofen is a GABA analogue which acts as a selective agonist of GABAB receptors, and is used as a muscle relaxant. However, it can aggravate absence seizures, and so is not used in epilepsy. Saclofen, phaclofen and SCH-50911 are selective GABAB antagonists. See also GABA receptor GABAA receptor GABAC receptor References ^ Chen K, Li H, Ye N, Zhang J, Wang J 2005. Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Res Bull 67 4: 310-8. doi:10.1016/j.brainresbull.2005.07.004. PMID 16182939. ^ a b c d e Martin I.L., and Dunn S.M.J. 2002. GABA receptors Tocris Cookson Ltd. ^ Dzitoyeva S, Dimitrijevic N, Manev H 2003. Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence. Proc Natl Acad Sci U S A 100 9: 5485-90. doi:10.1073/pnas.0830111100. PMID 12692303. ^ Dimitrijevic N, Dzitoyeva S, Satta R, Imbesi M, Yildiz S, Manev H 2005. Drosophila GABAB receptors are involved in behavioral effects of gamma-hydroxybutyric acid GHB. Eur J Pharmacol 519 3: 246-52. doi:10.1016/j.ejphar.2005.07.016. PMID 16129424. ^ Manev H, Dimitrijevic N 2004. Drosophila model for in vivo pharmacological analgesia research. Eur J Pharmacol 491 2-3: 207-8. doi:10.1016/j.ejphar.2004.03.030. PMID 15140638. ^ Dzitoyeva S, Gutnov A, Imbesi M, Dimitrijevic N, Manev H 2005. Developmental role of GABAB1 receptors in Drosophila. Brain Res Dev Brain Res 158 1-2: 111-4. doi:10.1016/j.devbrainres.2005.06.005. PMID 16054235. ^ a b MRC Medical Research Council. 2003. Glutamate receptors: Structures and functions. University of Brisotol Centre for Synaptic Plasticity. ^ Purves D., Augustine G.J., Fitzpatrick D., Katz L.C., LaMantia A.S., McNamara J.O., and Williams S.M. 2001. Neuroscience, Second ion. Sinauer Associates, Inc. External links IUPHAR GPCR Database - GABAB Receptors v d e Transmembrane receptor: G protein-coupled receptors Class A: Rhodopsin like Adrenergic α1 A, B, D, α2 A, B, C, β1, β2, β3 Eicosanoid CysLT 1, 2, LTB4 1, 2, FPRL1, OXE, Prostaglandin DP, EP 1, 2, 3, 4, PGF, Prostacyclin, Thromboxane Neuropeptide B/W 1, 2, FF 1, 2, S, Y 1, 2, 4, 5 Orphan GPR 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182 Purinergics Adenosine A1, A2a, A2b, A3, P2Y, 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14 Serotonin all but 5-HT3 5-HT1 A, B, D, E, F, 5-HT2 A, B, C, 5-HT 4, 5A, 6, 7 Other Acetylcholine M1, M2, M3, M4, M5 - Adrenomedullin - Anaphylatoxin C3a, C5a - Angiotensin 1, 2 - Apelin - Bile acid - Bombesin BRS3, GRPR, NMBR - Bradykinin B1, B2 - Cannabinoid CB1, CB2 - Chemokine - Cholecystokinin A, B - Dopamine D1, D2, D3, D4, D5 - EBI2 - Endothelin A, B - Estrogen - Formyl peptide 1, L1, L2 - Free fatty acid 1, 2, 3, 4 - FSH - Galanin 1, 2, 3 - Gonadotropin-releasing hormone 1, 2 - Ghrelin - Histamine H1, H2, H3, H4 - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid 1, 2, 3, 4, 5, 6, 7, 8 - MAS 1, 1L, D, E, F, G, X1, X2, X3, X4 - Melanocortin 1, 2, 3, 4, 5 - MCHR 1, 2 - Melatonin 1A, 1B- Motilin - neuromedin B, U 1, 2 - Neurotensin 1, 2 - Opioid Delta, Kappa, Mu, Nociceptin, but not Sigma - Olfactory - Opsin 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH - Orexin 1, 2 - Oxytocin - Oxoglutarate - PAF - Prokineticin 1, 2 - Prolactin-releasing peptide - Protease-activated 1, 2, 3, 4 - Relaxin 1, 2, 3, 4 - Somatostatin 1, 2, 3, 4, 5 - SREB - Succinate - TAAR 1, 2, 3, 5, 6, 8, 9 - Tachykinin 1, 2, 3 - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin 1A, 1B, 2 Class B: Secretin like Brain-specific angiogenesis inhibitor 1, 2, 3 - Cadherin 1, 2, 3 - Calcitonin - CD97 - Corticotropin-releasing hormone 1, 2 - EMR 1, 2, 3 - Glucagon GR, GIPR, GLP1R, GLP2R - Growth hormone releasing hormone - PACAPR1- GPR 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157 - Latrophilin 1, 2, 3, ELTD1 - Parathyroid hormone 1, 2 - Secretin - Vasoactive intestinal peptide 1, 2 Class C: Metabotropic glutamate / pheromone Calcium-sensing receptor - GABA B 1, 2 - Glutamate receptor Metabotropic glutamate 1, 2, 3, 4, 5, 6, 7, 8 - GPRC6A - GPR 156, 158, 179 - RAIG 1, 2, 3, 4 - Taste receptors TAS1R 1, 2, 3 TAS2R 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50 Frizzled / Smoothened Frizzled 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 - Smoothened Retrieved from http://en..org/wiki/GABAB_receptor Categories: Genes on chromosome 6 | Genes on chromosome 9 | Transmembrane receptorsHidden category: Protein pages needing a picture Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages УкраїнÑ?ька Français This page was last modified on 6 July 2008, at 02:34
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