GABAB受容体、GABABレセプター、GABA-B受容体、GABA-Bレセプター
- 関
- GABA-B receptor
WordNet
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/10/11 00:31:39」(JST)
[Wiki en表示]
| 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 |
GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) that are linked via G-proteins to potassium channels.[1] The changing potassium concentrations hyperpolarize the cell at the end of an action potential. The reversal potential the GABAB-mediated IPSP is -100 mV, which is much more hyperpolarized than the GABAA IPSP. GABAB receptors are found in the central as well as in the autonomic division of the peripheral nervous system.[citation needed]
Contents
- 1 Functions
- 2 Structure
- 3 Selective Ligands
- 3.1 Agonists
- 3.2 Positive Allosteric Modulators
- 3.3 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+.
GABAB receptors are involved in behavioral actions of ethanol,[2] gamma-Hydroxybutyric acid (GHB),[3] and possibly in pain.[4] Recent research suggests that these receptors may play an important developmental role.[5]
Structure
GABAB Receptors are similar in structure to and in the same receptor family with metabotropic glutamate receptors.[6] There are two subtypes of the receptor, GABAB1 and GABAB2,[7] and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini.[6]
It is speculated that binding of GABA causes the subunits to swing shut around the agonist like a venus fly trap.
Selective Ligands
Agonists
- GABA
- 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.
- gamma-Hydroxybutyrate (GHB)
- Phenibut
- 3-Aminopropylphosphinic acid
- Lesogaberan
- SKF-97541: 3-Aminopropyl(methyl)phosphinic acid, 10x more potent than baclofen as GABAB agonist, but also GABAC antagonist
- CGP-44532
Positive Allosteric Modulators
- CGP-7930[8][9]
- BHFF
- Fendiline
- BHF-177[10]
- BSPP
- GS-39783[11]
Antagonists
- 2-OH-saclofen
- Saclofen
- Phaclofen
- SCH-50911
- CGP-35348
- CGP-52432: 3-([(3,4-Dichlorophenyl)methyl]amino]propyl) diethoxymethyl)phosphinic acid, CAS# 139667-74-6
- CGP-55845: (2S)-3-([(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl)(phenylmethyl)phosphinic acid, CAS# 149184-22-5
- SGS-742 [12][13]
See also
- GABA receptor
- GABAA receptor
- GABAA-ρ receptor
References
- ^ Chen K, Li HZ, Ye N, Zhang J, Wang JJ (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.
- ^ 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 USA 100 (9): 5485–90. Bibcode:2003PNAS..100.5485D. doi:10.1073/pnas.0830111100. PMC 154371. PMID 12692303.
- ^ Dimitrijevic N, Dzitoyeva S, Satta R, Imbesi M, Yildiz S, Manev H (2005). "Drosophila GABA(B) 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 GABAB(1) 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 Edition. Sinauer Associates, Inc.
- ^ Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, Bettler B, Kaupmann K (November 2001). "Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501". Mol. Pharmacol. 60 (5): 963–71. PMID 11641424.
- ^ Adams CL, Lawrence AJ (2007). "CGP7930: a positive allosteric modulator of the GABAB receptor". CNS Drug Rev 13 (3): 308–16. doi:10.1111/j.1527-3458.2007.00021.x. PMID 17894647.
- ^ Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A (July 2008). "Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats". J. Pharmacol. Exp. Ther. 326 (1): 306–14. doi:10.1124/jpet.108.139204. PMC 2574924. PMID 18445779.
- ^ Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K (October 2003). "N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function". J. Pharmacol. Exp. Ther. 307 (1): 322–30. doi:10.1124/jpet.103.053074. PMID 12954816.
- ^ Froestl W, Gallagher M, Jenkins H, Madrid A, Melcher T, Teichman S, Mondadori CG, Pearlman R (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. PMID 15451390.
- ^ Bullock R (January 2005). "SGS-742 Novartis". Current Opinion in Investigational Drugs (London, England : 2000) 6 (1): 108–13. PMID 15675610.
External links
|
Cell surface receptor: G protein-coupled receptors
|
|
|
|
|
|
Class B: Secretin like
|
|
| Orphan |
- GPR (56
- 64
- 97
- 98
- 110
- 111
- 112
- 113
- 114
- 115
- 116
- 123
- 124
- 125
- 126
- 128
- 133
- 143
- 144
- 155
- 157)
|
|
| Other |
- Brain-specific angiogenesis inhibitor (1
- 2
- 3)
- Cadherin (1
- 2
- 3)
- Calcitonin
- CALCRL
- CD97
- Corticotropin-releasing hormone (1
- 2)
- EMR (1
- 2
- 3)
- Glucagon (GR
- GIPR
- GLP1R
- GLP2R)
- Growth hormone releasing hormone
- PACAPR1
- GPR
- Latrophilin (1
- 2
- 3
- ELTD1)
- Methuselah-like proteins
- Parathyroid hormone (1
- 2)
- Secretin
- Vasoactive intestinal peptide (1
- 2)
|
|
|
|
|
Class C: Metabotropic glutamate / pheromone
|
|
| Taste |
- TAS1R (1
- 2
- 3)
- TAS2R (1
- 3
- 4
- 5
- 7
- 8
- 9
- 10
- 13
- 14
- 16
- 19
- 20
- 30
- 31
- 38
- 39
- 40
- 41
- 42
- 43
- 45
- 46
- 50
- 60)
|
|
| Other |
- 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)
|
|
|
|
|
Class F: Frizzled / Smoothened
|
|
| Frizzled |
- Frizzled (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10)
|
|
| Smoothened |
|
|
|
|
|
B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Striking differences in synaptic facilitation along the dorsoventral axis of the hippocampus.
- Papatheodoropoulos C1.
- Neuroscience.Neuroscience.2015 Aug 20;301:454-70. doi: 10.1016/j.neuroscience.2015.06.029. Epub 2015 Jun 23.
- Hippocampus displays functional heterogeneity along its long axis which has been interpreted in terms of segregation of inputs. Recent evidence has shown that there are also important differences in the organization of the local neuronal circuitry between the dorsal (DH) and the ventral hippocampus
- PMID 26116517
- Stress-induced inhibition of LH pulses in female rats: role of GABA in arcuate nucleus.
- Li X1, Shao B2, Lin C2, O'Byrne KT2, Lin Y3.
- Journal of molecular endocrinology.J Mol Endocrinol.2015 Aug;55(1):9-19. doi: 10.1530/JME-15-0084. Epub 2015 May 21.
- Stress exerts profound inhibitory effects on reproductive function by suppression of the pulsatile release of GnRH and therefore LH. Besides the corticotrophin-releasing factor (CRF), this effect also might be mediated via GABAergic signaling within the arcuate nucleus (ARC) since its inhibitory eff
- PMID 25999179
- Chronic baclofen desensitizes GABAB-mediated G-protein activation and stimulates phosphorylation of kinases in mesocorticolimbic rat brain.
- Keegan BM1, Beveridge TJ1, Pezor JJ2, Xiao R1, Sexton T1, Childers SR1, Howlett AC3.
- Neuropharmacology.Neuropharmacology.2015 Aug;95:492-502. doi: 10.1016/j.neuropharm.2015.02.021. Epub 2015 Feb 25.
- The GABAB receptor is a therapeutic target for CNS and neuropathic disorders; however, few preclinical studies have explored effects of chronic stimulation. This study evaluated acute and chronic baclofen treatments on GABAB-activated G-proteins and signaling protein phosphorylation as indicators of
- PMID 25724082
Japanese Journal
- Glutamate Input in the Dorsal Raphe Nucleus As a Determinant of Escalated Aggression in Male Mice
- Takahashi Aki,Lee Ray X.,Iwasato Takuji,Itohara Shigeyoshi,Arima Hiroshi,Bettler Bernhard,Miczek Klaus A.,Koide Tsuyoshi
- The Journal of neuroscience 35(16), 6452-6463, 2015-04
- … Previously, we observed that microinjection of the GABAB receptor agonist baclofen into the DRN escalates aggressive behavior in male mice. … Here, we used a serotonin (5-HT) neuron-specific GABAB receptor knock-out mouse to demonstrate that baclofen acts on nonserotonergic neurons to escalate aggression. …
- NAID 120005611479
- RBL-2H3細胞およびラット腹腔滲出細胞に対するγ-アミノ酪酸のヒスタミン遊離抑制作用
- 川崎 梓,原 崇,城 斗志夫
- 日本食品科学工学会誌 61(8), 362-366, 2014
- … 塩基球様RBL-2H3細胞およびラット腹腔浸出細胞（PEC）に対し，10～1 000μmol/Lの範囲で濃度依存的にIgE誘導性およびイオノマイシン誘発性ヒスタミン遊離を抑制した．また，GABAB受容体作動薬バクロフェンもRBL-2H3細胞およびPECのヒスタミン遊離を抑制した．これらの結果から，GABAは好塩基球やマスト細胞に対する脱顆粒阻害活性を有し，この阻害活性はGABAB受容体を介して発揮されることが示唆された． …
- NAID 130004695486
- GABAB Receptor Gene Transfer Into the Nucleus Tractus Solitarii Induces Chronic Blood Pressure Elevation in Normotensive Rats
- LI Bo,LIU Qing,XUAN Chengluan,GUO Lirong,SHI Ruofan,ZHANG Qi,O'ROURKE Stephen T,LIU Kexiang,SUN Chengwen
- Circulation journal : official journal of the Japanese Circulation Society 77(10), 2558-2566, 2013-09-25
- NAID 10031191796
Related Links
- GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) that are linked via G-proteins to potassium channels. The changing potassium concentrations hyperpolarize the cell at the end of ...
Related Pictures
★リンクテーブル★
[★]
- 英
- GABA-B receptor、GABAB receptor
- 関
- GABA-Bレセプター、GABABレセプター、GABAB受容体
[★]
- 英
- GABAB receptor
- 関
- GABA-B受容体、GABA-Bレセプター、GABAB受容体
[★]
- 英
- GABAB receptor
- 関
- GABA-B受容体、GABABレセプター、GABAB受容体
[★]
- butyl
- 英
- γ-aminobutyric acid, γ-aminobutyrate, gamma aminobutyric acid
- 同
- γ-アミノ酪酸、4-アミノ酪酸、γ-アミノ酪酸、γアミノ酪酸、ガンマアミノブチル酸
- 関
- GABA受容体。ブチル
構造
生合成
[★]
