GABAB receptor

Receptor gama aminobuterne kiseline (GABA) B, 1
Identifikatori
Simbol GABBR1
Entrez 2550
HUGO 4070
OMIM 603540
RefSeq NM_021905
UniProt Q9UBS5
Drugi podaci
Lokus Hromozom 6 p21.3
Receptor gama aminobuterne kiseline (GABA) B, 2
Identifikatori
Simbol GABBR2
Alt. simboli GPR51
Entrez 9568
HUGO 4507
OMIM 607340
RefSeq NM_005458
UniProt O75899
Drugi podaci
Lokus Hromozom 9 q22.1-22.3

GABAB receptori (GABABR) su metabotropni transmembranski receptori za gama-aminobuternu kiselinu (GABA) koji su vezani putem G proteina za kalijumske kanale.[1] Promena koncentracije kalijuma hiperpolarizuje ćeliju na kraju akcionog potencijala. GABAB posredovana promena potencijala je -100 mV, to je znatno više od promene potencijala koju proizvodi GABAA. GABAB receptori su prisutni u centralnom i perifernom autonomnom nervnom sistemu.

Funkcije

Oni mogu da stimulišu otvaranje K+ kanala ćime se neuron približava ravnotežnom potencijalu K+ jona, te dolazi do popularizaciju neurona. Time se sprečava otvaranje natrijumovog kanala, dejstvo akcionog potencijala, i otvaranje VDCC kanala, te se zaustavlja otpuštanje neurotransmitera. GABAB receptori se smatraju inhibitornim receptorima.

GABAB receptori takođe mogu da umanje aktivnost adenilil ciklaze i da redukuju ćelijsku provodnost za Ca2+.

GABAB receptori posreduju dejstvo etanola,[2] i gama-hidroksibuterne kiseline (GHB).[3][4] Nedavna istraživanja sugeriraju da ovi receptori imaju važnu ulogu u razvoju organizma.[5]

Struktura

GABAB receptori imaju sličnu strukturu sa metabotropnim glutamatnim receptorima.[6] Poznata su dva podtipa receptora, GABAB1 i GABAB2,[7]. Oni se javljaju kao heterodimeri u neuronskim membranama. Do dimerizacije dolazi putem formiranja nevezujućih interakcija njihovih intracelularnih C terminusa.[6]

Smatra se da vezivanje liganda uzrokuje znatnu konformacionu promenu aktivnog mesta.

Selektivni ligandi

GABA
GHB
Lezogaberan

Agonisti

CGP-7930

Pozitivni alosterni modulatori

Faklofen
SCH-50911

Antagonisti

Reference

  1. 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. 
  2. 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. 
  3. 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. 
  4. 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. 
  5. 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. 
  6. 6,0 6,1 MRC (Medical Research Council). 2003. Glutamate receptors: Structures and functions. Arhivirano 2007-09-15 na Wayback Machine-u University of Brisotol Centre for Synaptic Plasticity.
  7. 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.
  8. 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. Arhivirano iz originala na datum 2008-10-11. Pristupljeno 2014-04-26. 
  9. 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. 
  10. 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. 
  11. 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. 
  12. 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. 
  13. Bullock R (January 2005). „SGS-742 Novartis”. Current Opinion in Investigational Drugs (London, England : 2000) 6 (1): 108–13. PMID 15675610. 

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