GABAB receptor

Agonisti

• GABA
• Baklofen je GABA analog koji deluje kao selektivni agonist GABA_B receptora, i koristi se kao relaksant mišića.
• Gama-hidroksibutirat (GHB)
• Fenibut
• 3-Aminopropilfosfinska kiselina
• Lesogaberan
• SKF-97541: 3-Aminopropil(metil)fosfinska kiselina, više od 10 puta je potentniji od baklofena kao GABA_B agonist, ali je i GABA_C antagonist
• CGP-44532

Pozitivni alosterni modulatori

• CGP-7930^[8][9]
• BHFF
• BHF-177^[10]
• BSPP
• GS-39783^[11]

Antagonisti

• Saklofen
• Faklofen
• SCH-50911
• CGP-35348
• CGP-52432: 3-([(3,4-Dihlorofenil)metil]amino]propil) dietoksimetil)fosfinska kiselina, CAS# 139667-74-6
• CGP-55845: (2S)-3-([(1S)-1-(3,4-Dihlorofenil)etil]amino-2-hidroksipropil)(fenilmetil)fosfinska kiselina, CAS# 149184-22-5
• SGS-742^[12][13]

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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. PMC 154371 . PMID 12692303. doi:10.1073/pnas.0830111100. 
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. PMID 16129424. doi:10.1016/j.ejphar.2005.07.016. 
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6. ^ ^{а б} MRC (Medical Research Council). 2003. Glutamate receptors: Structures and functions. Архивирано на сајту Wayback Machine (15. септембар 2007) 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 (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. Архивирано из оригинала 11. 10. 2008. г. Приступљено 31. 03. 2012. 
9. ^ Adams CL, Lawrence AJ (2007). „CGP7930: a positive allosteric modulator of the GABAB receptor”. CNS Drug Rev. 13 (3): 308—16. PMID 17894647. doi:10.1111/j.1527-3458.2007.00021.x. 
10. ^ Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A (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. PMC 2574924 . PMID 18445779. doi:10.1124/jpet.108.139204. 
11. ^ Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K (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. PMID 12954816. doi:10.1124/jpet.103.053074. 
12. ^ Froestl W, Gallagher M, Jenkins H, Madrid A, Melcher T, Teichman S, Mondadori CG, Pearlman R (2004). „SGS742: the first GABA(B) receptor antagonist in clinical trials”. Biochemical Pharmacology. 68 (8): 1479—87. PMID 15451390. doi:10.1016/j.bcp.2004.07.030. 
13. ^ Bullock R (2005). „SGS-742 Novartis”. Current Opinion in Investigational Drugs (London, England : 2000). 6 (1): 108—13. PMID 15675610.