| Identification | Back Directory | [Name]
(E)-GABAB receptor antagonist 1 | [CAS]
1611483-29-4 | [Synonyms]
(E)-GABAB receptor antagonist 1
3-Butenoic acid, 4-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-oxo-, (3E)- | [Molecular Formula]
C18H24O4 | [MOL File]
1611483-29-4.mol | [Molecular Weight]
304.38 |
| Chemical Properties | Back Directory | [Boiling point ]
404.3±37.0 °C(Predicted) | [density ]
1.125±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
2.05±0.54(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor[1][2]. | [References]
[1] Chen LH, et al. Discovery of a Negative Allosteric Modulator of GABAB Receptors. ACS Med Chem Lett. 2014 May 27;5(7):742-7. DOI:10.1021/ml500162z
[2] Bing Sun, et al. A negative allosteric modulator modulates GABAB-receptor signalling through GB2 subunits. Biochem J. 2016 Mar 15;473(6):779-87. DOI:10.1042/BJ20150979 |
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