(E)-GABAB receptor antagonist 1

• CAT Number: I017585
• CAS Number: 1611483-29-4
• Molecular Formula: C18H24O4
• Molecular Weight: 304.39
• Purity: ≥95%
• IUPAC Name: (E)-4-(3,5-ditert-butyl-4-hydroxyphenyl)-2-oxobut-3-enoic acid
• InChI: InChI=1S/C18H24O4/c1-17(2,3)12-9-11(7-8-14(19)16(21)22)10-13(15(12)20)18(4,5)6/h7-10,20H,1-6H3,(H,21,22)/b8-7+
• InChIKey: XIQDGAUDNMVMCD-BQYQJAHWSA-N
• SMILES: CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)/C=C/C(=O)C(=O)O

(E)-GABAB Receptor Antagonist 1 (CAT: I017585) is a selective negative allosteric modulator of GABAB receptors, acting as a trans-GABAB receptor antagonist. It decreases GABA-induced inositol trisphosphate (IP₃) production with an IC₅₀ of 37.9 μM in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins. Unlike orthosteric antagonists, this compound reduces the maximal GABA-induced response without altering EC₅₀ values, confirming its allosteric mechanism. (E)-GABAB Receptor Antagonist 1 serves as a valuable tool for studying inhibitory neurotransmission, GPCR modulation, and the role of GABAB signaling in neurological disorders, offering insights into therapeutic strategies targeting GABAergic dysfunction.