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Papers of the Week


Papers: 7 Sep 2024 - 13 Sep 2024


2024


Front Pharmacol


39253381


15

The deuterated pyrazoloquinolinone targeting α6 subunit-containing GABA receptor as novel candidate for inhibition of trigeminovascular system activation: implication for migraine therapy.

Authors

Fan PC, Chiou LC, Lai TH, Sharmin D, Cook J, Lee MT

Abstract

The α6 subunit-containing GABA receptors (α6GABARs) are highly expressed in the trigeminal ganglia (TG), the sensory hub of the trigeminovascular system (TGVS). Hypo-GABAergic transmission in the TG was reported to contribute to migraine-related behavioral and histopathological phenotypes. Previously, we found that Compound 6, an α6GABAR-selective positive allosteric modulator (PAM), significantly alleviated TGVS activation-induced peripheral and central sensitization in a capsaicin-induced migraine-mimicking model.