CAY10787 is an oxysterol and a negative allosteric modulator of GABA_Areceptors.^1,2It reduces GABA-induced currents in HEK cells expressing α₁β₁γ₂or α₄β₃γ₂subunit-containing GABA_Areceptors (IC₅₀s = 1.5 and 1 µM, respectively).²CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in the hot plate test in mice.

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