SCS

SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABA_A receptors with an IC₅₀ of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions^[1]. IC50 & Target:IC50: 32 nM (α2β1γ1θ; by VIPR measurement)
IC50: 4.5 nM (α2β1γ1θ), 5.3 nM (α2β1γ1), 7.9 nM (α1β1γ2s) (Measured by using whole-cell patch clamp)^[1] In Vitro:SCS (0.1 nM-3 μM) produces a concentration-dependent inhibition of GABA EC₂₀ currents recorded from Ltk^- cells expressing α2β1γ1θ, α2β1γ1 and α1β1γ2s receptors compared with α2β3γ2s and α1β2γ2s receptors upon which SCS has no effect^[1].
Inhibition by SCS is not voltage or use dependent^[1].
Structural determinants necessary for the inhibition of GABA_A receptors by SCS are located within the region arginine 238 and glycine 335 of the β1 subunit. T255 and I308 of the β1 subunit are required for inhibition by SCS^[1]. In Vivo:SCS (Salicylidene salicylhydrazide; 500-1000 mg/kg, i.p. or 800-1000 mg/kg, oral) produces abdominal constrictions in mice^[2].
SCS (10-75 mg/kg; i.p.; once) shows antinociceptive activity against tonic, phasic and Capsaicin (HY-10448) nociception in mice^[2].
SCS (10-75 mg/kg; i.p.; once) shows anti-inflammatory activity in mice^[2]. SCS (50 and 75 mg/kg; i.p.; once) shows antinociceptive activity against neuropathic nociception^[2].