Caymanmuricholic Acid; Purity- Greater Than Or Equal To 95%; Si

NS 11394 is an orally bioavailable positive allosteric modulator of the GABA_A receptor (K_i = 0.423 nM in rat cortical membranes). It is selective for GABA_A receptors containing α₁, α₂, α₃, or α₅ subunits (K_is = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α₄ or α₆ subunits (K_is = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits α₃ and α₅, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ). In vivo, NS 11394 inhibits the binding of [³H]flunitrazepam to benzodiazepine receptors in the forebrain of mice and rats, with respective EC₅₀ values of 0.38 and 1.3 mg/kg at 30 minutes and 0.49 and 0.69 mg/kg at 120 minutes following oral administration. NS 11394 (1-30 mg/kg) attenuates spontaneous nociceptive behaviors to formalin and capsaicin (Item No. ) injections in a rat model of neuropathic pain.

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