NS 11394

NS 11394

CAT N°: 23872
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From 48.00 40.80

NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes).{36345} It is selective for GABAA receptors containing ?1, ?2, ?3, or ?5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing ?4 or ?6 subunits (Kis = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits ?3 and ?5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ISO60177). 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. 92350) injections in a rat model of neuropathic pain.{36346}

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