HZ-166 is a Positive GABAA receptor modulator and a GABAA receptor subtype-selective benzodiazepine site ligand. HZ166 is antihyperalgesic in mouse models of inflammatory and neuropathic pain. Diminished GABAergic and glycinergic inhibition in the spinal dorsal horn contributes significantly to chronic pain of different origins. Accordingly, pharmacological facilitation of GABAergic inhibition by spinal benzodiazepines (BDZs) has been shown to reverse pathological pain in animals as well as in human patients. References: Yuan NY, Poe MM, Witzigmann C, Cook JM, Stafford D, Arnold LA. Characterization of GABA(A) receptor ligands with automated patch-clamp using human neurons derived from pluripotent stem cells. J Pharmacol Toxicol Methods. 2016 Nov - Dec;82:109-114. doi: 10.1016/j.vascn.2016.08.006. PubMed PMID: 27544543; PubMed Central PMCID: PMC5116268.
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CAS:612527-56-7