It displays an IC50 = 10 nM to mGluR1 and an IC50 = 342 nM to mGluR5, demonstrating significant selectivity for mGluR1 versus mGluR5. It was originally synthesized by Zheng et al. in 2005 and has been subsequently characterized to be psychoactive, acting as an analgesic and also impairing motor and cognitive function. It acts as a pan-central nervous system (CNS) depressant, diminishing electrophysiological activity broadly across spinal neurons.
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