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HexylHIBO is an antagonist of group I metabotropic glutamate receptors (mGluRs; Kbs = 140 and 110 µM for mGluR1α and mGluR5a, respectively).1 It is selective for group I mGluRs over mGluR2 (group II) and mGluR4a (group III) (Kbs = >1,000 µM for both), as well as AMPA, NMDA, and kainate receptors (IC50s = >100 µM for all). HexylHIBO (6.3 and 12.5 mg/kg, i.c.v.) inhibits NMDA-induced seizures in mice. It also potentiates increases in plasma adrenocorticotropic hormone (ACTH) levels in a rat model of restraint stress.2
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1. Synthesis and pharmacology of 3-
2. Metabotropic glutamate receptor-