ADX71743 [(1)-6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydrobenzo[d]oxazol-4(5H)-one] is a negative modulator of metabotropic glutamate receptor 7 (mGlu7), which has been suggested to be a promising target for a range of disorders of the central nervous system. In vitro, Schild plot analysis and reversibility tests at the target confirmed the negative allosteric modulator characteristics of ADX71743. In vivo, ADX71743 caused no impairment of locomotor activity in rodents but had an anxiolytic-like profile in the marble burying and elevated plus maze tests. Although ADX71743 caused a small reduction in amphetamine-induced hyperactivity in mice, it was inactive in the mouse 2,5-dimethoxy-4-iodoamphetamine-induced head twitch and the rat-conditioned avoidance-response tests. These in vivo data suggest that mGlu7 may be a valid target for treatment of anxiety disorders and that ADX71743 may be an appropriate tool.
See article at J Pharmacol Exp Ther 2013, 344:624–636.
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