MPEP hydrochloride

Description: MPEP hydrochloride is a highly potent, selective, and non-competitive antagonist of mGlu5 receptor with IC50 of 36 nM, it exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. MPEP reverses maze learning and PSD-95 deficits in Fmr1 knock-out mice. Unlike the NMDA antagonist MK-801, MPEP does not injure the adult retrosplenial cortex, in which it fails to induce heat shock protein 70 (Hsp70). Moreover, MPEP does not elicit to the same extent as MK-801 apoptosis in cortical areas at perinatal stages, as revealed by caspase 3 expression. These data identify new cellular targets for the anxiolytic and antidepressant effect of MPEP, indicating also in addition that in contrast to MK-801, it lacks the cortical neurotoxicity associated with psychotomimetic side-effects. MPEP has the potential use as anxiolytic/antidepressant drug.

References: Neuropharmacology. 1999 Oct; 38(10):1493-503; Br J Pharmacol. 2001 Apr; 132(7):1423-30.