MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

MPEP hydrochloride is an effective and highly specific non-competitive antagonist at the mGlu5 receptor subtype (IC50: 36 nM).

5-MPEP is a neutral allosteric site ligand of the metabotropic glutamate receptor subtype 5 (mGlu5), blocking the effects of both the allosteric antagonist MPEP and potentiator CDPPB.

VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity.

M-5MPEP is a mGlu5 antagonist.

MMPEP is both a selective non-competitive mGlu5 receptor antagonist with IC50 value of 36 nM and a mGlu4 receptor positive allosteric modulator.

Incadronate, also known as Cimadronate and YM-175, is a bone resorption inhibitor. Incadronate disodium inhibits macrophage migration to site of inflammation in vivo and proliferation and causes apoptosis in cancer cells in vitro. Incadronate disodium is a bone density conservation, antitumor and anti-inflammatory agent.

ML254 competitively interacts with the MPEP allosteric binding site. ML254 is highly selective for mGlu5 versus other mGlu receptors, has a clean ancillary Ricerca profile, and suitable dystrophia myotonica protein kinase (DMPK) properties for systemic dosing in rodents.