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Description: VU 0364439 (VU0364439; VU-0364439) is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with important biological activity. It inhibits mGlu4 with an EC50 value of 19.8 nM. Due to the fact that VU 0364439 possessed less favorable pharmacokinetic properties, thus it can not be used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds. The activation of the mGlu4 receptor, either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons.
References: Bioorg Med Chem Lett. 2010 Sep 1; 20(17):5175-8; J Med Chem. 2011 Jul 28; 54(14):5070-81.
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