VU 0361737 N-(4-Chloro-3-methoxyphenyl)-2-pyridinecarboxamide;VU 0361737;2-Pyridinecarboxamide, N-(4-chloro-3-methoxyphenyl)-;CID-44191096;ML128 1161205-04-4
VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.
IC50 value: 110 nM (EC50, for rat ), 240 nM (EC50, for human)
Target: mGlu4
in vitro: VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [3]
in vivo: VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [3]
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