mGlu4 receptor positive allosteric modulator (EC50 = 0.24 µM). Displays little activity at mGlu5 and mGlu8 receptors and no activity at mGlu1, 2, 3, 6 and 7 receptors. Blood-brain barrier permeable.
Solubility & Handling
Storage instructions
Room temperature
Solubility overview
Soluble in DMSO (100mM)
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References are publications that support the biological activity of the product
Radiosynthesis of N-(4-chloro-3-[(11)C]methoxyphenyl)-2-picolinamide ([(11)C]ML128) as a PET radiotracer for metabotropic glutamate receptor subtype 4 (mGlu4).
Kil KE et al (2013) Bioorg Med Chem 21(19) : 5955-62.
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.
Engers DW et al (2011) J Med Chem 54(4) : 1106-10.
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
Engers DW et al (2009) J Med Chem 52(14) : 4115-8.