RGM079 (RGM-079) is a potent, selective α7 nAChR positive allosteric modulator (PAM) with EC50 of 8.3 uM.
RGM079 exhibited a balanced pharmacokinetic profile and antioxidant properties comparable or even higher than well-known natural polyphenols.
RGM079 shows neuroprotective properties in Alzheimer's disease (AD)-toxicity related models.
RGM079 causes a concentration-dependent neuroprotective effect against the toxicity induced by okadaic acid (OA) in the human neuroblastoma cell line SH-SY5Y.
RGM079 is able to restore the cellular viability after exposure to OA and amyloid peptide Aβ1–42, with cell death almost completely prevented at 10 and 30 μM, respectively, in primary cultures of rat cortical neurons;
RGM079 shows in vivo analgesic activity in the complete CFA-induced paw inflammation model after intraperitoneal administration.
