BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. It exhibits good CNS-agent like properties and clinical candidate potential. BNC375 significantly potentiates the acetylcholine signal without changing the rapid receptor desensitization. In vivo, BNC375 (0.003-10.0 mg/kg, administered orally) exhibits a Minimum Effective Dose (MED) of 0.03 mg/kg, achieving full reversal of scopolamine-induced impairment at 1.0 mg/kg in a mouse T-maze model. It has a plasma half-life (t1/2) of 1.2 hours.
- Potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs.
- Exhibits good CNS-agent like properties.
- Clinical candidate potential.
- Significantly potentiates acetylcholine signal.
- Achieves full reversal of scopolamine-induced impairment in mouse T-maze model.
- Plasma half-life (t1/2) of 1.2 hours.