Overview
- Nagarajan, N. et al. (2001) Neuropharmacology 41, 650.
Alomone Labs CX 546 potentiates GluA1 channels expressed in Xenopus oocytes.Time course of current reversible potentiation by 12.6, 126 and 630 μM CX 546 (#C-210) of glutamate-elicited currents (100 μM, holding potential -80 mV).
The AMPAkine families of drugs are positive allosteric modulators of AMPA receptors in the mammalian brain. These compounds facilitate learning and memory in both humans and animals. Positive modulation of AMPA receptors by AMPAkines can improve channel function by increasing receptor sensitivity to endogenous ligands and specific agonists1.
The AMPAkine 1-(quinoxalin-6-ylcarbonyl)-piperidine (CX546) is a brain-penetrating compound, which facilitates AMPA receptor-mediated transmission. CX546 has an EC50 in a hippocampal slice preparation of 150 μM as measured by patch clamp in cultured hippocampal neurons. The action of CX546 on AMPA receptor transmission results in memory enhancement, which has been demonstrated in rodents, primates, and humans2.
Recent findings now indicate that CX546-mediated AMPA receptor enhancement strengthens neuronal survival signaling, leading to concomitant reduction in hippocampal damage3.
CX546 was researched as a treatment for Alzheimer's disease under the brand name Ampalex.
