Alpharmagen is developing α7 agonists to combat cognitive disorders such as schizophrenia and Alzheimer’s disease. We are currently preparing these compounds for testing in human clinical trials.
The α7 nicotinic acetylcholine receptor (nAChR) is an ion channel that is found in certain regions of the brain as well as the spleen and white blood cells. As its name suggests, this channel can be activated by ligands such as nicotine and acetylcholine, as well as others. These activators, or agonists, promote current to flow through the channel. However, overstimulation of the receptor can cause it to shutdown or desensitize. In a diseased state such as schizophrenia, there is a reduced number of α7 nAChRs in the brain and therefore the overall function of the nAChR system is diminished.
Partial agonists, such as those being developed by Alpharmagen, act to stimulate the α7 nAChR by binding to the acetylcholine site on the receptor. Alpharmagen has a portfolio of compounds that penetrate the brain and act to stimulate the nAChR at low concentrations, thus avoiding desensitization by the drug. These compounds have shown positive results in animal models of cognition and are currently being prepared for testing in human clinical trials.