Gabapentin is a widely prescribed non-opioid painkiller, but it has many side effects, including memory loss, mood changes, and lethargy. New research out of NYU shows promise for a small molecule called CBD3063*, which in rodents has been shown to inhibit pain at lower doses than gabapentin with none of the side effects. Like gabapentin, the new molecule works by interacting with the calcium channel Cav2.2 in pain neurons, but from the inside, rather than the outside, of the channel.
CBD3063 is based on a 15-amino acid peptide called CBD3*, which also inhibits pain. Researchers determined that only two of the amino acids were needed to inhibit influx of calcium ions into the neurons, and centered the development of the small molecule candidate on these two amino acids. They screened an enormous library of compounds via computer simulation to arrive at 77 molecules that might reduce calcium influx, and then further narrowed the field via experiments that involved measuring the electrical currents through the calcium channel. CBD3063 was found to treat several types of pain, including chemotherapy-induced neuropathy, inflammatory pain, and trigeminal nerve pain in animal models.
*Note that the small molecule CBD3063 and the peptide CBD3 have no relation to cannabidiol, a compound found in cannabis and also abbreviated CBD.