Researchers Develop Medication to Target CB1 Receptors That Shows Promise

A research team funded by the NIH has “developed a medication that shows promise in treating acute and chronic pain.”

The drug, VIP36, “targets the body’s cannabinoid receptor type 1 (CB1). It was found to be effective in three different animal models for pain and does not appear to cause the harmful side effects that have frustrated other efforts to target CB1.” CB1 receptors are found throughout the body and “are particularly dense in the brain’s pain circuitry. They have long been considered a potential target for non-opioid-based pain treatment.”

Previous attempts at targeting this pathway have been met with two challenges: “first, repeated exposure to a drug leads to tolerance that limits its efficacy. Second, the dose required to reduce pain in the periphery tends to be high enough for the drug to make its way into the central nervous system. In humans, this can cause unwanted changes in mood, cognition, or emotional state.” These researchers used computer modeling of the CB1 receptor to “design molecules that better interact with CB1,” leading to the development of this new, more narrow-focused drug.

CB1 is “part of a wide-ranging class of receptors known as G-protein-coupled receptors, which are involved in countless functions throughout the body including smell, vision, mood regulation, immune system responses, autonomic nervous system responses such as blood pressure and heart rate, and growth and metastasis of some tumors. In addition to their implications in pain care, the findings of this study could also help spur the design of other drugs that target similar receptors involved in other conditions.”