A search for novel positive and negative allosteric modulators of the cannabinoid CB1 receptor

Cannabinoid CB1 and CB2 receptors, and endogenously-produced compounds (“endocannabinoids”) that activate these receptors, constitute the “endocannabinoid system”. Research, here and elsewhere, has shown that the potency and/or maximum ability of drugs to activate CB1 receptors can be enhanced or inhibited by targeting “allosteric” sites on these receptors. This project would explore the ability of novel compounds to behave in vitro as allosteric CB1 receptor enhancers or inhibitors. Such compounds could well constitute important new medicines, since endocannabinoids are released onto CB1 receptors in certain disorders, in a manner that appears to ameliorate (e.g. multiple sclerosis), or exacerbate them (e.g. obesity).