Cannabinoid receptors, the molecular targets of the cannabis constituent De
lta(9)-tetrahydrocannabinol, are present throughout the body and are normal
ly bound by a family of endogenous lipids - the endocannabinoids, Release o
f endocannabinoids is stimulated in a receptor-dependent manner by neurotra
nsmitters and requires the enzymatic cleavage of phospholipid precursors pr
esent in the membranes of neurons and other cells. Once released, the endoc
annabinoids activate cannabinoid receptors on nearby cells and are rapidly
inactivated by transport and subsequent enzymatic hydrolysis. These compoun
ds might act near their site of synthesis to serve a variety of regulatory
functions, some of which are now beginning to be understood. Recent advance
s in the biochemistry and pharmacology of the endocannabinoid system in rel
ation to the opportunities that this system offers for the development of n
ovel therapeutic agents will be discussed.