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Endocannabinoids (eCBs) are endogenous lipids able to activate cannabinoid receptors, the primary molecular targets of the cannabis (Cannabis sativa or Cannabis indica) active principle Δ9-tetrahydrocannabinol (THC). During the last 25 years, several N-acylethanolamines and acylesters have been shown to act as eCBs, and a complex array of receptors, metabolic enzymes, (transmembrane, intracellular and extracellular) transporters, that altogether form the so-called “eCB system”, has been shown to finely tune the manifold biological activities of these lipid signals. It appears now urgent to develop selective drugs that allow dissection of the contribution of the distinct components of the eCB system to the overall biological activity of THC, other plant-derived cannabinoids (like cannabidiol) and eCBs, thus putting into a better perspective their relevance as key-players of health and disease conditions.

In this book, a modern view of natural compounds that evolved into synthetic drugs, able to selectively hit each element of the eCB system with very limited (if any) side effects, will be presented in separate chapters, written by widely recognized leaders in the field who will also discuss recent advances and future perspectives of drug design. In particular, Chapter 1 will explain why we need magic bullets to solve the endocannabinoid puzzle, and Chapter 2 will introduce the differences between phytocannabinoids and eCBs, along with a modern view of the eCB system. Then, Chapter 3 will describe natural compounds and synthetic drugs to target CB1 receptor, and Chapters 4, 5 and 6 will deliver the same information for CB2, non-cannabinoid and TRP receptors, respectively. After these eCB-binding receptors, the focus will be on metabolic enzymes of eCBs. Indeed, Chapter 7 will discuss natural compounds and synthetic drugs to target NAPE-PLD, and Chapters 8 and 9 will present those able to hit FAAH and MAGL, respectively. Last but not least, Chapter 10 will address eCB transporters and drugs able to modulate them, a highly debated hot topic within the (endo)cannabinoid community for many years.

The state-of-the-art information presented here should form the basis for more rational and effective therapeutic strategies to combat cannabinoid/eCB-related human pathologies. This appears indeed a very hot and timely topic, also in view of the increasing legalization and abuse of cannabis extracts all over the world. Of note, in recent papers we have shown how challenging it is to develop really selective drugs towards the eCB system that can be used as magic bullets for human health, avoiding potentially innovative therapeutics turning out to be killer pills for the patients.

Mauro Maccarrone

Department of Applied Clinical and Biotechnological Sciences, University of L'Aquila, I-67100 L'Aquila, Italy


European Center for Brain Research, IRCCS Santa Lucia Foundation

Rome, Italy

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