The Endocannabinoidome

The World of Endocannabinoids and Related Mediators

Vincenzo Di Marzo, Jenny Wang

• Publisher: Academic Press
• Year: 2014
• Print ISBN: 9780124201262
• eBook ISBN: 9780128004296
• Topic: Biological Sciences
• Subtopic: Pharmacology
• Index: Biological Sciences

The Endocannabinoidome: The World of Endocannabinoids and Related Mediators is dedicated to the latest research and studies on endocannabinoids and cannabinoid receptors to illustrate their important role in the discovery of new, endocannabinoid-related, lipid mediators. Written by leading experts across different disciplines, this book focuses on the biochemical and anlayticial aspects of novel lipid signals, their pharmacological activities and their potential utilization for the development of new and effective therapeutic strategies. The first book of its kind, The Endocannabinoidome is a meaningful reference for all those involved in experimental efforts to further the development of this field. - Explores the novel and exciting aspects of several endocannabinoid-like molecules for which researchers are still seeking a function - Discusses the novel metabolic pathways for endocannabinoids in order to explain the failure of some clinical trials with inhibitors of more conventional metabolic pathways - Incorporates pharmacology, biochemistry and potential clinical applications to provide researchers with a complete look at endocannabinoids

Chapter 1

Non-endocannabinoid N-Acylethanolamines and Monoacylglycerols: Old Molecules New Targets

Harald S. Hansen

Karen Kleberg

Helle Adser Hassing

Abstract

N-Acylethanolamine (NAE) and 2-monoacylglycerol (2-MAG) containing arachidonic acid are being called endocannabinoids since they can activate cannabinoid receptors. The same molecules containing stearic acid, palmitic acid, oleic acid, or linoleic acid cannot activate cannabinoid receptors, and are thus called non-endocannabinoid NAEs and 2-MAGs. However, these molecules do also have biological activities, e.g., via activation of the transcription factor PPARα, which mediate anti-inflammatory, antinociceptive, and anorectic effects. Furthermore, activation of the G-protein coupled receptor GPR119 in the small intestine could mediate release of the incretin hormone GLP-1. The present chapter describes the formation and degradation of these lipid molecules, as well as their pharmacology and their related drug targets.

Keywords

oleoylethanolamide

palmitoylethanolamide

2-oleoyl glycerol

dietary fat

fat sensor

signaling lipids

GPR119

PPARα

1.1 INTRODUCTION 1

1.2 FORMATION AND DEGRADATION OF N-ACYLETHANOLAMINES 2

1.3 BIOLOGICAL ROLES AND DRUG TARGETS OF NON-ENDOCANNABINOID N-ACYLETHANOLAMINES 4

1.4 FORMATION AND DEGRADATION OF NON-ENDOCANNABINOID 2-MONOACYLGLYCEROLS 5

1.5 BIOLOGICAL ROLES AND DRUG TARGETS OF NON-ENDOCANNABINOID 2-MONOACYLGLYCEROLS 7

1.6 CONCLUSION 8

ACKNOWLEDGMENT 9

REFERENCES 9

1.1. Introduction

The non-endocannabinoid N-acylethanolamines (NAEs) and mono-acylglycerols (2-MAGs) owe their “non-endocannabinoid” name to their structural resemblance with the true endocannabinoids, anandamide (= N-arachidonoylethanolamine) and 2-arachidonoyl glycerol (2-AG) combined with their lack of effects on t...

Table of contents

• Cover
• Title page
• Table of Contents
• Copyright
• Dedications
• Contributors
• Preface
• Acknowledgments
• Chapter 1: Non-endocannabinoid N-Acylethanolamines and Monoacylglycerols: Old Molecules New Targets
• Chapter 2: Omega-3 Polyunsaturated N-Acylethanolamines: A Link Between Diet and Cellular Biology
• Chapter 3: N-Acyl Amides: Ubiquitous Endogenous Cannabimimetic Lipids That Are in the Right Place at the Right Time
• Chapter 4: Oxidative Metabolites of Endocannabinoids Formed by Cyclooxygenase-2
• Chapter 5: N-Acyldopamines and N-Acylserotonins: From Synthetic Pharmacological Tools to Endogenous Multitarget Mediators
• Chapter 6: The Pharmacology of Prostaglandin F2α Ethanolamide and Bimatoprost Reveals a Unique Feedback Mechanism on Endocannabinoid Actions
• Chapter 7: Prostamide F2α Biosynthesizing Enzymes
• Chapter 8: Metabolic Enzymes for Endocannabinoids and Endocannabinoid-Like Mediators
• Chapter 9: Endocannabinoidomics: “Omics” Approaches Applied to Endocannabinoids and Endocannabinoid-Like Mediators
• Chapter 10: Common Receptors for Endocannabinoid-Like Mediators and Plant Cannabinoids
• Index