Measuring Endocannabinoid Hydrolysis: Refining our Tools and Understanding
Journal Title: The AAPS Journal - Year 2009, Vol 11, Issue 2
Abstract
Endocannabinoids (eCBs) are lipid transmitters that are released from membrane precursors in response to specific stimuli, activate cannabinoid receptors—the molecular targets of compounds produced by Cannabis sativa—and are then rapidly inactivated by uptake and enzymatic hydrolysis. This signaling system is implicated in a wide range of biological processes, including pain sensation, immunomodulation, appetite regulation, development, and cognitive and emotional states. The balance between eCB release and inactivation determines the extent of eCB accumulation, with enzymatic hydrolysis functioning as an important limiting step. Pharmacological inhibition of eCB-hydrolyzing enzymes offers great therapeutic and experimental promise for enhancing this ubiquitous signaling system only where and when these transmitters are naturally produced. The following mini-review summarizes the latest developments concerning eCB-hydrolyzing enzymes, with an emphasis on the techniques used to measure their activities and how these have helped increase our understanding of the role that eCBs play in regulating fundamental biological functions.
Authors and Affiliations
William Marrs, Nephi Stella
Keywords
Related Articles
- EP ID EP681480
- DOI 10.1208/s12248-009-9109-0
- Views 79
- Downloads 0
Understanding the Effect of API Properties on Bioavailability Through Absorption Modeling
This article inadvertently failed to include two of the theme issue guest editors. The complete listing of the guest editors is shown in this erratum.
A Neutralizing Antibody Assay Based on a Reporter of Antibody-Dependent Cell-Mediated Cytotoxicity
Benralizumab is a humanized anti-IL5 receptor α (IL5Rα) monoclonal antibody (mAb) with enhanced (afucosylation) antibody-dependent cell-mediated cytotoxicity (ADCC) function. An ADCC reporter cell-based n...
Nonviral gene delivery: What we know and what is next
Gene delivery using nonviral approaches has been extensively studied as a basic tool for intracellular gene transfer and gene therapy. In the past, the primary focus has been on application of physical, chemical, and bio...
Physiologically Based Absorption Modelling to Predict the Impact of Drug Properties on Pharmacokinetics of Bitopertin
The online version of this article (doi:10.1208/s12248-014-9639-y) contains supplementary material, which is available to authorized users.
Hidalgo, I. J., Raub, T. J., and Borchardt, R. T.: Characterization of the Human Colon Carcinoma Cell Line (Caco-2) as a Model System for Intestinal Epithelial Permeability, Gastroenterology, 96, 736–749, 1989—The Backstory
This manuscript was written with the knowledge and input of Ismael J. Hidalgo and Thomas J. Raub, who were coauthors of the 1989 Gastroenterology paper describing for the first time Caco-2 cell monolayers as a cell cultu...