Abstract Context: Skeletal muscle endocannabinoids and sphingolipids (particularly sphingomyelins) are inversely associated with sleeping energy expenditure (SLEEP) in humans. The endocannabinoid system may increase sphingolipid synthesis via cannabinoid receptor-1. …
Condition: Endocannabinoid System (ECS)
The Endocannabinoid-CB Receptor System: Importance for development and in pediatric disease
Abstract Endogenous cannabinoids (endocannabinoids) and their cannabinoid CB1 and CB2 receptors, are present from the early stages of gestation and play a number of vital roles for the developing organism….
The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: D9-tetrahydrocannabinol, cannabidiol and D9-tetrahydrocannabivarin
Cannabis sativa is the source of a unique set of compounds known collectively as plant cannabinoids or phytocannabinoids. This review focuses on the manner with which three of these compounds,…
Agonistic Properties of Cannabidiol at 5-HT1a Receptors
Cannabidiol (CBD) is a major, biologically active, but psycho-inactive component of cannabis. In this cell culture-based report, CBD is shown to displace the agonist, [3H]8-OHDPAT from the cloned human 5-HT1a…
Allosteric Modulation of the Cannabinoid CB1 Receptor
We investigated the pharmacology of three novel compounds, Org 27569 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4- piperidin-1-yl-phenyl)-ethyl]-amide), Org 27759 (3-ethyl-5- fluoro-1H-indole-2-carboxylic acid [2-94-dimethylamino-phenyl)-ethyl]-amide), and Org 29647 (5-chloro-3-ethyl-1H-indole2-carboxylic acid (1-benzyl-pyrrolidin-3-yl)-amide, 2-enedioic acid salt), at…
Anandamide and 2-arachidonoylglycerol: Pharmacological Properties, Functional Features, and Emerging Specificities of the Two Major Endocannabinoids
Since the discovery of endocannabinoids and their receptors, two major members of the endocannabinoid family, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), have been regarded almost as twin brothers. Pharmacological properties were…
Antiangiogenic Activity of the Endocannabinoid Anandamide: Correlation to its Tumor-Suppressor Efficacy
Endocannabinoids are now emerging as suppressors of key cell-signaling pathways involved in cancer cell growth, invasion, and metastasis. We have previously observed that the metabolically stable anandamide analog, 2-methyl-2′-F-anandamide (Met-F-AEA)…
Biphasic Effects of Cannabinoids on Acetylcholine Release in the Hippocampus: Site and Mechanism of Action
Cannabinoids have been shown to critically modulate cholinergic neurotransmission in the hippocampus, yet opposing effects of cannabinoid receptor 1 (CB1R) agonists on hippocampal synaptic acetylcholine (ACh) efflux have been reported….
Cannabidiol displays unexpectedly high potency as an antagonist of CB1 and CB2 receptor agonists in vitro
Background and purpose: A nonpsychoactive constituent of the cannabis plant, cannabidiol has been demonstrated to have low affinity for both cannabinoid CB1 and CB2 receptors. We have shown previously that…
Cannabidiol is a negative allosteric modulator of the type 1 cannabinoid receptor
Background and purpose: Cannabidiol has been reported to act as an antagonist of cannabinoid agonists at type 1 cannabinoid receptors (CB1). We hypothesized that cannabidiol can inhibit cannabinoid agonist activity…