An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors
- Susan M. Huang, T. Bisogno, V. Di Marzo
- BiologyProceedings of the National Academy of Sciences…
- 11 June 2002
The hypothesis, based on previous structure-activity relationship studies and the availability of biosynthetic precursors, that N-arachidonoyl-dopamine (NADA) is an endogenous “capsaicin-like” substance in mammalian nervous tissues is examined and found that NADA occurs in nervous tissues.
Leptin-regulated endocannabinoids are involved in maintaining food intake
It is shown that following temporary food restriction, CB1 receptor knockout mice eat less than their wild-type littermates, and the CB1 antagonist SR141716A reduces food intake in wild- type but not knockout mice, which indicates that endocannabinoids in the hypothalamus may tonically activate CB1 receptors to maintain food intake and form part of the neural circuitry regulated by leptin.
Endocannabinoid levels in rat limbic forebrain and hypothalamus in relation to fasting, feeding and satiation: stimulation of eating by 2‐arachidonoyl glycerol
- T. Kirkham, C. Williams, F. Fezza, V. Marzo
- Biology, PsychologyBritish Journal of Pharmacology
- 1 June 2002
These findings provide the first direct evidence of altered brain levels of endocannabinoids, and of 2‐AG in particular, during fasting and feeding, and supports a role for endoc cannabinoidoids in the control of appetitive motivation.
Endocannabinoids control spasticity in a multiple sclerosis model
These studies provide definitive evidence for the tonic control of spasticity by the endocannabinoid system and open new horizons to therapy of multiple sclerosis, and other neuromuscular diseases, based on agents modulating endoc cannabinoidoid levels and action, which exhibit little psychotropic activity.
Changes in endocannabinoid contents in the brain of rats chronically exposed to nicotine, ethanol or cocaine
Anandamide inhibits metabolism and physiological actions of 2-arachidonoylglycerol in the striatum
It is found that stimulation of metabotropic glutamate 5 receptors by 3,5-dihydroxyphenylglycine (DHPG) depressed inhibitory transmission in the striatum through selective involvement of 2-AG metabolism and stimulation of presynaptic CB1 receptors.
Cannabinoid CB1‐receptor mediated regulation of gastrointestinal motility in mice in a model of intestinal inflammation
It is concluded that inflammation of the gut increases the potency of cannabinoid agonists possibly by ‘up‐regulating’ CB1 receptor expression; in addition, endocannabinoids, whose turnover is increased in inflamed gut, might tonically inhibit intestinal motility.
Characterization of the endocannabinoid system in boar spermatozoa and implications for sperm capacitation and acrosome reaction
It is shown that sperm cells have a complete and efficient endocannabinoid system, and that activation of cannabinoid or vanilloid receptors controls, at different time-points, sperm functions required for fertilization.
Lipid Rafts Control Signaling of Type-1 Cannabinoid Receptors in Neuronal Cells
- M. Bari, N. Battista, F. Fezza, A. Finazzi-Agro’, M. Maccarrone
- Biology, ChemistryJournal of Biological Chemistry
- 1 April 2005
Treatment of rat C6 glioma cells with the raft disruptor methyl-β-cyclodextrin doubles the binding efficiency of type-1 cannabinoid receptors (CB1R), and CB1R activation underlies the protective effect of MCD against apoptosis.
Neuroprotection by the Endogenous Cannabinoid Anandamide and Arvanil against In Vivo Excitotoxicity in the Rat: Role of Vanilloid Receptors and Lipoxygenases
This study assessed whether VR1 is involved in neuroprotection by AEA and by arvanil, a hydrolysis-stable AEA analog that is a ligand for both VR1 and CB1, and the putative involvement of lipoxygenase metabolites of AEA in conveying neuroprotection.