International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2
- R. Pertwee, A. Howlett, R. Ross
- Biology, ChemistryPharmacological Reviews
- 15 November 2010
This review summarizes current data indicating the extent to which cannabinoid receptor ligands undergo orthosteric or allosteric interactions with non- CB1, non-CB2 established GPCRs, deorphanized receptors such as GPR55, ligand-gated ion channels, transient receptor potential (TRP) channels, and other ion channels or peroxisome proliferator-activated nuclear receptors.
Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain
- T. Bisogno, F. Howell, P. Doherty
- BiologyJournal of Cell Biology
- 10 November 2003
The cloning and enzymatic characterization of the first specific sn-1 DAG lipases are reported, providing a possible explanation for a fundamental change in endocannabinoid function during brain development.
Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide
- T. Bisogno, L. Hanuš, V. Di Marzo
- Biology, ChemistryBritish Journal of Pharmacology
- 1 October 2001
Results suggest that VR1 receptors, or increased levels of endogenous AEA, might mediate some of the pharmacological effects of CBD and its analogues, and (−)‐5′‐DMH‐CBD represents a valuable candidate for further investigation as inhibitor of AEA uptake and a possible new therapeutic agent.
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.
Identification and Functional Characterization of Brainstem Cannabinoid CB2 Receptors
- M. V. Van Sickle, M. Duncan, K. Sharkey
- Biology, MedicineScience
- 14 October 2005
These functional CB2 receptors in the brainstem were activated by a CB2 receptor agonist, 2-arachidonoylglycerol, and by elevated endogenous levels of endocannabinoids, which also act at CB1 receptors.
CB1 Cannabinoid Receptors and On-Demand Defense Against Excitotoxicity
- G. Marsicano, S. Goodenough, B. Lutz
- Biology, ChemistryScience
- 3 October 2003
The endogenous cannabinoid system provides on-demand protection against acute excitotoxicity in central nervous system neurons and could not be triggered in mutant mice.
Non-psychotropic plant cannabinoids: new therapeutic opportunities from an ancient herb.
- A. Izzo, F. Borrelli, R. Capasso, V. Di Marzo, R. Mechoulam
- Biology, MedicineTIPS - Trends in Pharmacological Sciences
- 1 October 2009
Regulation, function, and dysregulation of endocannabinoids in models of adipose and beta-pancreatic cells and in obesity and hyperglycemia.
- I. Matias, M. Gonthier, V. Di Marzo
- Biology, MedicineJournal of Clinical Endocrinology and Metabolism
- 1 August 2006
Peripheral endocannabinoid overactivity might explain why CB(1) blockers cause weight-loss independent reduction of lipogenesis, of hypoadiponectinemia, and of hyperinsulinemia in obese animals and humans.
Antitumor Activity of Plant Cannabinoids with Emphasis on the Effect of Cannabidiol on Human Breast Carcinoma
- A. Ligresti, A. S. Moriello, V. Di Marzo
- BiologyJournal of Pharmacology and Experimental…
- 1 September 2006
Results obtained in a panel of tumor cell lines clearly indicate that, of the five natural compounds tested, cannabidiol is the most potent inhibitor of cancer cell growth, with significantly lower potency in noncancer cells.
Role in anxiety behavior of the endocannabinoid system in the prefrontal cortex.
- T. Rubino, N. Realini, D. Parolaro
- Biology, PsychologyCerebral Cortex
- 1 June 2008
Findings support an anxiolytic role for physiological increases in AEA in the PFC, whereas more marked increases or decreases of this endocannabinoid might lead to an anxiogenic response due to TRPV1 stimulation or the lack of CB1 activation, respectively.
...
...