Abstract

Anandamide and 2-arachidonoyl-glycerol (2-Ara-Gl) which we isolated from porcine brain in 1992 and from canine gut in 1995 respective are the major endogenous cannabinoids identified so far. Anandamide is accompanied by numerous acylethanolamides; 2-Ara-Gl is accompanies by numerous 2-acyl- glycerols. We have preliminary data which indicates that these entourage compounds"""""""" enhance receptor binding of the endogenous ligands, potentiate their in vivo effects and inhibit their hydrolysis. We plan to explore these preliminary findings. We also plan to investigate whether anandamide and/or 2-Aa-Gl have cerebroprotective effects. Preliminary data with anandamide point in this direction. We have synthesized arachidonoyl derivatives which are non hydrolysable. We plan to investigate their properties and compare them to 2-Ara-Gl and anandamide. Finally, we plan to synthesize the major cannabidiol metabolites, 7-hydroxyl-cannabidiol and cannabidiol-7-oic acid and test their possible interactions with THC binding and on in vivo activity.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute on Drug Abuse (NIDA)
Type
Research Program Projects (P01)
Project #
5P01DA009789-05
Application #
6201618
Study Section
Project Start
1999-09-07
Project End
2000-08-31
Budget Start
1997-10-01
Budget End
1998-09-30
Support Year
5
Fiscal Year
1999
Total Cost
Indirect Cost

  Institution

Name
Virginia Commonwealth University
Department
Type
DUNS #
City
Richmond
State
VA
Country
United States
Zip Code
23298

  Publications

Donvito, Giulia; Nass, Sara R; Wilkerson, Jenny L et al. (2018) The Endogenous Cannabinoid System: A Budding Source of Targets for Treating Inflammatory and Neuropathic Pain. Neuropsychopharmacology 43:52-79
Wilkerson, Jenny L; Curry, Zachary A; Kinlow, Pamela D et al. (2018) Evaluation of different drug classes on transient sciatic nerve injury-depressed marble burying in mice. Pain 159:1155-1165
Mitjavila, Jose; Yin, Danielle; Kulkarni, Pushkar M et al. (2018) Enantiomer-specific positive allosteric modulation of CB1 signaling in autaptic hippocampal neurons. Pharmacol Res 129:475-481
Wilkerson, Jenny L; Ghosh, Sudeshna; Mustafa, Mohammed et al. (2017) The endocannabinoid hydrolysis inhibitor SA-57: Intrinsic antinociceptive effects, augmented morphine-induced antinociception, and attenuated heroin seeking behavior in mice. Neuropharmacology 114:156-167
Wilkerson, Jenny L; Niphakis, Micah J; Grim, Travis W et al. (2016) The Selective Monoacylglycerol Lipase Inhibitor MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model. J Pharmacol Exp Ther 357:145-56
Buczynski, Matthew W; Herman, Melissa A; Hsu, Ku-Lung et al. (2016) Diacylglycerol lipase disinhibits VTA dopamine neurons during chronic nicotine exposure. Proc Natl Acad Sci U S A 113:1086-91
Staiano, Rosaria I; Loffredo, Stefania; Borriello, Francesco et al. (2016) Human lung-resident macrophages express CB1 and CB2 receptors whose activation inhibits the release of angiogenic and lymphangiogenic factors. J Leukoc Biol 99:531-40
Tessaris, Daniele; Matarazzo, Patrizia; Lala, Roberto et al. (2016) Odontoiatric perspectives and osteonecrosis of the jaw as a possible adverse effect of bisphosphonates therapy in fibrous dysplasia and McCune-Albright syndrome. J Pediatr Endocrinol Metab 29:333-6
Kocova, Mirjana; Zdraveska, Nikolina; Kacarska, Rozana et al. (2016) Diagnostic approach in children with unusual symptoms of acquired hypothyroidism. When to look for pituitary hyperplasia? J Pediatr Endocrinol Metab 29:297-303
Anavi-Goffer, Sharon; Ross, Ruth A (2016) A Functional Assay for GPR55: Envision Protocol. Methods Mol Biol 1412:77-83

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