Ganesh A Thakur
Affiliation: Northeastern University
- Prophylactic cannabinoid administration blocks the development of paclitaxel-induced neuropathic nociception during analgesic treatment and following cessation of drug deliveryElizabeth J Rahn
Neuroscience and Behavior Program, Department of Psychology, University of Georgia, Athens, GA, USA
Mol Pain 10:27. 2014..The impact of chronic drug infusion on transcriptional regulation of mRNA markers of astrocytes (GFAP), microglia (CD11b) and cannabinoid receptors (CB1, CB2) was assessed in lumbar spinal cords of paclitaxel and vehicle-treated rats...
- The maintenance of cisplatin- and paclitaxel-induced mechanical and cold allodynia is suppressed by cannabinoid CB₂ receptor activation and independent of CXCR4 signaling in models of chemotherapy-induced peripheral neuropathyLiting Deng
Program in Neuroscience, Indiana University, Bloomington, IN, USA
Mol Pain 8:71. 2012..A secondary objective was to investigate the potential contribution of alpha-chemokine receptor (CXCR4) signaling to both chemotherapy-induced neuropathy and CB₂ agonist efficacy...
- Novel adamantyl cannabinoids as CB1 receptor probesGanesh A Thakur
Center for Drug Discovery, Northeastern University, 116 Mugar Hall, 360 Huntington Avenue, Boston, Massachusetts 02115, USA
J Med Chem 56:3904-21. 2013....
- Latest advances in cannabinoid receptor agonistsGanesh A Thakur
Northeastern University, Center for Drug Discovery, 116 Mugar Hall, Boston, MA 02115, USA
Expert Opin Ther Pat 19:1647-73. 2009..The last decade has witnessed remarkable advances in the development of cannabinergic ligands displaying high selectivity and potency towards two subtypes of cannabinoid receptors, namely CB1 and CB2...
- Diuretic effects of cannabinoidsCarol A Paronis
Department of Pharmaceutical Sciences, Northeastern University, Mailstop 206, 140TF 360 Huntington Avenue, Boston, MA 02115, USA
J Pharmacol Exp Ther 344:8-14. 2013..These data indicate that cannabinoids have robust diuretic effects in rats that are mediated via CB1 receptor mechanisms...
- Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activityAtmaram D Khanolkar
Center for Drug Discovery, Northeastern University, 116 Mugar Hall, 360 Huntington Avenue, Boston, Massachusetts 02115 5000, USA
J Med Chem 50:6493-500. 2007..In vitro testing revealed that the novel compounds are CB2 agonists, while in vivo testing of cannabilactones 4b and 5 found them to possess potent peripheral analgesic activity...
- Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligandsHeidi Teng
Center for Drug Discovery, 116 Mugar Life Sciences Building, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, United States
Bioorg Med Chem Lett 21:5999-6002. 2011..We also found that 4c, 4d, and 5 exhibited 3- to 12-fold selectivity for hCB2 over rCB1 receptors and may serve as new chemotypes for the development of CB2-selective cannabinergics...
- Diuretic effects of cannabinoid agonists in miceGirish R Chopda
Department of Pharmaceutical Sciences, Northeastern University, Boston, MA 02115, USA Electronic address
Eur J Pharmacol 721:64-9. 2013....
- Controlled-deactivation cannabinergic ligandsRishi Sharma
Center for Drug Discovery and Departments of Chemistry and Chemical Biology and Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts 02115, United States
J Med Chem 56:10142-57. 2013..In further in vitro and in vivo experiments key analogues were shown to be potent CB1 receptor agonists and to exhibit CB1-mediated hypothermic and analgesic effects. ..
- Methods for the synthesis of cannabinergic ligandsGanesh A Thakur
Center for Drug Discovery, Department of Pharmaceutical Sciences, Northeastern University, Boston, MA, USA
Methods Mol Med 123:113-48. 2006....
- Natural cannabinoids: templates for drug discoveryGanesh A Thakur
Center for Drug Discovery, Northeastern University, 360 Huntington Avenue, 116 Mugar Life Sciences Building, Boston, MA 02115, USA
Life Sci 78:454-66. 2005..This review briefly summarizes the biosynthesis of cannabinoids and endocannabinoids and focuses on their side chain SAR...
- (-)-7'-Isothiocyanato-11-hydroxy-1',1'-dimethylheptylhexahydrocannabinol (AM841), a high-affinity electrophilic ligand, interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptorRobert P Picone
Center for Drug Discovery, Department of Pharmaceutical Sciences, University of Connecticut, Storrs, USA
Mol Pharmacol 68:1623-35. 2005..These studies present the first report of tandem applications of affinity labeling, site-directed mutagenesis, and interactive ligand docking for CB1...
- CB1 cannabinoid receptor ligandsGanesh A Thakur
Center for Drug Discovery, University of Connecticut, Storrs, 06269, USA
Mini Rev Med Chem 5:631-40. 2005..This review highlights the important CB1 cannabinergic ligands developed to date...
- Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of α7 nicotinic acGanesh A Thakur
Department of Pharmaceutical Sciences, Bouve College of Pharmacy, Northeastern University, 140 The Fenway, 360 Huntington Avenue, Boston, Massachusetts, 02115, United States
J Med Chem 56:8943-7. 2013..X-ray crystallography studies revealed the absolute stereochemistry of 1b to be 3aR,4S,9bS. 1b represents the most potent ago-PAM of α7 nAChRs available to date and is considered for further in vivo evaluation. ..
- Mass spectrometry-based proteomics of human cannabinoid receptor 2: covalent cysteine 6.47(257)-ligand interaction affording megagonist receptor activationDennis W Szymanski
Center for Drug Discovery, Department of Chemistry and Chemical Biology, College of Science, Northeastern University, Boston, Massachusetts 02115 5000, United States
J Proteome Res 10:4789-98. 2011..47(257). These data demonstrate how integration of MS-based proteomics into a ligand-assisted protein structure (LAPS) experimental paradigm can offer guidance to structure-enabled GPCR agonist design...
- Adamantyl cannabinoids: a novel class of cannabinergic ligandsDai Lu
Center for Drug Discovery, Northeastern University, 116 Mugar Life Sciences Building, Boston, Massachusetts 02115, USA
J Med Chem 48:4576-85. 2005....
- In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569Thomas F Gamage
aDepartment of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia bResearch Triangle Institute International, Durham, North Carolina cSchool of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Aberdeen, Scotland, UK dDepartment of Pharmaceutical Sciences and Center for Drug Discovery, School of Pharmacy, Bouve College of Health Sciences, Northeastern University, Boston, Massachusetts, USA eDepartment of Pharmacology and Toxicology, University of Toronto, Toronto, Canada
Behav Pharmacol 25:182-5. 2014..These findings question the utility of Org27569 as a 'gold standard' CB1 AM and underscore the need for the development of CB1 AMs with pharmacology that translates from the molecular level to the whole animal. ..