Thakur Lab
Publications
- Synthesis, characterization and redox properties of ruthenium (II) phenolato Schiff base mixed ligand complexes
Rao, P.S.; Thakur, G.A.; Lahiri, G.K.
Indian Journal of Chemistry. Section A: Inorganic, Physical, Theoretical and Analytical; v. 35(11); ISSN 0376-4710; CODEN IJCADU; Nov 1996; p. 946-951
- A novel example of metal mediated aromatic thiolation in ruthenium complex: crystal structure of RuII (SC6H4N:NC5H4N)2
Santra, B. K.; Thakur G. A.; Ghosh, P.; Pramanik, A.; Lahiri, G. K.
Inorganic Chemistry, 35 (10). pp. 3050-3052. ISSN 0020-1669
- Synthesis, characterization and redox properties of ruthenium (II) dithiocarbonato complexes having 2,2'-bipyridine co-ligands
Thakur, G. A.; Narayanswami, K.; Lahiri, G. K.
Indian Journal of Chemistry. Section A: Inorganic, Physical, Theoretical and Analytical; v. 35(5); ISSN 0376-4710; CODEN IJCADU; May 1996; p. 379-384
- A convenient and effective synthesis of 3-(3,5-Dimethoxyphenyl)propanal
Nikas, S. P., Thakur, G. A., Makriyannis, A.
Synthetic Communications, Volume 32, Issue 11, 2002, pages 1751-1756
- Cannabinergic Ligands
Palmer, S. L.; Thakur, G. A.; Makriyannis, A.
Chem Phys Lipids. 2002 Dec 31;121(1-2):3-19.
- Synthesis of side chain specifically deuterated(-)-d9-tetrahydrocannabinoids
Nikas, S. P.; Thakur,G. A. and Makriyannis, A.
J Label Compd Radiopharm 2002; 45: 1065–1076.
- Regiospecifically deuterated (-)-d9-tetrahydrocannabivarins
Nikas, S. P., Thakur, G. A., Makriyannis, A.
J. Chem. Soc. Perkin. Trans.1, 2002, 22, 2544-2548
- Enantiomeric resolution of a novel chiral cannabinoid receptor ligand
Thakur, G. A., Palmer, S., Harrington, P. E., Stergiades, I. A., Tius, M. A., Makriyannis, A.
J. Biochem. Biophys. Methods, 2002, 54(1-3), 415-422.
- Adamantyl Cannabinoids: A novel class of cannabinergic ligands
Lu, D., Meng, Z., Thakur, G. A., Fan, P., Steed, J., Tartal, C. L., Hurst, D. P., Reggio, P. H., Deschamps, J. R., Parrish, D. A., George, C., Jarbe, T. U., Lamb, R. J., Makriyannis, A.
J. Med. Chem., 2005, 48 (14), 4576-4585
- Behavioral effects of the novel cannabinoid CB1 agonist AM411
10. McLaughlin, P. J., Lu, D., Winston, K. M., Thakur, G. A., Swezey, L. A., Makriyannis, A., Salamone, J. D.
Pharmacol. Biochem. Behav., 2005, 81(1), 78-88
- The novel cannabinoid agonist AM 411 produces a biphasic effect on accuracy in a visual target detection task in rats
McLaughlin, P. J., Brown, C. M., Winston, K. M., Thakur, G. A., Lu, D., Makriyannis, A., Salamone, J. D.
Behav. Pharmacol., 2005, 16(5-6), 477-486
- (-)-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 receptor
Picone, R. P., Khanolkar, A. D., Xu, W., Ayotte L. A., Thakur, G. A., Hurst, D. P., Abood, M. E., Reggio, P. H., Fourier, D. J., Makriyannis, A.
Mol. Pharmacol., 2005, 68 (6), 1623-1635
- CB1 Cannabinoid receptor ligands
Thakur, G. A., Nikas, S. P., Makriyannis, A.
Mini Reviews in Medicinal Chemistry, 2005, 5(7), 631-640
- Natural cannabinoids: templates for drug discovery
Thakur, G. A., Duclos, R.,I.,Jr., Makriyannis, A.
Life Sci., 2005, 78(5), 454-466
- Cannabinoid receptors as therapeutic targets
Pavlopoulos, S., Thakur, G. A., Nikas, S. P., Makriyannis, A.
Curr. Pharm. Design, 2006, 12(14), 1751-1769
- Mutation studies of Ser7.39 and Ser2.60 in the human CB1 cannabinoid receptor: evidence for a serine induced bend in CB1 transmembrane helix 7
Kapur, A., Hurst, D. P., Fleischer, D., Whitnell, R., Thakur, G. A., Makriyannis, A., Reggio, P. H., Abood, M. E.
Mol. Pharmacol., 2007, 71(6), 1512-1524
- A concise methodology for the synthesis of (−)-Δ9-tetrahydrocannabinol and (−)-Δ9-tetrahydrocannabivarin metabolites and their regiospecifically deuterated analogs
Nikas, S. P., Thakur, G. A., Parrish, D. A., Alapafuja, S. O., Huestis, M., Makriyannis, A.
Tetrahedron, 2007, 63, 8112-8123
- Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity
Khanolkar, A. D., Lu, D., Ibrahim, M., Duclos, R.I. Jr., Thakur, G. A., Malan, T. P. Jr., Porreca, F., Veerappan, V., Tian, X., George, C., Parrish, D. A., Papahatjis, D. P., Makriyannis, A.
J. Med. Chem., 2007, 50 (26), 6493-6500
- The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats
Sink, K.S., McLaughlin, P.J., Wood, J.A., Brown, C., Fan, P., Vemuri, V.K., Peng, Y., Olzewska, T., Thakur, G.A., Makriyannis, A., Parker, L.A., Salamone, J.D.
Neuropsychopharmacology, 2008, 33(4), 946-955
- Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction
Kapur, A., Samaniego, P., Thakur, G. A., Makriyannis, A., Abood, M. E.
JPET, 2008, 325 (1), 341-8
- Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties
Bergman, J., Delatte, M. S., Paronis, C. A., Vemuri, V. K., Thakur, G. A., Makriyannis, A.
Physiol. Behav., 2008, 93(4-5), 666-70
- Selective activation of cannabinoid CB2 receptors suppresses neuropathic nociception induced by treatment with the chemotherapeutic agent paclitaxel in rats
Rahn, E. J., Zvonok, A. M., Thakur, G. A., Khanolkar, A. D., Makriyannis, A., Hohmann, A. G.
JPET., 2008, 327(2), 584-91
- Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for a receptor subtype-specific binding motif and modeling GPCR activation
Pei, Y., Mercier, R. W., Anday, J. K., Thakur, G. A., Zvonok, A. M., Reggio, P. H., Janero, D. R., Makriyannis, A.
Chem. Biol., 2008, 15(11), 1207-19
- Intracerebroventricular administration of cannabinoid CB1 receptor antagonists AM251 and AM4113 fails to alter food-reinforced behavior in rats
Sink K. S., Segovia K. N., Nunes E. J., Collins L. E., Vemuri V. K., Thakur G. A., Makriyannis A., Salamone J. D
Pschopharmacology (Berl.), 2009, 206(2), 223-232
- Recent advances in cannabinoid receptor agonist
Thakur, G. A٭,.Tichkule, R., Bajaj, S., Makriyannis, A.
Expert Opinion on Therapeutic Patents. 2009, 19 (12), 1647-73
- Heteroadamantyl Cannabinoids
Dixon, D. D., Sethumadhavan, D., Benneche, T., Banaag, A. R., Tius, M. A., Thakur, G. A., Bowman, A., Wood, J., Makriyannis, A.
J. Med. Chem., 2010, 53(15), 5656-66
- Pharmacological characterization of putative cannabinoid CB2 agonist from the cannabilactone class: Antinociception without central nervous system side-effects
Rahn, E., Thakur, G. A., Zvonok, A. M., Vemuri, V. K., Makriaynnis, A., Hohmann, A. G.
Pharmacology, Biochemistry & Behavior, 2011, 98, 493-502
- Conformationally restricted analogs of BAY59-3074 as novel cannabinoid receptor ligands
Teng, H., Thakur, G. A., Makriyanis, A
Bioorg. Med. Chem. Lett., 2011, 21, 5999-6002
- Mass spectrometry-based proteomics of human cannabinoid receptor 2: covalent cysteine 6.47(257)-ligand interaction affording megagonist receptor activation
Szymanski,D. W., Papanastasiou, M., Melchior, K., Zvonok, N., Mercier, R. W., Janero, D. R.,
Thakur, G. A., Cha, S., Wu, B., Karger, B., Makriyannis, A
J. Proteom. Res. 2011, 10, 4789-4798
- Immunofluorescent spectral analysis reveals the intrathecal cannabinoid agonist, AM1241, produces spinal anti-inflammatory cytokine responses in neuropathic rats exhibiting relief from allodynia
Wilkerson, J.L., Gentry, K.R., Dengler, E.C., Wallace, J.A., Kerwin, A.A., Kuhn, M.N., Zvonok, A.M., Thakur, G.A., Makriyannis, A., Milligan, E.D.
Brain and Behaviour, 2012, 2(2), 155-177
- Intrathecal cannabilactone CB(2)R agonist, AM1710, controls pathological pain and restores basal cytokine levels
Wilkerson, J.L., Gentry, K.R., Dengler, E.C., Wallace, J.A., Kerwin, A.A., Armijo, L.M., Kuhn, M.N., Thakur, G.A., Makriyannis, A., Milligan, E.D.
Pain, 2012, 153(5), 1091-1106
- C3-Heteroaroyl cannabinoids as photolabeling ligands for the CB2 cannabinoid receptor
Dixon, D.D., Tius, M.A., Thakur, G.A., Zhou, H., Bowman, A.L., Shukla, V.G., Peng, Y., Makriyannis, A.
Bioorg Med Chem Lett., 2012, 22(16), 5322-5325
- 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 neuropathy
Deng, L., Guindon, J., Vemuri, K.V., Thakur, G.A., White, F.A., Makriyannis, A., Hohmann, A.
Molecular Pain 2012, 8: 71
- Analysis of tolerance and behavioral/physical dependence during chronic CB1 agonist treatment: effects of CB1 agonists, antagonists, and noncannabinoid drugs
Desai, R.V., Thakur, G.A., Vemuri, K.V., Bajaj, S.B., Makriyannis, A., Bergman, A.
JPET, 2013, 344, 319-328
- Diuretic Effects of Cannabinoids
Paronis, C.A., Thakur, G.A., Bajaj, S.B., Nikas, S.P., Vemuri, K.V., Makriyannis, A., Bergman, J.
JPET, 2013, 314, 8-14
- Novel Adamantyl Cannabinoids as CB1 Receptor Probes
Thakur, G.A.*, Bajaj, S.B., Paronis, C.A., Peng, Y., Bowman, A.L. Barak, L., Caron, M.G. Parrish, D.A., Deschamps, J., Makriyannis, A.
J. Med. Chem. 2013, 6(10):3904-3921
- Behavioral effects of the novel potent cannabinoid CB1 agonist AM4054
McLaughlin, P.J., Thakur, G.A., McClure, E.D., Brown, C.M., Winston, K.M., Wood, J.T., Makriyannis, A., Salamone, J.D.
Pharmcol. Biochem. Behav. 2013, 119:16-22
- Effects of a novel CB1 agonist on visual attention in male rats: role of strategy and expectancy in task accuracy
Miller R.L., Thakur G.A., Stewart W.N., Bow J.P., Bajaj S., Makriyannis A., McLaughlin P.J.
Exp Clin Psychopharmacol. 2013; 21(5):416-25
- Cannabinoid discrimination and antagonism by CB(1) neutral and inverse agonist antagonists
Kangas BD, Delatte M.S., Vemuri V.K., Thakur GA, Nikas SP, Subramanian KV, Shukla VG, Makriyannis A, Bergman J.
J. Pharmacol. Exp. Ther. 2013, 344(3):561-567
- Cannabinoid discrimination and antagonism by CB(1) neutral and inverse agonist antagonists
Kangas BD, Delatte M.S., Vemuri V.K., Thakur GA, Nikas SP, Subramanian KV, Shukla VG, Makriyannis A, Bergman J.
J. Pharmacol. Exp. Ther. 2013, 344(3):561-567
- Microwave-assisted expeditious and efficient synthesis of cyclopentene ring-fused tetrahydroquinoline derivatives using three-component Povarov reaction
Kulkarni AR, Thakur G.A.*
Tetrahedron Lett. 2013, 54(48), 6592-6595
- 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 Acetylcholine Receptors
Thakur GA*, Kulkarni AR, Deschamps JR, Papke RL
J. Med. Chem. 2013; 56(21):8943-7
- The activity of GAT107, an allosteric activator and positive modulator of α7 nAChR, is regulated by aromatic amino acids that span the subunit interface
Papke RL, Horenstein NA, Kulkarni AR, Stokes C, Corrie LW, Maeng CY, Thakur G.A.*
J. Biol. Chem. 2014, 289(7), 4515-4517
- Controlled-detoxification Cannabinergic Ligands
Sharma R, Nikas SP, Paronis CA, Wood JT, Halikhedkar A, Guo JJ, Thakur G.A., Kulkarni S, Benchama O, Raghav JG, Gifford RS, Järbe TU, Bergman J, Makriyannis A.
J. Med. Chem. 2013, 56(24):10142-10157
- Investigation of the in vivo pharmacological effects of the CB1 receptor allosteric modulator Org-27569
Gamage, T., Ignatowska-Jankowska, B. M., Abdelrahman, M., Trembleau. L., Thakur, G. A., Tichkule, R. B. ; Poklis, J. ; Ross, R. A., Pertwee, R. G. and Lichtman, A. H.
Behav Pharmacol. 2014 April ; 25(2): 182–185
- Prophylactic cannabinoid administration blocks the development of paclitaxel-induced neuropathic nociception during analgesic treatment and following cessation of drug delivery
Rahn, E.J., Deng, L., Thakur, G.A., Vemuri, V.K., Zvonok, A. M., Lai, Y. Y. Makriyannis, A. and Hohmann, A.G.
Molecular Pain. 2014, 10(1):27
Book Chapters
- Structural requirements for cannabinoid receptor probes
Thakur, G. A., Nikas, S. P., Li, C., Makriyannis, A.
Handbook of Experimental Pharmacology, 2005, 168, 209-246
- Methods for the synthesis of cannabinergic ligands
2. Thakur, G. A., Nikas, S. P., Duclos, R. I., Jr., Makriyannis, A.
Methods Mol. Med., 2006, 123, 113-148