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Cannabinoid CB1 receptor neutral antagonist AM4113 inhibits heroin self-administration without depressive side effects in rats.

He XH, Jordan CJ, Vemuri K, Bi GH, Zhan J, Gardner EL, Makriyannis A, Wang YL, Xi ZX.

Acta Pharmacol Sin. 2018 Jul 2. doi: 10.1038/s41401-018-0059-x. [Epub ahead of print]


Controlled-Deactivation CB1 Receptor Ligands as a Novel Strategy to Lower Intraocular Pressure.

Miller S, Kulkarni S, Ciesielski A, Nikas SP, Mackie K, Makriyannis A, Straiker A.

Pharmaceuticals (Basel). 2018 May 22;11(2). pii: E50. doi: 10.3390/ph11020050.


Hydrogen-Deuterium Exchange Mass Spectrometry to Study Protein Complexes.

Kochert BA, Iacob RE, Wales TE, Makriyannis A, Engen JR.

Methods Mol Biol. 2018;1764:153-171. doi: 10.1007/978-1-4939-7759-8_10.


A lethal synergy induced by phellinus linteus and camptothecin11 in colon cancer cells.

Yu T, Ganapathy S, Shen L, Peng B, Kim SH, Makriyannis A, Chen C.

Oncotarget. 2018 Jan 4;9(5):6308-6319. doi: 10.18632/oncotarget.23918. eCollection 2018 Jan 19.


Expression, Purification and Characterization of the Human Cannabinoid 1 Receptor.

Mallipeddi S, Zvonok N, Makriyannis A.

Sci Rep. 2018 Feb 13;8(1):2935. doi: 10.1038/s41598-018-19749-5.


Effects of Distal Mutations on the Structure, Dynamics and Catalysis of Human Monoacylglycerol Lipase.

Tyukhtenko S, Rajarshi G, Karageorgos I, Zvonok N, Gallagher ES, Huang H, Vemuri K, Hudgens JW, Ma X, Nasr ML, Pavlopoulos S, Makriyannis A.

Sci Rep. 2018 Jan 29;8(1):1719. doi: 10.1038/s41598-017-19135-7.


Long-Lasting In Vivo Effects of the Cannabinoid CB1 Antagonist AM6538.

Paronis CA, Chopda GR, Vemuri K, Zakarian AS, Makriyannis A, Bergman J.

J Pharmacol Exp Ther. 2018 Mar;364(3):485-493. doi: 10.1124/jpet.117.245647. Epub 2018 Jan 8.


Secretion, isotopic labeling and deglycosylation of N-acylethanolamine acid amidase for biophysical studies.

Pavlopoulos S, Pelekoudas DN, Benchama O, Rawlins CM, Agar JN, West JM, Malamas M, Zvonok N, Makriyannis A.

Protein Expr Purif. 2018 May;145:108-117. doi: 10.1016/j.pep.2017.12.005. Epub 2017 Dec 15.


Cannabinoid-1 receptor neutral antagonist reduces binge-like alcohol consumption and alcohol-induced accumbal dopaminergic signaling.

Balla A, Dong B, Shilpa BM, Vemuri K, Makriyannis A, Pandey SC, Sershen H, Suckow RF, Vinod KY.

Neuropharmacology. 2018 Mar 15;131:200-208. doi: 10.1016/j.neuropharm.2017.10.040. Epub 2017 Nov 3.


Adipocyte cannabinoid receptor CB1 regulates energy homeostasis and alternatively activated macrophages.

Ruiz de Azua I, Mancini G, Srivastava RK, Rey AA, Cardinal P, Tedesco L, Zingaretti CM, Sassmann A, Quarta C, Schwitter C, Conrad A, Wettschureck N, Vemuri VK, Makriyannis A, Hartwig J, Mendez-Lago M, Bindila L, Monory K, Giordano A, Cinti S, Marsicano G, Offermanns S, Nisoli E, Pagotto U, Cota D, Lutz B.

J Clin Invest. 2017 Nov 1;127(11):4148-4162. doi: 10.1172/JCI83626. Epub 2017 Oct 16.


Cannabinoid CB1 Discrimination: Effects of Endocannabinoids and Catabolic Enzyme Inhibitors.

Leonard MZ, Alapafuja SO, Ji L, Shukla VG, Liu Y, Nikas SP, Makriyannis A, Bergman J, Kangas BD.

J Pharmacol Exp Ther. 2017 Dec;363(3):314-323. doi: 10.1124/jpet.117.244392. Epub 2017 Sep 25.


The role of human monoacylglycerol lipase (hMAGL) binding pocket in breakup of unsaturated phospholipid membranes.

Karageorgos I, Silin VI, Zvonok N, Marino J, Janero DR, Makriyannis A.

Anal Biochem. 2017 Nov 1;536:90-95. doi: 10.1016/j.ab.2017.08.009. Epub 2017 Aug 17.


Inhibitor of Endocannabinoid Deactivation Protects Against In Vitro and In Vivo Neurotoxic Effects of Paraoxon.

Farizatto KLG, McEwan SA, Naidoo V, Nikas SP, Shukla VG, Almeida MF, Byrd A, Romine H, Karanian DA, Makriyannis A, Bahr BA.

J Mol Neurosci. 2017 Sep;63(1):115-122. doi: 10.1007/s12031-017-0963-4. Epub 2017 Aug 12.


Ligand-Assisted Protein Structure (LAPS): An Experimental Paradigm for Characterizing Cannabinoid-Receptor Ligand-Binding Domains.

Janero DR, Korde A, Makriyannis A.

Methods Enzymol. 2017;593:217-235. doi: 10.1016/bs.mie.2017.06.022. Epub 2017 Jul 3.


CB₁ receptor antagonism in the bed nucleus of the stria terminalis interferes with affective opioid withdrawal in rats.

Wills KL, DeVuono MV, Limebeer CL, Vemuri K, Makriyannis A, Parker LA.

Behav Neurosci. 2017 Aug;131(4):304-11. doi: 10.1037/bne0000201.


Crystal structures of agonist-bound human cannabinoid receptor CB1.

Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ.

Nature. 2017 Jul 27;547(7664):468-471. doi: 10.1038/nature23272. Epub 2017 Jul 5.


C1'-Azacycloalkyl Hexahydrocannabinols.

Ho TC, Shimada N, Tius MA, Nikas SP, Zhang W, Makriyannis A.

J Org Chem. 2017 Aug 4;82(15):7839-7849. doi: 10.1021/acs.joc.7b00988. Epub 2017 Jul 17.


s signalling of the CB1 receptor and the influence of receptor number.

Finlay DB, Cawston EE, Grimsey NL, Hunter MR, Korde A, Vemuri VK, Makriyannis A, Glass M.

Br J Pharmacol. 2017 Aug;174(15):2545-2562. doi: 10.1111/bph.13866. Epub 2017 Jun 19.


Suppression of PKC causes oncogenic stress for triggering apoptosis in cancer cells.

Ganapathy S, Peng B, Shen L, Yu T, Lafontant J, Li P, Xiong R, Makriyannis A, Chen C.

Oncotarget. 2017 May 9;8(19):30992-31002. doi: 10.18632/oncotarget.16047.


Dual therapy targeting the endocannabinoid system prevents experimental diabetic nephropathy.

Barutta F, Grimaldi S, Gambino R, Vemuri K, Makriyannis A, Annaratone L, di Marzo V, Bruno G, Gruden G.

Nephrol Dial Transplant. 2017 Oct 1;32(10):1655-1665. doi: 10.1093/ndt/gfx010.


Binding Site Characterization of AM1336, a Novel Covalent Inverse Agonist at Human Cannabinoid 2 Receptor, Using Mass Spectrometric Analysis.

Mallipeddi S, Kreimer S, Zvonok N, Vemuri K, Karger BL, Ivanov AR, Makriyannis A.

J Proteome Res. 2017 Jul 7;16(7):2419-2428. doi: 10.1021/acs.jproteome.7b00023. Epub 2017 Jun 19.


Human Cannabinoid Receptor 2 Ligand-Interaction Motif: Transmembrane Helix 2 Cysteine, C2.59(89), as Determinant of Classical Cannabinoid Agonist Activity and Binding Pose.

Zhou H, Peng Y, Halikhedkar A, Fan P, Janero DR, Thakur GA, Mercier RW, Sun X, Ma X, Makriyannis A.

ACS Chem Neurosci. 2017 Jun 21;8(6):1338-1347. doi: 10.1021/acschemneuro.7b00003. Epub 2017 Mar 1.


Differential effects of cannabinoid CB1 inverse agonists and antagonists on impulsivity in male Sprague Dawley rats: identification of a possibly clinically relevant vulnerability involving the serotonin 5HT1A receptor.

McLaughlin PJ, Jagielo-Miller JE, Plyler ES, Schutte KK, Vemuri VK, Makriyannis A.

Psychopharmacology (Berl). 2017 Mar;234(6):1029-1043. doi: 10.1007/s00213-017-4548-2. Epub 2017 Feb 1.


N-acylethanolamine-hydrolyzing acid amidase and fatty acid amide hydrolase inhibition differentially affect N-acylethanolamine levels and macrophage activation.

Alhouayek M, Bottemanne P, Makriyannis A, Muccioli GG.

Biochim Biophys Acta. 2017 May;1862(5):474-484. doi: 10.1016/j.bbalip.2017.01.001. Epub 2017 Jan 6.


Two Janus Cannabinoids That Are Both CB2 Agonists and CB1 Antagonists.

Dhopeshwarkar A, Murataeva N, Makriyannis A, Straiker A, Mackie K.

J Pharmacol Exp Ther. 2017 Feb;360(2):300-311. doi: 10.1124/jpet.116.236539. Epub 2016 Dec 7.


Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets.

Mallipeddi S, Janero DR, Zvonok N, Makriyannis A.

Biochem Pharmacol. 2017 Mar 15;128:1-11. doi: 10.1016/j.bcp.2016.11.014. Epub 2016 Nov 24. Review.


Prophylactic treatment with the tricyclic antidepressant desipramine prevents development of paclitaxel-induced neuropathic pain through activation of endogenous analgesic systems.

Deng L, Lee WH, Xu Z, Makriyannis A, Hohmann AG.

Pharmacol Res. 2016 Dec;114:75-89. doi: 10.1016/j.phrs.2016.10.007. Epub 2016 Oct 20.


Crystal Structure of the Human Cannabinoid Receptor CB1.

Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S, Korde A, Laprairie RB, Stahl EL, Ho JH, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ.

Cell. 2016 Oct 20;167(3):750-762.e14. doi: 10.1016/j.cell.2016.10.004.


Ral A, via activating the mitotic checkpoint, sensitizes cells lacking a functional Nf1 to apoptosis in the absence of protein kinase C.

Ganapathy S, Fagman JB, Shen L, Yu T, Zhou X, Dai W, Makriyannis A, Chen C.

Oncotarget. 2016 Dec 20;7(51):84326-84337. doi: 10.18632/oncotarget.12607.


Acute and chronic effects of cannabidiol on Δ⁹-tetrahydrocannabinol (Δ⁹-THC)-induced disruption in stop signal task performance.

Jacobs DS, Kohut SJ, Jiang S, Nikas SP, Makriyannis A, Bergman J.

Exp Clin Psychopharmacol. 2016 Oct;24(5):320-330. Epub 2016 Aug 15.


The CB1 Neutral Antagonist AM4113 Retains the Therapeutic Efficacy of the Inverse Agonist Rimonabant for Nicotine Dependence and Weight Loss with Better Psychiatric Tolerability.

Gueye AB, Pryslawsky Y, Trigo JM, Poulia N, Delis F, Antoniou K, Loureiro M, Laviolette SR, Vemuri K, Makriyannis A, Le Foll B.

Int J Neuropsychopharmacol. 2016 Dec 30;19(12). pii: pyw068. doi: 10.1093/ijnp/pyw068. Print 2016 Dec.


Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.

Kulkarni S, Nikas SP, Sharma R, Jiang S, Paronis CA, Leonard MZ, Zhang B, Honrao C, Mallipeddi S, Raghav JG, Benchama O, Järbe TU, Bergman J, Makriyannis A.

J Med Chem. 2016 Jul 28;59(14):6903-19. doi: 10.1021/acs.jmedchem.6b00717. Epub 2016 Jul 13.


A high efficacy cannabinergic ligand (AM4054) used as a discriminative stimulus: Generalization to other adamantyl analogs and Δ(9)-THC in rats.

Järbe TU, LeMay BJ, Thakur GA, Makriyannis A.

Pharmacol Biochem Behav. 2016 Sep;148:46-52. doi: 10.1016/j.pbb.2016.06.001. Epub 2016 Jun 2.


Tolerance to the Diuretic Effects of Cannabinoids and Cross-Tolerance to a κ-Opioid Agonist in THC-Treated Mice.

Chopda GR, Parge V, Thakur GA, Gatley SJ, Makriyannis A, Paronis CA.

J Pharmacol Exp Ther. 2016 Aug;358(2):334-41. doi: 10.1124/jpet.116.232132. Epub 2016 May 26.


A comparison of novel, selective fatty acid amide hydrolase (FAAH), monoacyglycerol lipase (MAGL) or dual FAAH/MAGL inhibitors to suppress acute and anticipatory nausea in rat models.

Parker LA, Limebeer CL, Rock EM, Sticht MA, Ward J, Turvey G, Benchama O, Rajarshi G, Wood JT, Alapafuja SO, Makriyannis A.

Psychopharmacology (Berl). 2016 Jun;233(12):2265-75. doi: 10.1007/s00213-016-4277-y. Epub 2016 Apr 6.


Endocannabinoid Signaling Regulates Sleep Stability.

Pava MJ, Makriyannis A, Lovinger DM.

PLoS One. 2016 Mar 31;11(3):e0152473. doi: 10.1371/journal.pone.0152473. eCollection 2016.


CB1 antagonism produces behaviors more consistent with satiety than reduced reward value in food-maintained responding in rats.

Thompson EE, Jagielo-Miller JE, Vemuri VK, Makriyannis A, McLaughlin PJ.

J Psychopharmacol. 2016 May;30(5):482-91. doi: 10.1177/0269881116639287. Epub 2016 Mar 22.


Effects of various cannabinoid ligands on choice behaviour in a rat model of gambling.

Gueye AB, Trigo JM, Vemuri KV, Makriyannis A, Le Foll B.

Behav Pharmacol. 2016 Apr;27(2-3 Spec Issue):258-69. doi: 10.1097/FBP.0000000000000222.


Blockade of Nicotine and Cannabinoid Reinforcement and Relapse by a Cannabinoid CB1-Receptor Neutral Antagonist AM4113 and Inverse Agonist Rimonabant in Squirrel Monkeys.

Schindler CW, Redhi GH, Vemuri K, Makriyannis A, Le Foll B, Bergman J, Goldberg SR, Justinova Z.

Neuropsychopharmacology. 2016 Aug;41(9):2283-93. doi: 10.1038/npp.2016.27. Epub 2016 Feb 18.


Comparisons of Δ9-Tetrahydrocannabinol and Anandamide on a Battery of Cognition-Related Behavior in Nonhuman Primates.

Kangas BD, Leonard MZ, Shukla VG, Alapafuja SO, Nikas SP, Makriyannis A, Bergman J.

J Pharmacol Exp Ther. 2016 Apr;357(1):125-33. doi: 10.1124/jpet.115.228189. Epub 2016 Jan 29.


Self-administration of the anandamide transport inhibitor AM404 by squirrel monkeys.

Schindler CW, Scherma M, Redhi GH, Vadivel SK, Makriyannis A, Goldberg SR, Justinova Z.

Psychopharmacology (Berl). 2016 May;233(10):1867-77. doi: 10.1007/s00213-016-4211-3. Epub 2016 Jan 23.


17β-estradiol (E2) in membranes: Orientation and dynamic properties.

Guo JJ, Yang DP, Tian X, Vemuri VK, Yin D, Li C, Duclos RI Jr, Shen L, Ma X, Janero DR, Makriyannis A.

Biochim Biophys Acta. 2016 Feb;1858(2):344-53. doi: 10.1016/j.bbamem.2015.11.015. Epub 2015 Dec 1.


Effects of fatty acid amide hydrolase (FAAH) inhibitors on working memory in rats.

Panlilio LV, Thorndike EB, Nikas SP, Alapafuja SO, Bandiera T, Cravatt BF, Makriyannis A, Piomelli D, Goldberg SR, Justinova Z.

Psychopharmacology (Berl). 2016 May;233(10):1879-88. doi: 10.1007/s00213-015-4140-6. Epub 2015 Nov 12.


Specific Inter-residue Interactions as Determinants of Human Monoacylglycerol Lipase Catalytic Competency: A ROLE FOR GLOBAL CONFORMATIONAL CHANGES.

Tyukhtenko S, Karageorgos I, Rajarshi G, Zvonok N, Pavlopoulos S, Janero DR, Makriyannis A.

J Biol Chem. 2016 Feb 5;291(6):2556-65. doi: 10.1074/jbc.M115.670257. Epub 2015 Nov 10.


Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).

Kulkarni PM, Kulkarni AR, Korde A, Tichkule RB, Laprairie RB, Denovan-Wright EM, Zhou H, Janero DR, Zvonok N, Makriyannis A, Cascio MG, Pertwee RG, Thakur GA.

J Med Chem. 2016 Jan 14;59(1):44-60. doi: 10.1021/acs.jmedchem.5b01303. Epub 2015 Nov 28.


Protection from Radiation-Induced Pulmonary Fibrosis by Peripheral Targeting of Cannabinoid Receptor-1.

Bronova I, Smith B, Aydogan B, Weichselbaum RR, Vemuri K, Erdelyi K, Makriyannis A, Pacher P, Berdyshev EV.

Am J Respir Cell Mol Biol. 2015 Oct;53(4):555-62. doi: 10.1165/rcmb.2014-0331OC.


[INCREMENT]9-Tetrahydrocannabinol discriminative stimulus effects of AM2201 and related aminoalkylindole analogs in rats.

Järbe TU, Gifford RS, Zvonok A, Makriyannis A.

Behav Pharmacol. 2016 Apr;27(2-3 Spec Issue):211-4. doi: 10.1097/FBP.0000000000000196.


In vitro and non-invasive in vivo effects of the cannabinoid-1 receptor agonist AM841 on gastrointestinal motor function in the rat.

Abalo R, Chen C, Vera G, Fichna J, Thakur GA, López-Pérez AE, Makriyannis A, Martín-Fontelles MI, Storr M.

Neurogastroenterol Motil. 2015 Dec;27(12):1721-35. doi: 10.1111/nmo.12668. Epub 2015 Sep 20.


Molecular-interaction and signaling profiles of AM3677, a novel covalent agonist selective for the cannabinoid 1 receptor.

Janero DR, Yaddanapudi S, Zvonok N, Subramanian KV, Shukla VG, Stahl E, Zhou L, Hurst D, Wager-Miller J, Bohn LM, Reggio PH, Mackie K, Makriyannis A.

ACS Chem Neurosci. 2015 Aug 19;6(8):1400-10. doi: 10.1021/acschemneuro.5b00090. Epub 2015 May 29.


Design and synthesis of novel prostaglandin E2 ethanolamide and glycerol ester probes for the putative prostamide receptor(s).

Shelnut EL, Nikas SP, Finnegan DF, Chiang N, Serhan CN, Makriyannis A.

Tetrahedron Lett. 2015 Mar 11;56(11):1411-1415.

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