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Expert Opinion on Drug Discovery Volume 6, 2011 - Issue 10
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Cannabinoid 1 G protein-coupled receptor (periphero-)neutral antagonists: emerging therapeutics for treating obesity-driven metabolic disease and reducing cardiovascular risk

David R Janero Northeastern University, Center for Drug Discovery, 360 Huntington Avenue, 116 Mugar Hall, Boston, MA 02115-5000, USA+1 617 373 2208; +1 617 373 7493; [email protected]
,
Loren Lindsley Northeastern University, Center for Drug Discovery, 360 Huntington Avenue, 116 Mugar Hall, Boston, MA 02115-5000, USA+1 617 373 2208; +1 617 373 7493; [email protected];Novartis Institutes for BioMedical Research, Cardiovascular and Metabolism Disease Area, Cambridge, MA 02139, USA
,
Venkata Kiran Vemuri Northeastern University, Center for Drug Discovery, 360 Huntington Avenue, 116 Mugar Hall, Boston, MA 02115-5000, USA+1 617 373 2208; +1 617 373 7493; [email protected]
&
Alexandros Makriyannis Northeastern University, Center for Drug Discovery, 360 Huntington Avenue, 116 Mugar Hall, Boston, MA 02115-5000, USA+1 617 373 2208; +1 617 373 7493; [email protected]
Pages 995-1025 | Published online: 02 Sep 2011

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David R. Janero & Ganesh A. Thakur. (2016) Leveraging allostery to improve G protein-coupled receptor (GPCR)-directed therapeutics: cannabinoid receptor 1 as discovery target. Expert Opinion on Drug Discovery 11:12, pages 1223-1237.
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David R Janero. (2014) Medications development for substance-use disorders: contextual influences (dis)incentivizing pharmaceutical-industry positioning. Expert Opinion on Drug Discovery 9:11, pages 1265-1279.
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David R Janero. (2014) Synthetic agents in the context of metabolic/bariatric surgery: expanding the scope and impact of diabetes drug discovery. Expert Opinion on Drug Discovery 9:3, pages 221-228.
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David R. Janero. (2012) Cannabinoid-1 receptor (CB1R) blockers as medicines: beyond obesity and cardiometabolic disorders to substance abuse/drug addiction with CB1R neutral antagonists. Expert Opinion on Emerging Drugs 17:1, pages 17-29.
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Articles from other publishers (13)

Tao Jiang, Chuyun Xu, Huifang Liu, Muyi Liu, Minmin Wang, Jiarui Jiang, Guangji Zhang, Chuqi Yang, Jianbo Huang & Zhaohuan Lou. (2021) Linderae Radix Ethanol Extract Alleviates Diet-Induced Hyperlipidemia by Regulating Bile Acid Metabolism Through gut Microbiota. Frontiers in Pharmacology 12.
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Silvana Russo & Walter Filgueira De Azevedo. (2019) Advances in the Understanding of the Cannabinoid Receptor 1 – Focusing on the Inverse Agonists Interactions. Current Medicinal Chemistry 26:10, pages 1908-1919.
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Vincenzo Micale, Filippo Drago, Pia K. Noerregaard, Christian E. Elling & Carsten T. Wotjak. (2019) The Cannabinoid CB1 Antagonist TM38837 With Limited Penetrance to the Brain Shows Reduced Fear-Promoting Effects in Mice. Frontiers in Pharmacology 10.
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David R. Janero, V. Kiran Vemuri & Alexandros Makriyannis. 2019. Cannabis Use Disorders. Cannabis Use Disorders 43 54 .
Srikrishnan Mallipeddi, David R. Janero, Nikolai Zvonok & Alexandros Makriyannis. (2017) Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets. Biochemical Pharmacology 128, pages 1-11.
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Stephan Hjorth, Cecilia Karlsson, Aurelija Jucaite, Katarina Varnäs, Ulrika Wählby Hamrén, Peter Johnström, Balázs Gulyás, Sean R. Donohue, Victor W. Pike, Christer Halldin & Lars Farde. (2016) A PET study comparing receptor occupancy by five selective cannabinoid 1 receptor antagonists in non-human primates. Neuropharmacology 101, pages 519-530.
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David R. Janero, Suma Yaddanapudi, Nikolai Zvonok, Kumar V. Subramanian, Vidyanand G. Shukla, Edward Stahl, Lei Zhou, Dow Hurst, James Wager-Miller, Laura M. Bohn, Patricia H. Reggio, Ken Mackie & Alexandros Makriyannis. (2015) Molecular-Interaction and Signaling Profiles of AM3677, a Novel Covalent Agonist Selective for the Cannabinoid 1 Receptor. ACS Chemical Neuroscience 6:8, pages 1400-1410.
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David R. Janero & Alexandros Makriyannis. (2014) Terpenes and Lipids of the Endocannabinoid and Transient-Receptor-Potential-Channel Biosignaling Systems. ACS Chemical Neuroscience 5:11, pages 1097-1106.
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Alexandros Makriyannis. (2014) 2012 Division of Medicinal Chemistry Award Address. Trekking the Cannabinoid Road: A Personal Perspective. Journal of Medicinal Chemistry 57:10, pages 3891-3911.
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Chun-Ping ChangChien-Huang WuJen-Shin SongMing-Chen ChouYing-Chieh WongYinchiu LinTeng-Kuang YehAmit A. SadaniMing-Hung OuKun-Hung ChenPei-Hsuan ChenPo-Chu KuoChen-Tso TsengKuei-Hua ChangShi-Liang TsengYu-Sheng ChaoMing-Shiu HungKak-Shan Shia. (2013) Discovery of 1-(2,4-Dichlorophenyl)- N -(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1 H -pyrazole-3-carboxamide as a Novel Peripherally Restricted Cannabinoid-1 Receptor Antagonist with Significant Weight-Loss Efficacy in Diet-Induced Obese Mice . Journal of Medicinal Chemistry 56:24, pages 9920-9933.
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Yue Ye Huang, Aaron M Gusdon & Shen Qu. (2013) Nonalcoholic fatty liver disease: molecular pathways and therapeutic strategies. Lipids in Health and Disease 12:1.
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Detlef Schuppan & Jörn M Schattenberg. (2013) Non-alcoholic steatohepatitis: Pathogenesis and novel therapeutic approaches. Journal of Gastroenterology and Hepatology 28, pages 68-76.
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E T Wargent, M S Zaibi, C Silvestri, D C Hislop, C J Stocker, C G Stott, G W Guy, M Duncan, V Di Marzo & M A Cawthorne. (2013) The cannabinoid Δ9-tetrahydrocannabivarin (THCV) ameliorates insulin sensitivity in two mouse models of obesity. Nutrition & Diabetes 3:5, pages e68-e68.
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