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Review

Latest advances in cannabinoid receptor antagonists and inverse agonists

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Pages 1405-1423 | Published online: 04 Oct 2006

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (4)

Mayank Kumar Sharma, Prashant R Murumkar, Mahesh A Barmade, Rajani Giridhar & Mange Ram Yadav. (2015) A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents. Expert Opinion on Therapeutic Patents 25:10, pages 1093-1116.
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Doris Riether. (2012) Selective cannabinoid receptor 2 modulators: a patent review 2009 – present. Expert Opinion on Therapeutic Patents 22:5, pages 495-510.
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E Kate Högenauer. (2007) Latest advances in the cannabinoids. Expert Opinion on Therapeutic Patents 17:12, pages 1457-1476.
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Didier M Lambert. (2007) CB1 cannabinoid receptor antagonism for treating inflammation and arthritis. Expert Opinion on Therapeutic Patents 17:8, pages 1027-1031.
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Articles from other publishers (25)

Luying Chen, Ge Yan & Tomohiko Ohwada. (2022) Building on endogenous lipid mediators to design synthetic receptor ligands. European Journal of Medicinal Chemistry 231, pages 114154.
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Mayank Kumar Sharma, Prashant R. Murumkar, Ashish M. Kanhed, Rajani Giridhar & Mange Ram Yadav. (2014) Prospective therapeutic agents for obesity: Molecular modification approaches of centrally and peripherally acting selective cannabinoid 1 receptor antagonists. European Journal of Medicinal Chemistry 79, pages 298-339.
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Mukesh C. Sharma. (2013) Discovery of new lead pyrimidines derivatives as potential cannabinoid CB1 receptor antagonistic through molecular modeling and pharmacophore approach. Medicinal Chemistry Research 23:5, pages 2287-2311.
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Linjing Mu, Daniel Bieri, Roger Slavik, Konstantin Drandarov, Adrienne Müller, Stjepko Čermak, Markus Weber, Roger Schibli, Stefanie D. Krämer & Simon M. Ametamey. (2013) Radiolabeling and in vitro / in vivo evaluation of N-(1-adamantyl)-8-methoxy-4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxamide as a PET probe for imaging cannabinoid type 2 receptor . Journal of Neurochemistry 126:5, pages 616-624.
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Mariko Kitajima, Masumi Iwai, Ruri Kikura-Hanajiri, Yukihiro Goda, Mitsuru Iida, Hisatoshi Yabushita & Hiromitsu Takayama. (2011) Discovery of indole alkaloids with cannabinoid CB1 receptor antagonistic activity. Bioorganic & Medicinal Chemistry Letters 21:7, pages 1962-1964.
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Mingzhang Gao, Min Wang, Kathy D. Miller, Gary D. Hutchins & Qi-Huang Zheng. (2010) Synthesis and in vitro biological evaluation of carbon-11-labeled quinoline derivatives as new candidate PET radioligands for cannabinoid CB2 receptor imaging. Bioorganic & Medicinal Chemistry 18:6, pages 2099-2106.
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Jos H.M. Lange, Martina A.W. van der Neut, Henri C. Wals, Gijs D. Kuil, Alice J.M. Borst, Arie Mulder, Arnold P. den Hartog, Hicham Zilaout, Wouter Goutier, Herman H. van Stuivenberg & Bernard J. van Vliet. (2010) Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies. Bioorganic & Medicinal Chemistry Letters 20:3, pages 1084-1089.
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Herbert H. Seltzman. (2009) Recent CB1 cannabinoid receptor antagonists and inverse agonists. Drug Development Research 70:8, pages 601-615.
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Jos H.M. Lange, Arnold P. den Hartog, Martina A.W. van der Neut, Bernard J. van Vliet & Chris G. Kruse. (2009) Synthesis and SAR of 1,4,5,6-tetrahydropyridazines as potent cannabinoid CB1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 19:19, pages 5675-5678.
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Brijesh Kumar Srivastava, Rina Soni, Jayendra Z. Patel, Amit Joharapurkar, Nisha Sadhwani, Samadhan Kshirsagar, Bhupendra Mishra, Vijay Takale, Sunil Gupta, Purvi Pandya, Prashant Kapadnis, Manish Solanki, Harilal Patel, Prasenjit Mitra, Mukul R. Jain & Pankaj R. Patel. (2009) Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect. Bioorganic & Medicinal Chemistry Letters 19:9, pages 2546-2550.
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Duen-Ren Hou, Safiul Alam, Ting-Chun Kuan, Mani Ramanathan, Tsung-Pang Lin & Ming-Shiu Hung. (2009) 1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 19:3, pages 1022-1025.
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Philippe Diaz, Sharangdhar S. Phatak, Jijun Xu, Fanny Astruc-Diaz, Claudio N. Cavasotto & Mohamed Naguib. (2008) 6-Methoxy- N -alkyl Isatin Acylhydrazone Derivatives as a Novel Series of Potent Selective Cannabinoid Receptor 2 Inverse Agonists: Design, Synthesis, and Binding Mode Prediction . Journal of Medicinal Chemistry 52:2, pages 433-444.
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Shi-Liang Tseng, Ming-Shiu Hung, Chun-Ping Chang, Jen-Shin Song, Chia-Liang Tai, Hua-Hao Chiu, Wan-Ping Hsieh, Yinchiu Lin, Wan-Ling Chung, Chun-Wei Kuo, Chien-Huang Wu, Cheng-Ming Chu, Yen-Shih Tung, Yu-Sheng Chao & Kak-Shan Shia. (2008) Bioisosteric Replacement of the Pyrazole 5-Aryl Moiety of N -(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1 H -pyrazole-3-carboxamide (SR141716A). A Novel Series of Alkynylthiophenes as Potent and Selective Cannabinoid-1 Receptor Antagonists . Journal of Medicinal Chemistry 51:17, pages 5397-5412.
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Serena Pasquini, Lorenzo Botta, Teresa Semeraro, Claudia Mugnaini, Alessia Ligresti, Enza Palazzo, Sabatino Maione, Vincenzo Di Marzo & Federico Corelli. (2008) Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 2. Synthesis and Structure−Activity Relationship of Potent and Selective Cannabinoid-2 Receptor Agonists Endowed with Analgesic Activity in Vivo. Journal of Medicinal Chemistry 51:16, pages 5075-5084.
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Daniel Pagé, Elise Balaux, Luc Boisvert, Ziping Liu, Claire Milburn, Maxime Tremblay, Zhongyong Wei, Simon Woo, Xuehong Luo, Yun-Xing Cheng, Hua Yang, Sanjay Srivastava, Fei Zhou, William Brown, Miroslaw Tomaszewski, Christopher Walpole, Leila Hodzic, Stéphane St-Onge, Claude Godbout, Dominic Salois & Keymal Payza. (2008) Novel benzimidazole derivatives as selective CB2 agonists. Bioorganic & Medicinal Chemistry Letters 18:13, pages 3695-3700.
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Romano SilvestriMaria Grazia CascioGiuseppe La ReginaFrancesco PiscitelliAntonio LavecchiaAntonella BrizziSerena PasquiniMaurizio BottaEttore NovellinoVincenzo Di MarzoFederico Corelli. (2008) Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1 H -pyrrol-1-yl)-1 H -pyrazole-3-carboxamides . Journal of Medicinal Chemistry 51:6, pages 1560-1576.
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Cheng-Ming Chu, Ming-Shiu Hung, Min-Tsang Hsieh, Chun-Wei Kuo, Suja T. D.Jen-Shin Song, Hua-Hao Chiu, Yu-Sheng Chao & Kak-Shan Shia. (2008) Bioisosteric replacement of the pyrazole 3-carboxamide moiety of rimonabant. A novel series of oxadiazoles as CB1 cannabinoid receptor antagonists. Organic & Biomolecular Chemistry 6:18, pages 3399.
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Chia-Liang Tai, Ming-Shiu Hung, Vijay D. Pawar, Shi-Liang Tseng, Jen-Shin Song, Wan-Ping Hsieh, Hua-Hao Chiu, Hui-Chuan Wu, Min-Tsang Hsieh, Chun-Wei Kuo, Chia-Chien Hsieh, Jing-Po Tsao, Yu-Sheng Chao & Kak-Shan Shia. (2008) Design, synthesis, and biological evaluation of novel alkenylthiophenes as potent and selective CB1 cannabinoid receptor antagonists. Org. Biomol. Chem. 6:3, pages 447-450.
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Didier M Lambert & Giulio G Muccioli. (2007) Endocannabinoids and related N-acylethanolamines in the control of appetite and energy metabolism: emergence of new molecular players. Current Opinion in Clinical Nutrition and Metabolic Care 10:6, pages 735-744.
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Amy J. Tallett, John E. Blundell & John R. Rodgers. (2007) Acute anorectic response to cannabinoid CB1 receptor antagonist/inverse agonist AM 251 in rats: indirect behavioural mediation. Behavioural Pharmacology 18:7, pages 591-600.
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Daniel Pagé, Hua Yang, William Brown, Christopher Walpole, Manon Fleurent, Meredith Fyfe, François Gaudreault & Stéphane St-Onge. (2007) New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. Bioorganic & Medicinal Chemistry Letters 17:22, pages 6183-6187.
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Giulio G. Muccioli. (2007) Blocking the Cannabinoid Receptors: Drug Candidates and Therapeutic Promises. Chemistry & Biodiversity 4:8, pages 1805-1827.
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Bruce A. Ellsworth, Ying Wang, Yeheng Zhu, Annapurna Pendri, Samuel W. Gerritz, Chongqing Sun, Kenneth E. Carlson, Liya Kang, Rose A. Baska, Yifan Yang, Qi Huang, Neil T. Burford, Mary Jane Cullen, Susan Johnghar, Kamelia Behnia, Mary Ann Pelleymounter, William N. Washburn & William R. Ewing. (2007) Discovery of pyrazine carboxamide CB1 antagonists: The introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series. Bioorganic & Medicinal Chemistry Letters 17:14, pages 3978-3982.
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Roger A. Smith, Zahra Fathi, Furahi Achebe, Christiana Akuche, Su-Ellen Brown, Soongyu Choi, Jianmei Fan, Susan Jenkins, Harold C.E. Kluender, Anish Konkar, Rico Lavoie, Ronald Mays, Jennifer Natoli, Stephen J. O’Connor, Astrid A. Ortiz, Ning Su, Christy Taing, Susan Tomlinson, Theresa Tritto, Gan Wang, Stephan-Nicholas Wirtz, Wai Wong, Xiao-Fan Yang, Shihong Ying & Zhonghua Zhang. (2007) Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity. Bioorganic & Medicinal Chemistry Letters 17:10, pages 2706-2711.
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Roger A. Smith, Zahra Fathi, Su-Ellen Brown, Soongyu Choi, Jianmei Fan, Susan Jenkins, Harold C.E. Kluender, Anish Konkar, Rico Lavoie, Ronald Mays, Jennifer Natoli, Stephen J. O’Connor, Astrid A. Ortiz, Brent Podlogar, Christy Taing, Susan Tomlinson, Theresa Tritto & Zhonghua Zhang. (2007) Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives. Bioorganic & Medicinal Chemistry Letters 17:3, pages 673-678.
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