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Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 – 2014)

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Mengkang Gao, Yusui Wang, Lanqi Liu, Zhenrui Qiao & Lin Yan. (2021) A patent review of transient receptor potential vanilloid type 1 modulators (2014–present). Expert Opinion on Therapeutic Patents 31:2, pages 169-187.
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Tom Rouwette, Luca Avenali, Julia Sondermann, Pratibha Narayanan, David Gomez-Varela & Manuela Schmidt. (2015) Modulation of nociceptive ion channels and receptors via protein-protein interactions: implications for pain relief. Channels 9:4, pages 175-185.
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Chunxia Liu, Ruoyang Miao, Faisal Raza, Hai Qian & Xin Tian. (2023) Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain. European Journal of Medicinal Chemistry 245, pages 114893.
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Liying Dong, Qiqi Zhou, Qianqian Liang, Zhen Qiao, Yani Liu, Liming Shao & Kewei Wang. (2022) Identification of a Partial and Selective TRPV1 Agonist CPIPC for Alleviation of Inflammatory Pain. Molecules 27:17, pages 5428.
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Mircea Iftinca, Manon Defaye & Christophe Altier. (2020) TRPV1-Targeted Drugs in Development for Human Pain Conditions. Drugs 81:1, pages 7-27.
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Jin Mi Kang, Sun Ok Kwon, Jihyae Ann, Peter M. Blumberg, Heejin Ha, Young Dong Yoo, Robert Frank-Foltyn, Bernhard Lesch, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2020) Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 30:23, pages 127548.
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Da-Som Choi, Yeounjung Ji, Yongwoo Jang, Wook-Joo Lee & Won-Sik Shim. (2020) Crotamiton, an Anti-Scabies Agent, Suppresses Histamine- and Chloroquine-Induced Itch Pathways in Sensory Neurons and Alleviates Scratching in Mice. Biomolecules & Therapeutics 28:6, pages 569-575.
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John H Van Drie & Liang Tong. (2020) Cryo-EM as a powerful tool for drug discovery. Bioorganic & Medicinal Chemistry Letters 30:22, pages 127524.
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Ádám Horváth, Tünde Biró-Sütő, Boglárka Kántás, Maja Payrits, Rita Skoda-Földes, Eszter Szánti-Pintér, Zsuzsanna Helyes & Éva Szőke. (2020) Antinociceptive Effects of Lipid Raft Disruptors, a Novel Carboxamido-Steroid and Methyl β-Cyclodextrin, in Mice by Inhibiting Transient Receptor Potential Vanilloid 1 and Ankyrin 1 Channel Activation. Frontiers in Physiology 11.
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Félix Viana & Thomas Voets. 2020. The Oxford Handbook of the Neurobiology of Pain. The Oxford Handbook of the Neurobiology of Pain 179 199 .
Cunbin Nie, Qifei Li, Yue Qiao, Jing Hu, Mengkang Gao, Yusui Wang, Zhenrui Qiao, Qiang Wang, Lin Yan & Hai Qian. (2020) Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. European Journal of Medicinal Chemistry 194, pages 112236.
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Andras Garami, Yury P. Shimansky, Zoltan Rumbus, Robson C.L. Vizin, Nelli Farkas, Judit Hegyi, Zsolt Szakacs, Margit Solymar, Alexandra Csenkey, Dan A. Chiche, Ram Kapil, Donald J. Kyle, Wade D. Van Horn, Peter Hegyi & Andrej A. Romanovsky. (2020) Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: Insights from mathematical modeling and meta-analysis. Pharmacology & Therapeutics 208, pages 107474.
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Songyeon Ahn, Yong Soo Kim, Myeong Seup Kim, Jihyae Ann, Heejin Ha, Young Dong Yoo, Young Ho Kim, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2020) Discovery of indane propanamides as potent and selective TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 30:3, pages 126838.
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Elizete Maria Rita Pereira, Jéssica Mabelle Souza, Natália Virtude Carobin, Juliana Figueira Silva, Duana Carvalho Santos, Cláudio Antonio Silva Júnior, Nancy Scardua Binda, Márcia Helena Borges, Ronaldo Alves Pinto Nagem, Christopher Kushmerick, Juliano Ferreira, Célio Jose Castro Junior, Fabíola Mara Ribeiro & Marcus Vinicius Gomez. (2020) Phoneutria toxin PnTx3-5 inhibits TRPV1 channel with antinociceptive action in an orofacial pain model. Neuropharmacology 162, pages 107826.
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Alessandro Alaimo & Josep Rubert. (2019) The Pivotal Role of TRP Channels in Homeostasis and Diseases throughout the Gastrointestinal Tract. International Journal of Molecular Sciences 20:21, pages 5277.
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Larry V. Pearce, Jihyae Ann, Peter M. Blumberg & Jeewoo Lee. (2019) Combination of a Rapidly Penetrating Agonist and a Slowly Penetrating Antagonist Affords Agonist Action of Limited Duration at the Cellular Level. Biomolecules & Therapeutics 27:5, pages 435-441.
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Jinyu Li, Cunbin Nie, Yue Qiao, Jing Hu, Qifei Li, Qiang Wang, Xiaohui Pu, Lin Yan & Hai Qian. (2019) Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. European Journal of Medicinal Chemistry 178, pages 433-445.
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Dorte X. Gram, Josefine Fribo, Istvan Nagy, Carsten Gotfredsen, Ana Charrua, John B. Hansen, Anker J. Hansen & Arpad Szallasi. (2019) TRPV1 Antagonists as Novel Anti-Diabetic Agents: Regulation of Oral Glucose Tolerance and Insulin Secretion Through Reduction of Low-Grade Inflammation?. Medical Sciences 7:8, pages 82.
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Bo Xie & Xin-Yu Li. (2019) Inflammatory mediators causing cutaneous chronic itch in some diseases via transient receptor potential channel subfamily V member 1 and subfamily A member 1. The Journal of Dermatology 46:3, pages 177-185.
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Asier Carral-Menoyo, Alexander Misol, Marcos Gómez-Redondo, Nuria Sotomayor & Esther Lete. (2019) Palladium(II)-Catalyzed Intramolecular C–H Alkenylation for the Synthesis of Chromanes. The Journal of Organic Chemistry 84:4, pages 2048-2060.
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Alexander Dietrich. (2019) Modulators of Transient Receptor Potential (TRP) Channels as Therapeutic Options in Lung Disease. Pharmaceuticals 12:1, pages 23.
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Mingxiang Gao, Cunbin Nie, Jinyu Li, Beibei Song, Xinru Cheng, Erying Sun, Lin Yan & Hai Qian. (2019) Design, synthesis and biological evaluation of N1-(isoquinolin-5-yl)-N2-phenylpyrrolidine-1,2-dicarboxamide derivatives as potent TRPV1 antagonists. Bioorganic Chemistry 82, pages 100-108.
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Angelika Andrzejewska, Klaudia Staszak, Marta Kaczmarek-Ryś, Ryszard Słomski & Szymon Hryhorowicz. (2018) Understanding cannabinoid receptors: structure and function. Acta Universitatis Lodziensis. Folia Biologica et Oecologica 14, pages 1-13.
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Pierre Arsenault, Dan Chiche, William Brown, Jeffrey Miller, Roi Treister, Richard Leff, Philippe Walker & Nathaniel Katz. (2018) NEO6860, modality-selective TRPV1 antagonist: a randomized, controlled, proof-of-concept trial in patients with osteoarthritis knee pain. PAIN Reports 3:6, pages e696.
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Éva Sághy, Maja Payrits, Tünde Bíró-Sütő, Rita Skoda-Földes, Eszter Szánti-Pintér, János Erostyák, Géza Makkai, György SétálóJr.Jr., László Kollár, Tamás Kőszegi, Rita Csepregi, János Szolcsányi, Zsuzsanna Helyes & Éva Szőke. (2018) Carboxamido steroids inhibit the opening properties of transient receptor potential ion channels by lipid raft modulation. Journal of Lipid Research 59:10, pages 1851-1863.
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Changhoon Kim, Jihyae Ann, Sunho Lee, Eunhye Kim, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2018) 4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands. Bioorganic & Medicinal Chemistry 26:15, pages 4509-4517.
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A. Garami, E. Pakai, H. A. McDonald, R. M. Reilly, A. Gomtsyan, J. J. Corrigan, E. Pinter, D. X. D. Zhu, S. G. Lehto, N. R. Gavva, P. R. Kym & A. A. Romanovsky. (2018) TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds’ pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development. Acta Physiologica 223:3, pages e13038.
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Xiaona Du, Haixia Gao, David Jaffe, Hailin Zhang & Nikita Gamper. (2018) M-type K + channels in peripheral nociceptive pathways . British Journal of Pharmacology 175:12, pages 2158-2172.
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Seol Rin Park, Juhyun Kim, Sun Young Lee, Young-Ho Park & Hee-Doo Kim. (2018) 2-Methylacrylamide as a bioisoster of thiourea group for 1,3-dibenzylthioureido TRPV1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 28:11, pages 2080-2083.
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