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Fangjie Jin, Yuting Wen, Guoqiang Lin, Shaopeng Yu, Chao Wang, Wenbo Ye & Jiange Zhang. (2023) Design, synthesis, and analgesia evaluation of novel Transient Receptor Potential Vanilloid 1 (TRPV1) agonists modified from Cannabidiol (CBD). Bioorganic & Medicinal Chemistry 90, pages 117379.
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Kalliopi Stasi, Qusai Alshare, Monish Jain, Michael Wald & Yifang Li. (2022) Topical Ocular TRPV1 Antagonist SAF312 (Libvatrep) Demonstrates Safety, Low Systemic Exposure, and No Anesthetic Effect in Healthy Participants. Translational Vision Science & Technology 11:11, pages 15.
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Jin Mi Kang, Sun Ok Kwon, Jihyae Ann, Sunho Lee, Changhoon Kim, Nayeon Do, Jin Ju Jeong, Peter M. Blumberg, Heejin Ha, Thi Ngoc Lan Vu, Sanghee Yoon, Sun Choi, Robert Frank-Foltyn, Bernhard Lesch, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2021) 2-(Halogenated Phenyl) acetamides and propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 48, pages 128266.
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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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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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Changhoon Kim, Jihyae Ann, Sunho Lee, Wei Sun, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2018) Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 28:14, pages 2539-2542.
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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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M. S. Komarova, N. N. Potapieva & M. V. Nikolaev. (2018) Non-Competitive but pH-Dependent Action of SB-366791 on Proton-Induced Activation of TRPV1 Receptors. Biochemistry (Moscow), Supplement Series A: Membrane and Cell Biology 12:2, pages 107-113.
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Yan Li, Robert Y. North, Laurence D. Rhines, Claudio Esteves Tatsui, Ganesh Rao, Denaya D. Edwards, Ryan M. Cassidy, Daniel S. Harrison, Caj A. Johansson, Hongmei Zhang & Patrick M. Dougherty. (2018) DRG Voltage-Gated Sodium Channel 1.7 Is Upregulated in Paclitaxel-Induced Neuropathy in Rats and in Humans with Neuropathic Pain. The Journal of Neuroscience 38:5, pages 1124-1136.
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Katsushi Kumata, Joji Yui, Yiding Zhang, Yusuke Kurihara, Masanao Ogawa, Wakana Mori, Masayuki Fujinaga & Ming-Rong Zhang. (2017) [ 11 C]BCTC: Radiosynthesis and in vivo binding to transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in the mouse trigeminal nerve. Bioorganic & Medicinal Chemistry Letters 27:19, pages 4521-4524.
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Sunho Lee, Changhoon Kim, Jihyae Ann, Shivaji A. Thorat, Eunhye Kim, Jongmi Park, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2017) Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 27:18, pages 4383-4388.
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Maxim V. Nikolaev, Natalia A. Dorofeeva, Margarita S. Komarova, Yuliya V. Korolkova, Yaroslav A. Andreev, Irina V. Mosharova, Eugene V. Grishin, Denis B. Tikhonov & Sergey A. Kozlov. (2017) TRPV1 activation power can switch an action mode for its polypeptide ligands. PLOS ONE 12:5, pages e0177077.
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Sunho Lee, Dong Wook Kang, HyungChul Ryu, Changhoon Kim, Jihyae Ann, Hobin Lee, Eunhye Kim, Sunhye Hong, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2017) t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry 25:8, pages 2451-2462.
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Rajendra Kristam, Shashidhar N. Rao, Anne Sudha D’Cruz, Vijayalakshmi Mahadevan & Vellarkad N. Viswanadhan. (2017) TRPV1 antagonism by piperazinyl-aryl compounds: A Topomer-CoMFA study and its use in virtual screening for identification of novel antagonists. Journal of Molecular Graphics and Modelling 72, pages 112-128.
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Fan Yang & Jie Zheng. (2017) Understand spiciness: mechanism of TRPV1 channel activation by capsaicin. Protein & Cell 8:3, pages 169-177.
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Jihyae Ann, Wei Sun, Xing Zhou, Aeran Jung, Jisoo Baek, Sunho Lee, Changhoon Kim, Suyoung Yoon, Sunhye Hong, Sun Choi, Noe A. Turcios, Brienna K.A. Herold, Timothy E. Esch, Nancy E. Lewin, Adelle Abramovitz, Larry V. Pearce, Peter M. Blumberg & Jeewoo Lee. (2016) Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template. Bioorganic & Medicinal Chemistry Letters 26:15, pages 3603-3607.
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Jihyae Ann, Yooran Ki, Suyoung Yoon, Myeong Seop Kim, Jung-Un Lee, Changhoon Kim, Sunho Lee, Aeran Jung, Jisoo Baek, Sunhye Hong, Sun Choi, Larry V. Pearce, Timothy E. Esch, Noe A. Turcios, Nancy E. Lewin, Adebowale E. Ogunjirin, Brienna K.A. Herold, Anna K. McCall, Peter M. Blumberg & Jeewoo Lee. (2016) 2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry 24:6, pages 1231-1240.
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Jihyae Ann, Aeran Jung, Mi-Yeon Kim, Hyuk-Min Kim, HyungChul Ryu, Sunjoo Kim, Dong Wook Kang, Sunhye Hong, Minghua Cui, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2015) Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry 23:21, pages 6844-6854.
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Phuong-Thao Tran, Ho Shin Kim, Jihyae Ann, Sung-Eun Kim, Changhoon Kim, Mannkyu Hong, Van-Hai Hoang, Van T.H. Ngo, Sunhye Hong, Minghua Cui, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph & Jeewoo Lee. (2015) α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 25:11, pages 2326-2330.
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HyungChul Ryu, Sejin Seo, Jee-Young Lee, Tae-Hwan Ha, Sunho Lee, Aeran Jung, Jihyae Ann, Sung-Eun Kim, Suyoung Yoon, Mannkyu Hong, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Klaus Schiene, Hannelore Stockhausen, Thomas Christoph, Sven Frormann & Jeewoo Lee. (2015) Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists. European Journal of Medicinal Chemistry 93, pages 101-108.
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Wei Sun, Hyo-Shin Kim, Sunho Lee, Aeran Jung, Sung-Eun Kim, Jihyae Ann, Suyoung Yoon, Sun Choi, Jin Hee Lee, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Klaus Schiene, Hannelore Stockhausen, Thomas Christoph, Sven Frormann & Jeewoo Lee. (2015) 6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 25:4, pages 803-806.
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HyungChul Ryu, Sejin Seo, Seong-Hee Cho, Ho Shin Kim, Aeran Jung, Dong Wook Kang, Karam Son, Minghua Cui, Sun-hye Hong, Pankaz Kumar Sharma, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Hannelore Stockhausen, Klaus Schiene, Thomas Christoph, Sven Frormann & Jeewoo Lee. (2014) 2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 24:16, pages 4039-4043.
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HyungChul Ryu, Sejin Seo, Myeong Seop Kim, Mi-Yeon Kim, Ho Shin Kim, Jihyae Ann, Phuong-Thao Tran, Van-Hai Hoang, Jieun Byun, Minghua Cui, Karam Son, Pankaz Kumar Sharma, Sun Choi, Peter M. Blumberg, Robert Frank-Foltyn, Gregor Bahrenberg, Babette-Yvonne Koegel, Thomas Christoph, Sven Frormann & Jeewoo Lee. (2014) 2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 24:16, pages 4044-4047.
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Bernd Nilius & Arpad Szallasi. (2014) Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine. Pharmacological Reviews 66:3, pages 676-814.
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Ho Shin Kim, Mi-Kyoung Jin, Sang-Uk Kang, Ju-Ok Lim, Phuong-Thao Tran, Van-Hai Hoang, Jihyae Ann, Tae-Hwan Ha, Larry V. Pearce, Vladimir A. Pavlyukovets, Peter M. Blumberg & Jeewoo Lee. (2014) α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters 24:12, pages 2685-2688.
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Tae-Hwan Ha, HyungChul Ryu, Sung-Eun Kim, Ho Shin Kim, Jihyae Ann, Phuong-Thao Tran, Van-Hai Hoang, Karam Son, Minghua Cui, Sun Choi, Peter M. Blumberg, Robert Frank, Gregor Bahrenberg, Klaus Schiene, Thomas Christoph, Sven Frormann & Jeewoo Lee. (2013) TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides. Bioorganic & Medicinal Chemistry 21:21, pages 6657-6664.
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Carlene Moore, Ferda CevikbasH. Amalia Pasolli, Yong Chen, Wei KongCordula KempkesPuja Parekh, Suk Hee Lee, Nelly-Ange Kontchou, Iwei YehNan Marie JokerstElaine Fuchs, Martin SteinhoffWolfgang B. Liedtke. (2013) UVB radiation generates sunburn pain and affects skin by activating epidermal TRPV4 ion channels and triggering endothelin-1 signaling. Proceedings of the National Academy of Sciences 110:34.
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Shivaji A. Thorat, Dong Wook Kang, HyungChul Ryu, Myeong Seop Kim, Ho Shin Kim, Jihyae Ann, Taehwan Ha, Sung-Eun Kim, Karam Son, Sun Choi, Peter M. Blumberg, Robert Frank, Gregor Bahrenberg, Klaus Schiene, Thomas Christoph & Jeewoo Lee. (2013) 2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists: Structure activity relationships of the 2-oxy pyridine C-region. European Journal of Medicinal Chemistry 64, pages 589-602.
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Ismet Dorange, Rickard Forsblom, Istvan Macsari, Mats Svensson, Johan Bylund, Yevgeni Besidski, Jan Blid, Daniel Sohn & Ylva Gravenfors. (2012) Discovery of novel pyrrolopyridazine scaffolds as transient receptor potential vanilloid (TRPV1) antagonists. Bioorganic & Medicinal Chemistry Letters 22:22, pages 6888-6895.
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