Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation
Chen, Jun, Joshi, Shailen K., DiDomenico, Stanley, Perner, Richard J., Mikusa, Joe P., Gauvin, Donna M., Segreti, Jason A., Han, Ping, Zhang, Xu-Feng, Niforatos, Wende, Bianchi, Bruce R., Baker, Scott J., Zhong, Chengmin, Simler, Gricelda H., McDonald, Heath A., Schmidt, Robert G., McGaraughty, Steve P., Chu, Katharine L., Faltynek, Connie R., Kort, Michael E., Reilly, Regina M., Kym, Philip R.
Published in Pain (Amsterdam) (01.05.2011)
Published in Pain (Amsterdam) (01.05.2011)
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Journal Article
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists
Perner, Richard J., Koenig, John R., DiDomenico, Stanley, Gomtsyan, Arthur, Schmidt, Robert G., Lee, Chih-Hung, Hsu, Margaret C., McDonald, Heath A., Gauvin, Donna M., Joshi, Shailen, Turner, Teresa M., Reilly, Regina M., Kym, Philip R., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (01.07.2010)
Published in Bioorganic & medicinal chemistry (01.07.2010)
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Journal Article
A-425619 [1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a Novel and Selective Transient Receptor Potential Type V1 Receptor Antagonist, Blocks Channel Activation by Vanilloids, Heat, and Acid
El Kouhen, Rachid, Surowy, Carol S, Bianchi, Bruce R, Neelands, Torben R, McDonald, Heath A, Niforatos, Wende, Gomtsyan, Arthur, Lee, Chih-Hung, Honore, Prisca, Sullivan, James P, Jarvis, Michael F, Faltynek, Connie R
Published in The Journal of pharmacology and experimental therapeutics (01.07.2005)
Published in The Journal of pharmacology and experimental therapeutics (01.07.2005)
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Journal Article
TRPV1b overexpression negatively regulates TRPV1 responsiveness to capsaicin, heat and low pH in HEK293 cells
Vos, Melissa H., Neelands, Torben R., McDonald, Heath A., Choi, Won, Kroeger, Paul E., Puttfarcken, Pamela S., Faltynek, Connie R., Moreland, Robert B., Han, Ping
Published in Journal of neurochemistry (01.11.2006)
Published in Journal of neurochemistry (01.11.2006)
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Journal Article
(R)-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) Blocks Polymodal Activation of Transient Receptor Potential Vanilloid 1 Receptors in Vitro and Heat-Evoked Firing of Spinal Dorsal Horn Neurons in Vivo
Surowy, Carol S, Neelands, Torben R, Bianchi, Bruce R, McGaraughty, Steve, El Kouhen, Rachid, Han, Ping, Chu, Katharine L, McDonald, Heath A, Vos, Melissa, Niforatos, Wende, Bayburt, Erol K, Gomtsyan, Arthur, Lee, Chih-Hung, Honore, Prisca, Sullivan, James P, Jarvis, Michael F, Faltynek, Connie R
Published in The Journal of pharmacology and experimental therapeutics (01.09.2008)
Published in The Journal of pharmacology and experimental therapeutics (01.09.2008)
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Journal Article
Characterization of A-425619 at native TRPV1 receptors: A comparison between dorsal root ganglia and trigeminal ganglia
McDonald, Heath A., Neelands, Torben R., Kort, Michael, Han, Ping, Vos, Melissa H., Faltynek, Connie R., Moreland, Robert B., Puttfarcken, Pamela S.
Published in European journal of pharmacology (31.10.2008)
Published in European journal of pharmacology (31.10.2008)
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Journal Article
Small Molecule IL-36γ Antagonist as a Novel Therapeutic Approach for Plaque Psoriasis
Todorović, Viktor, Su, Zhi, Putman, C. Brent, Kakavas, Stevan J., Salte, Katherine M., McDonald, Heath A., Wetter, Joseph B., Paulsboe, Stephanie E., Sun, Qi, Gerstein, Clare E., Medina, Limary, Sielaff, Bernhard, Sadhukhan, Ramkrishna, Stockmann, Henning, Richardson, Paul L., Qiu, Wei, Argiriadi, Maria A., Henry, Rodger F., Herold, J. Martin, Shotwell, J. Brad, McGaraughty, Steve P., Honore, Prisca, Gopalakrishnan, Sujatha M., Sun, Chaohong C., Scott, Victoria E.
Published in Scientific reports (24.06.2019)
Published in Scientific reports (24.06.2019)
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Journal Article
Cytokine induced 3‐D organotypic psoriasis skin model demonstrates distinct roles for NF‐κB and JAK pathways in disease pathophysiology
Todorović, Viktor, McDonald, Heath A., Hoover, Paul, Wetter, Joseph B., Marinopoulos, Anastasia E., Woody, Clarissa L., Miller, Loan, Finkielsztein, Ariel, Dunstan, Robert W., Paller, Amy S., Honore, Prisca, Getsios, Spiro, Scott, Victoria E.
Published in Experimental dermatology (01.07.2022)
Published in Experimental dermatology (01.07.2022)
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Journal Article
[3H]A-778317 [1-((R)-5-tert-Butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a Novel, Stereoselective, High-Affinity Antagonist Is a Useful Radioligand for the Human Transient Receptor Potential Vanilloid-1 (TRPV1) Receptor
Bianchi, Bruce R, El Kouhen, Rachid, Neelands, Torben R, Lee, Chih-Hung, Gomtsyan, Arthur, Raja, Shirish N, Vaidyanathan, Sriajan N, Surber, Bruce, McDonald, Heath A, Surowy, Carol S, Faltynek, Connie R, Moreland, Robert B, Jarvis, Michael F, Puttfarcken, Pamela S
Published in The Journal of pharmacology and experimental therapeutics (01.10.2007)
Published in The Journal of pharmacology and experimental therapeutics (01.10.2007)
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Journal Article
Small Molecule and Pooled CRISPR Screens Investigating IL17 Signaling Identify BRD2 as a Novel Contributor to Keratinocyte Inflammatory Responses
Slivka, Peter F, Hsieh, Chen-Lin, Lipovsky, Alex, Pratt, Steven D, Locklear, John, Namovic, Marian T, McDonald, Heath A, Wetter, Joseph, Edelmayer, Rebecca, Hu, Min, Murphy, Erin, Domanus, Marc, Lu, Charles, Duggan, Ryan, King, Jacob, Scott, Victoria E, Donnelly-Roberts, Diana, Slavin, Anthony, Gopalakrishnan, Sujatha, Chung, Namjin, Goedken, Eric R
Published in ACS chemical biology (17.05.2019)
Published in ACS chemical biology (17.05.2019)
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Journal Article
Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature
Reilly, Regina M, McDonald, Heath A, Puttfarcken, Pamela S, Joshi, Shailen K, Lewis, LaGeisha, Pai, Madhavi, Franklin, Pamela H, Segreti, Jason A, Neelands, Torben R, Han, Ping, Chen, Jun, Mantyh, Patrick W, Ghilardi, Joseph R, Turner, Teresa M, Voight, Eric A, Daanen, Jerome F, Schmidt, Robert G, Gomtsyan, Arthur, Kort, Michael E, Faltynek, Connie R, Kym, Philip R
Published in The Journal of pharmacology and experimental therapeutics (01.08.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.08.2012)
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Journal Article
Discovery of (R)‑1-(7-Chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): A Temperature-Neutral Transient Receptor Potential Vanilloid‑1 (TRPV1) Antagonist with Analgesic Efficacy
Voight, Eric A, Gomtsyan, Arthur R, Daanen, Jerome F, Perner, Richard J, Schmidt, Robert G, Bayburt, Erol K, DiDomenico, Stanley, McDonald, Heath A, Puttfarcken, Pamela S, Chen, Jun, Neelands, Torben R, Bianchi, Bruce R, Han, Ping, Reilly, Regina M, Franklin, Pamela H, Segreti, Jason A, Nelson, Richard A, Su, Zhi, King, Andrew J, Polakowski, James S, Baker, Scott J, Gauvin, Donna M, Lewis, LaGeisha R, Mikusa, Joseph P, Joshi, Shailen K, Faltynek, Connie R, Kym, Philip R, Kort, Michael E
Published in Journal of medicinal chemistry (11.09.2014)
Published in Journal of medicinal chemistry (11.09.2014)
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Journal Article
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists
Gomtsyan, Arthur, Schmidt, Robert G, Bayburt, Erol K, Gfesser, Gregory A, Voight, Eric A, Daanen, Jerome F, Schmidt, Diana L, Cowart, Marlon D, Liu, Huaqing, Altenbach, Robert J, Kort, Michael E, Clapham, Bruce, Cox, Phil B, Shrestha, Anurupa, Henry, Rodger, Whittern, David N, Reilly, Regina M, Puttfarcken, Pamela S, Brederson, Jill-Desiree, Song, Ping, Li, Bin, Huang, Susan M, McDonald, Heath A, Neelands, Torben R, McGaraughty, Steve P, Gauvin, Donna M, Joshi, Shailen K, Banfor, Patricia N, Segreti, Jason A, Shebley, Mohamad, Faltynek, Connie R, Dart, Michael J, Kym, Philip R
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Journal Article
Identification of (R)-1-(5-tert-Butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a Potent TRPV1 Antagonist for Pain Management
Gomtsyan, Arthur, Bayburt, Erol K, Schmidt, Robert G, Surowy, Carol S, Honore, Prisca, Marsh, Kennan C, Hannick, Steven M, McDonald, Heath A, Wetter, Jill M, Sullivan, James P, Jarvis, Michael F, Faltynek, Connie R, Lee, Chih-Hung
Published in Journal of medicinal chemistry (14.02.2008)
Published in Journal of medicinal chemistry (14.02.2008)
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Journal Article
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists
Schmidt, Robert G., Bayburt, Erol K., Latshaw, Steven P., Koenig, John R., Daanen, Jerome F., McDonald, Heath A., Bianchi, Bruce R., Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Marsh, Kennan C., Lee, Chih-Hung, Faltynek, Connie R., Gomtsyan, Arthur
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
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Journal Article
Endogenous opioid mechanisms partially mediate P2X 3 /P2X 2/3 ‐related antinociception in rat models of inflammatory and chemogenic pain but not neuropathic pain
McGaraughty, Steve, Honore, Prisca, Wismer, Carol T, Mikusa, Joseph, Zhu, Chang Z, McDonald, Heath A, Bianchi, Bruce, Faltynek, Connie R, Jarvis, Michael F
Published in British journal of pharmacology (30.01.2009)
Published in British journal of pharmacology (30.01.2009)
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Journal Article
Novel Transient Receptor Potential Vanilloid 1 Receptor Antagonists for the Treatment of Pain: Structure−Activity Relationships for Ureas with Quinoline, Isoquinoline, Quinazoline, Phthalazine, Quinoxaline, and Cinnoline Moieties
Gomtsyan, Arthur, Bayburt, Erol K, Schmidt, Robert G, Zheng, Guo Zhu, Perner, Richard J, Didomenico, Stanley, Koenig, John R, Turner, Sean, Jinkerson, Tammie, Drizin, Irene, Hannick, Steven M, Macri, Bryan S, McDonald, Heath A, Honore, Prisca, Wismer, Carol T, Marsh, Kennan C, Wetter, Jill, Stewart, Kent D, Oie, Tetsuro, Jarvis, Michael F, Surowy, Carol S, Faltynek, Connie R, Lee, Chih-Hung
Published in Journal of medicinal chemistry (10.02.2005)
Published in Journal of medicinal chemistry (10.02.2005)
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Journal Article
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists
Brown, Brian S., Keddy, Ryan, Zheng, Guo Zhu, Schmidt, Robert G., Koenig, John R., McDonald, Heath A., Bianchi, Bruce R., Honore, Prisca, Jarvis, Michael F., Surowy, Carol S., Polakowski, James S., Marsh, Kennan C., Faltynek, Connie R., Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry (15.09.2008)
Published in Bioorganic & medicinal chemistry (15.09.2008)
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Journal Article
2′, 3′‐ O ‐(2,4,6,Trinitrophenyl)‐ATP and A‐317491 are competitive antagonists at a slowly desensitizing chimeric human P2X 3 receptor
Neelands, Torben R, Burgard, Edward C, Uchic, Marie E, McDonald, Heath A, Niforatos, Wende, Faltynek, Connie R, Lynch, Kevin J, Jarvis, Michael F
Published in British journal of pharmacology (30.01.2009)
Published in British journal of pharmacology (30.01.2009)
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Journal Article
TRPV1 ligands with hyperthermic, hypothermic and no temperature effects in rats
Gomtsyan, Arthur, McDonald, Heath A, Schmidt, Robert G, Daanen, Jerome F, Voight, Eric A, Segreti, Jason A, Puttfarcken, Pamela S, Reilly, Regina M, Kort, Michael E, Dart, Michael J, Kym, Philip R
Published in Temperature (Austin) (30.06.2015)
Published in Temperature (Austin) (30.06.2015)
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