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
TRPA1 Modulation of Spontaneous and Mechanically Evoked Firing of Spinal Neurons in Uninjured, Osteoarthritic, and Inflamed Rats
McGaraughty, Steve, Chu, Katharine L, Perner, Richard J, DiDomenico, Stan, Kort, Michael E, Kym, Philip R
Published in Molecular pain (05.03.2010)
Published in Molecular pain (05.03.2010)
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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
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
A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model
Puttfarcken, Pamela S., Han, Ping, Joshi, Shailen K., Neelands, Torben R., Gauvin, Donna M., Baker, Scott J., Lewis, La Geisha R., Bianchi, Bruce R., Mikusa, Joseph P., Koenig, John R., Perner, Richard J., Kort, Michael E., Honore, Prisca, Faltynek, Connie R., Kym, Philip R., Reilly, Regina M.
Published in Pain (Amsterdam) (01.08.2010)
Published in Pain (Amsterdam) (01.08.2010)
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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
α-Methylation at benzylic fragment of N-aryl- N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model
Gomtsyan, Arthur, Bayburt, Erol K., Keddy, Ryan, Turner, Sean C., Jinkerson, Tammie K., Didomenico, Stanley, Perner, Richard J., Koenig, John R., Drizin, Irene, McDonald, Heath A., Surowy, Carol S., Honore, Prisca, Mikusa, Joe, Marsh, Kennan C., Wetter, Jill M., Faltynek, Connie R., Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
Published in Bioorganic & medicinal chemistry letters (15.07.2007)
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Journal Article
An automated electrophysiological assay for differentiating Ca(v)2.2 inhibitors based on state dependence and kinetics
Swensen, Andrew M, Niforatos, Wende, Vortherms, Timothy A, Perner, Richard J, Li, Tao, Schrimpf, Michael R, Scott, Victoria E, Lee, Lance, Jarvis, Michael F, McGaraughty, Steve
Published in Assay and drug development technologies (01.12.2012)
Published in Assay and drug development technologies (01.12.2012)
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Journal Article
In Vitro Structure−Activity Relationship and In Vivo Characterization of 1-(Aryl)-3-(4-(amino)benzyl)urea Transient Receptor Potential Vanilloid 1 Antagonists
Perner, Richard J, DiDomenico, Stanley, Koenig, John R, Gomtsyan, Arthur, Bayburt, Erol K, Schmidt, Robert G, Drizin, Irene, Zheng, Guo Zhu, Turner, Sean C, Jinkerson, Tammie, Brown, Brian S, Keddy, Ryan G, Lukin, Kurill, McDonald, Heath A, Honore, Prisca, Mikusa, Joe, Marsh, Kennan C, Wetter, Jill M, St. George, Karen, Jarvis, Michael F, Faltynek, Connie R, Lee, Chih-Hung
Published in Journal of medicinal chemistry (26.07.2007)
Published in Journal of medicinal chemistry (26.07.2007)
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Journal Article
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor
DeNinno, Michael P, Schoenleber, Robert, Perner, Richard J, Lijewski, Linda, Asin, Karen E, Britton, Donald R, MacKenzie, Robert, Kebabian, John W
Published in Journal of medicinal chemistry (01.08.1991)
Published in Journal of medicinal chemistry (01.08.1991)
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Journal Article
P2X receptor ligands and pain
Shieh, Char-Chang, Jarvis, Michael F, Lee, Chih-Hung, Perner, Richard J
Published in Expert opinion on therapeutic patents (01.08.2006)
Published in Expert opinion on therapeutic patents (01.08.2006)
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Journal Article
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3- d]pyrimidines as adenosine kinase inhibitors
Perner, Richard J., Lee, Chih-Hung, Jiang, Meiqun, Gu, Yu-Gui, DiDomenico, Stanley, Bayburt, Erol K., Alexander, Karen M., Kohlhaas, Kathy L., Jarvis, Michael F., Kowaluk, Elizabeth L., Bhagwat, Shripad S.
Published in Bioorganic & medicinal chemistry letters (02.06.2005)
Published in Bioorganic & medicinal chemistry letters (02.06.2005)
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Journal Article
Structure–activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists
Drizin, Irene, Gomtsyan, Arthur, Bayburt, Erol K., Schmidt, Robert G., Zheng, Guo Zhu, Perner, Richard J., DiDomenico, Stanley, Koenig, John R., Turner, Sean C., Jinkerson, Tammie K., Brown, Brian S., Keddy, Ryan G., McDonald, Heath A., Honore, Prisca, Wismer, Carol T., Marsh, Kennan C., Wetter, Jill M., Polakowski, James S., Segreti, Jason A., Jarvis, Michael F., Faltynek, Connie R., Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry (15.07.2006)
Published in Bioorganic & medicinal chemistry (15.07.2006)
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Journal Article
5,6,7-Trisubstituted 4-Aminopyrido[2,3-d]pyrimidines as Novel Inhibitors of Adenosine Kinase
Perner, Richard J, Gu, Yu-Gui, Lee, Chih-Hung, Bayburt, Erol K, McKie, Jeffery, Alexander, Karen M, Kohlhaas, Kathy L, Wismer, Carol T, Mikusa, Joe, Jarvis, Michael F, Kowaluk, Elizabeth A, Bhagwat, Shripad S
Published in Journal of medicinal chemistry (20.11.2003)
Published in Journal of medicinal chemistry (20.11.2003)
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Journal Article
Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
Zheng, Guo Zhu, Mao, Yue, Lee, Chih-Hung, Pratt, John K., Koenig, John R., Perner, Richard J., Cowart, Marlon D., Gfesser, Gregory A., McGaraughty, Steve, Chu, Katharine L., Zhu, Chang, Yu, Haixia, Kohlhaas, Kathy, Alexander, Karen M., Wismer, Carol T., Mikusa, Joseph, Jarvis, Michael F., Kowaluk, Elizabeth A., Stewart, Andrew O.
Published in Bioorganic & medicinal chemistry letters (15.09.2003)
Published in Bioorganic & medicinal chemistry letters (15.09.2003)
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Journal Article
Pyridopyrimidine analogues as novel adenosine kinase inhibitors
Zheng, Guo Zhu, Lee, Chih-Hung, Pratt, John K, Perner, Richard J, Jiang, Mei Qun, Gomtsyan, Arthur, Matulenko, Mark A, Mao, Yui, Koenig, John R, Kim, Ki H, Muchmore, Steve, Yu, Haixia, Kohlhaas, Kathy, Alexander, Karen M, McGaraughty, Steve, Chu, Katharine L, Wismer, Carol T, Mikusa, Joseph, Jarvis, Michael F, Marsh, Kennan, Kowaluk, Elizabeth A, Bhagwat, Shripad S, Stewart, Andrew O
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
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Journal Article
The enantioselective synthesis of the potent dopamine D1 agonist (1R,3S)-3-(1'-adamantyl)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyran (A77636)
DeNinno, Michael P, Perner, Richard J, Morton, Howard E, DiDomenico, Stanley
Published in Journal of organic chemistry (01.12.1992)
Published in Journal of organic chemistry (01.12.1992)
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Journal Article
α-Μethylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model
GOMTSYAN, Arthur, BAYBURT, Erol K, SUROWY, Carol S, HONORE, Prisca, MIKUSA, Joe, MARSH, Kennan C, WETTER, Jill M, FALTYNEK, Connie R, LEE, Chih-Hung, KEDDY, Ryan, TURNER, Sean C, JINKERSON, Tammie K, DIDOMENICO, Stanley, PERNER, Richard J, KOENIG, John R, DRIZIN, Irene, MCDONALD, Heath A
Published in Bioorganic & medicinal chemistry letters (2007)
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Published in Bioorganic & medicinal chemistry letters (2007)
Journal Article
Adenosine kinase inhibitors: Polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity: Recent advances in the design of kinase inhibitors as novel therapeutic agents
GUO ZHU ZHENG, YUE MAO, CHANG ZHU, HAIXIA YU, KOHLHAAS, Kathy, ALEXANDER, Karen M, WISMER, Carol T, MIKUSA, Joseph, JARVIS, Michael F, KOWALUK, Elizabeth A, STEWART, Andrew O, LEE, Chih-Hung, PRATT, John K, KOENIG, John R, PERNER, Richard J, COWART, Marlon D, GFESSER, Gregory A, MCGARAUGHTY, Steve, CHU, Katharine L
Published in Bioorganic & medicinal chemistry letters (2003)
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Published in Bioorganic & medicinal chemistry letters (2003)
Journal Article
TRPA1 antagonists
Chen Jun, Vasudevan Anil, Kort Michael E, DiDomenico Stanley, Perner Richard J
Year of Publication 05.09.2017
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Year of Publication 05.09.2017
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