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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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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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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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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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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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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Discovery of TRPV1 antagonist ABT-116
Brown, Brian S, Keddy, Ryan, Perner, Richard J, DiDomenico, Stanley, Koenig, John R, Jinkerson, Tammie K, Hannick, Steven M, McDonald, Heath A, Bianchi, Bruce R, Honore, Prisca, Puttfarcken, Pamela S, Moreland, Robert B, Marsh, Kennan C, Faltynek, Connie R, Lee, Chih-Hung
Published in Bioorganic & medicinal chemistry letters (01.06.2010)
Published in Bioorganic & medicinal chemistry letters (01.06.2010)
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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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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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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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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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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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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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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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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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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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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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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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Discovery of 4-Amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin- 3-yl)pyrido[2,3-d]pyrimidine, an Orally Active, Non-Nucleoside Adenosine Kinase Inhibitor
Lee, Chih-Hung, Jiang, Meiqun, Cowart, Marlon, Gfesser, Greg, Perner, Richard, Kim, Ki Hwan, Gu, Yu Gui, Williams, Michael, Jarvis, Michael F, Kowaluk, Elizabeth A, Stewart, Andrew O, Bhagwat, Shripad S
Published in Journal of medicinal chemistry (21.06.2001)
Published in Journal of medicinal chemistry (21.06.2001)
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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)
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