A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat
Jarvis, Michael F, Honore, Prisca, Shieh, Char-Chang, Chapman, Mark, Joshi, Shailen, Zhang, Xu-Feng, Kort, Michael, Carroll, William, Marron, Brian, Atkinson, Robert, Thomas, James, Liu, Dong, Krambis, Michael, Liu, Yi, McGaraughty, Steve, Chu, Katharine, Roeloffs, Rosemarie, Zhong, Chengmin, Mikusa, Joseph P, Hernandez, Gricelda, Gauvin, Donna, Wade, Carrie, Zhu, Chang, Pai, Madhavi, Scanio, Marc, Shi, Lei, Drizin, Irene, Gregg, Robert, Matulenko, Mark, Hakeem, Ahmed, Gross, Michael, Johnson, Matthew, Marsh, Kennan, Wagoner, P. Kay, Sullivan, James P, Faltynek, Connie R, Krafte, Douglas S
Published in Proceedings of the National Academy of Sciences - PNAS (15.05.2007)
Published in Proceedings of the National Academy of Sciences - PNAS (15.05.2007)
Get full text
Journal Article
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain
Drizin, Irene, Gregg, Robert J., Scanio, Marc J.C., Shi, Lei, Gross, Michael F., Atkinson, Robert N., Thomas, James B., Johnson, Matthew S., Carroll, William A., Marron, Brian E., Chapman, Mark L., Liu, Dong, Krambis, Michael J., Shieh, Char-Chang, Zhang, XuFeng, Hernandez, Gricelda, Gauvin, Donna M., Mikusa, Joseph P., Zhu, Chang Z., Joshi, Shailen, Honore, Prisca, Marsh, Kennan C., Roeloffs, Rosemarie, Werness, Stephen, Krafte, Douglas S., Jarvis, Michael F., Faltynek, Connie R., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (15.06.2008)
Published in Bioorganic & medicinal chemistry (15.06.2008)
Get full text
Journal Article
Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H-4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models
Cowart, Marlon D., Altenbach, Robert J., Liu, Huaqing, Hsieh, Gin C., Drizin, Irene, Milicic, Ivan, Miller, Thomas R., Witte, David G., Wishart, Neil, Fix-Stenzel, Shannon R., McPherson, Michael J., Adair, Ronald M., Wetter, Jill M., Bettencourt, Brian M., Marsh, Kerman C., Sullivan, James P., Honore, Prisca, Esbenshade, Timothy A., Brioni, Jorge D.
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
Get full text
Journal Article
Structure−Activity Studies for a Novel Series of Tricyclic Substituted Hexahydrobenz[e]isoindole α1A Adrenoceptor Antagonists as Potential Agents for the Symptomatic Treatment of Benign Prostatic Hyperplasia (BPH)
Meyer, Michael D, Altenbach, Robert J, Basha, Fatima Z, Carroll, William A, Condon, Stephen, Elmore, Steven W, Kerwin, James F, Sippy, Kevin B, Tietje, Karin, Wendt, Michael D, Hancock, Arthur A, Brune, Michael E, Buckner, Steven A, Drizin, Irene
Published in Journal of medicinal chemistry (20.04.2000)
Published in Journal of medicinal chemistry (20.04.2000)
Get full text
Journal Article
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Na(v)1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain
Kort, Michael E., Drizin, Irene, Gregg, Robert J., Scanio, Marc J. C., Shi, Lei, Gross, Michael F., Atkinson, Robert N., Johnson, Matthew S., Pacofsky, Gregory J., Thomas, James B., Carroll, William A., Krambis, Michael J., Liu, Dong, Shieh, Char-Chang, Zhang, XuFeng, Hernandez, Gricelda, Mikusa, Joseph P., Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Roeloffs, Rosemarie, Marsh, Kennan C., Murray, Bernard P., Liu, Jinrong, Werness, Stephen, Faltynek, Connie R., Krafte, Douglas S., Jarvis, Michael F., Chapman, Mark L., Marron, Brian E.
Published in Journal of medicinal chemistry (14.02.2008)
Published in Journal of medicinal chemistry (14.02.2008)
Get full text
Journal Article
Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models
Cowart, Marlon D, Altenbach, Robert J, Liu, Huaqing, Hsieh, Gin C, Drizin, Irene, Milicic, Ivan, Miller, Thomas R, Witte, David G, Wishart, Neil, Fix-Stenzel, Shannon R, McPherson, Michael J, Adair, Ronald M, Wetter, Jill M, Bettencourt, Brian M, Marsh, Kennan C, Sullivan, James P, Honore, Prisca, Esbenshade, Timothy A, Brioni, Jorge D
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
Get full text
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)
Get full text
Journal Article
Discovery and Biological Evaluation of 5-Aryl-2-furfuramides, Potent and Selective Blockers of the Nav1.8 Sodium Channel with Efficacy in Models of Neuropathic and Inflammatory Pain
Kort, Michael E, Drizin, Irene, Gregg, Robert J, Scanio, Marc J. C, Shi, Lei, Gross, Michael F, Atkinson, Robert N, Johnson, Matthew S, Pacofsky, Gregory J, Thomas, James B, Carroll, William A, Krambis, Michael J, Liu, Dong, Shieh, Char-Chang, Zhang, XuFeng, Hernandez, Gricelda, Mikusa, Joseph P, Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Roeloffs, Rosemarie, Marsh, Kennan C, Murray, Bernard P, Liu, Jinrong, Werness, Stephen, Faltynek, Connie R, Krafte, Douglas S, Jarvis, Michael F, Chapman, Mark L, Marron, Brian E
Published in Journal of medicinal chemistry (14.02.2008)
Published in Journal of medicinal chemistry (14.02.2008)
Get full text
Journal Article
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain
Scanio, Marc J C, Shi, Lei, Drizin, Irene, Gregg, Robert J, Atkinson, Robert N, Thomas, James B, Johnson, Matthew S, Chapman, Mark L, Liu, Dong, Krambis, Michael J, Liu, Yi, Shieh, Char-Chang, Zhang, Xufeng, Simler, Gricelda H, Joshi, Shailen, Honore, Prisca, Marsh, Kennan C, Knox, Alison, Werness, Stephen, Antonio, Brett, Krafte, Douglas S, Jarvis, Michael F, Faltynek, Connie R, Marron, Brian E, Kort, Michael E
Published in Bioorganic & medicinal chemistry (15.11.2010)
Published in Bioorganic & medicinal chemistry (15.11.2010)
Get full text
Journal Article
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Nav1.8 sodium channel with efficacy in a model of neuropathic pain
SCANIO, Marc J. C, LEI SHI, YI LIU, SHIEH, Char-Chang, XUFENG ZHANG, SIMLER, Gricelda H, JOSHI, Shailen, HONORE, Prisca, MARSH, Kennan C, KNOX, Alison, WERNESS, Stephen, ANTONIO, Brett, DRIZIN, Irene, KRAFTE, Douglas S, JARVIS, Michael F, FALTYNEK, Connie R, MARRON, Brian E, KORT, Michael E, GREGG, Robert J, ATKINSON, Robert N, THOMAS, James B, JOHNSON, Matthew S, CHAPMAN, Mark L, DONG LIU, KRAMBIS, Michael J
Published in Bioorganic & medicinal chemistry (15.11.2010)
Published in Bioorganic & medicinal chemistry (15.11.2010)
Get full text
Journal Article
Rigidified 2-aminopyrimidines as histamine H 4 receptor antagonists: Effects of substitution about the rigidifying ring
Koenig, John R., Liu, Huaqing, Drizin, Irene, Witte, David G., Carr, Tracy L., Manelli, Arlene M., Milicic, Ivan, Strakhova, Marina I., Miller, Thomas R., Esbenshade, Timothy A., Brioni, Jorge D., Cowart, Marlon
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Get full text
Journal Article
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives
Kort, Michael E, Atkinson, Robert N, Thomas, James B, Drizin, Irene, Johnson, Matthew S, Secrest, Matthew A, Gregg, Robert J, Scanio, Marc J C, Shi, Lei, Hakeem, Ahmed H, Matulenko, Mark A, Chapman, Mark L, Krambis, Michael J, Liu, Dong, Shieh, Char-Chang, Zhang, XuFeng, Simler, Gricelda, Mikusa, Joseph P, Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Roeloffs, Rosemarie, Werness, Stephen, Antonio, Brett, Marsh, Kennan C, Faltynek, Connie R, Krafte, Douglas S, Jarvis, Michael F, Marron, Brian E
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Get full text
Journal Article
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: Effects of substitution about the rigidifying ring
KOENIG, John R, HUAQING LIU, BRIONI, Jorge D, COWART, Marlon, DRIZIN, Irene, WITTE, David G, CARR, Tracy L, MANELLI, Arlene M, MILICIC, Ivan, STRAKHOVA, Marina I, MILLER, Thomas R, ESBENSHADE, Timothy A
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Get full text
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)
Get full text
Journal Article
Rigidified 2-aminopyrimidines as histamine H sub(4) receptor antagonists: Effects of substitution about the rigidifying ring
Koenig, John R, Liu, Huaqing, Drizin, Irene, Witte, David G, Carr, Tracy L, Manelli, Arlene M, Milicic, Ivan, Strakhova, Marina I, Miller, Thomas R, Esbenshade, Timothy A, Brioni, Jorge D, Cowart, Marlon
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Get full text
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)
Get full text
Journal Article
Structure–Activity studies for a novel series of tricyclic dihydropyrimidines as K ATP channel openers (KCOs)
Drizin, Irene, Holladay, Mark W., Yi, Lin, Zhang, Henry Q., Gopalakrishnan, Sujatha, Gopalakrishnan, Murali, Whiteaker, Kristi L., Buckner, Steven A., Sullivan, James P., Carroll, William A.
Published in Bioorganic & medicinal chemistry letters (03.06.2002)
Published in Bioorganic & medicinal chemistry letters (03.06.2002)
Get full text
Journal Article
Structure-activity studies for a novel series of tricyclic dihydropyrimidines as KATP channel openers (KCOs)
DRIZIN, Irene, HOLLADAY, Mark W, LIN YI, ZHANG, Henry Q, GOPALAKRISHNAN, Sujatha, GOPALAKRISHNAN, Murali, WHITEAKER, Kristi L, BUCKNER, Steven A, SULLIVAN, James P, CARROLL, William A
Published in Bioorganic & medicinal chemistry letters (03.06.2002)
Published in Bioorganic & medicinal chemistry letters (03.06.2002)
Get full text
Journal Article
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na v1.8 sodium channel with efficacy in a model of neuropathic pain
Scanio, Marc J.C., Shi, Lei, Drizin, Irene, Gregg, Robert J., Atkinson, Robert N., Thomas, James B., Johnson, Matthew S., Chapman, Mark L., Liu, Dong, Krambis, Michael J., Liu, Yi, Shieh, Char-Chang, Zhang, XuFeng, Simler, Gricelda H., Joshi, Shailen, Honore, Prisca, Marsh, Kennan C., Knox, Alison, Werness, Stephen, Antonio, Brett, Krafte, Douglas S., Jarvis, Michael F., Faltynek, Connie R., Marron, Brian E., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (2010)
Published in Bioorganic & medicinal chemistry (2010)
Get full text
Journal Article
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K-ATP channel openers: Discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K-ATP opener that selectively inhibits spontaneous bladder contractions
Carroll, WA, Altenbach, RJ, Bai, H, Brioni, JD, Brune, ME, Buckner, SA, Cassidy, C, Chen, YY, Coghlan, MJ, Daza, AV, Drizin, Fey, TA, Fitzgerald, M, Gopalakrishnan, M, Gregg, RJ, Henry, RF, Holladay, MW, King, LL, Kort, ME, Kym, PR, Milicic, Tang, R, Turner, SC, Whiteaker, KL, Yi, L, Zhang, H, Sullivan, JP
Published in Journal of medicinal chemistry (03.06.2004)
Published in Journal of medicinal chemistry (03.06.2004)
Get full text
Journal Article