Search Results - "WETTER, Jill M"

Soy Protein Containing Diet Attenuates Murine Drug Exposure and Activity via Hepatic and Intestinal Cytochrome P450 Induction by Wetter, Jill M, Ciurlionis, Rita, Krause, Caitlin J, Liguori, Michael J, Goess, Christian, Mathieu, Suzanne, Kalvass, J Cory

“…Pharmacokinetic variability in drug plasma exposure between different studies within the same species is not unexpected due to a variety of factors (such as…”
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A-412997 is a selective dopamine D4 receptor agonist in rats by MORELAND, Robert B, PATEL, Meena, HSIEH, Gin C, WETTER, Jill M, MARSH, Kennan, BRIONI, Jorge D

“…A-412997 (2-(3',4',5',6'-tetrahydro-2'H-[2,4'] bipyridinyl-1'-yl)-N-m-tolyl-acetamide) is a highly selective dopamine D4 receptor agonist that binds with high…”
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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 by 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

“…A new structural class of histamine H4 receptor antagonists (6−14) was designed based on rotationally restricted 2,4-diaminopyrimidines. Series compounds…”
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H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats by HSIEH, Gin C, CHANDRAN, Prasant, WETTER, Jill M, MARSH, Kennan C, HANCOCK, Arthur A, COWART, Marlon D, ESBENSHADE, Timothy A, BRIONI, Jorge D, HONORE, Prisca, SALYERS, Anita K, PAI, Madhavi, ZHU, Chang Z, WENSINK, Erica J, WITTE, David G, MILLER, Thomas R, MIKUSA, Joe P, BAKER, Scott J

“…The histamine H(4) receptor (H(4)R) is expressed primarily on cells involved in inflammation and immune responses. To determine the potential role of H(4)R in…”
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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 by 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

“…Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1…”
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Structure−Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands by Altenbach, Robert J, Adair, Ronald M, Bettencourt, Brian M, Black, Lawrence A, Fix-Stenzel, Shannon R, Gopalakrishnan, Sujatha M, Hsieh, Gin C, Liu, Huaqing, Marsh, Kennan C, McPherson, Michael J, Milicic, Ivan, Miller, Thomas R, Vortherms, Timothy A, Warrior, Usha, Wetter, Jill M, Wishart, Neil, Witte, David G, Honore, Prisca, Esbenshade, Timothy A, Hancock, Arthur A, Brioni, Jorge D, Cowart, Marlon D

“…A series of 2-aminopyrimidines was synthesized as ligands of the histamine H4 receptor (H4R). Working in part from a pyrimidine hit that was identified in an…”
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Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems by Hsieh, Gin C, Honore, Prisca, Pai, Madhavi, Wensink, Erica J, Chandran, Prasant, Salyers, Anita K, Wetter, Jill M, Zhao, Chen, Liu, Huaqing, Decker, Michael W, Esbenshade, Timothy A, Cowart, Marlon D, Brioni, Jorge D

“…Abstract The histamine H3 receptor is predominantly expressed in the central nervous system and plays a role in diverse physiological mechanisms. In the…”
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cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia by Liu, Huaqing, Altenbach, Robert J, Carr, Tracy L, Chandran, Prasant, Hsieh, Gin C, Lewis, La Geisha R, Manelli, Arlene M, Milicic, Ivan, Marsh, Kennan C, Miller, Thomas R, Strakhova, Marina I, Vortherms, Timothy A, Wakefield, Brian D, Wetter, Jill M, Witte, David G, Honore, Prisca, Esbenshade, Timothy A, Brioni, Jorge D, Cowart, Marlon D

“…cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine, 4 (A-987306) is a new histamine H4 antagonist. The compound is potent…”
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Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain by Beebe, Xenia, Yeung, Clinton M., Darczak, Daria, Shekhar, Shashank, Vortherms, Timothy A., Miller, Loan, Milicic, Ivan, Swensen, Andrew M., Zhu, Chang Z., Banfor, Patricia, Wetter, Jill M., Marsh, Kennan C., Jarvis, Michael F., Scott, Victoria E., Schrimpf, Michael R., Lee, Chih-Hung

“…A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines…”
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Discovery of diphenyl lactam derivatives as N-type calcium channel blockers by Doherty, George A., Bhatia, Pramila, Vortherms, Timothy A., Marsh, Kennan C., Wetter, Jill M., Mack, Helmut, Scott, Victoria E., Jarvis, Michael F., Stewart, Andrew O.

“…A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and…”
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Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca2+ channel blockers with analgesic activity by Beebe, Xenia, Darczak, Daria, Henry, Rodger F., Vortherms, Timothy, Janis, Richard, Namovic, Marian, Donnelly-Roberts, Diana, Kage, Karen L., Surowy, Carol, Milicic, Ivan, Niforatos, Wende, Swensen, Andrew, Marsh, Kennan C., Wetter, Jill M., Franklin, Pamela, Baker, Scott, Zhong, Chengmin, Simler, Gricelda, Gomez, Erica, Boyce-Rustay, Janel M., Zhu, Chang Z., Stewart, Andrew O., Jarvis, Michael F., Scott, Victoria E.

“…A novel 4-aminocyclopentapyrrolidine series of N-type Ca2+ channel blockers have been discovered. Enantioselective synthesis of the…”
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Diaryldiamines with Dual Inhibition of the Histamine H3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in Pain by Altenbach, Robert J, Black, Lawrence A, Strakhova, Marina I, Manelli, Arlene M, Carr, Tracy L, Marsh, Kennan C, Wetter, Jill M, Wensink, Erica J, Hsieh, Gin C, Honore, Prisca, Garrison, Tiffany Runyan, Brioni, Jorge D, Cowart, Marlon D

“…A series of compounds was designed as dual inhibitors of the H3 receptor and the norepinephrine transporter. Compound 5 (rNET K i = 14 nM; rH3R K i = 37 nM)…”
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Enrichment with Wood Blocks Does Not Affect Toxicity Assessment in an Exploratory Toxicology Model Using Sprague-Dawley Rats by Ditewig, Amy C, Bratcher, Natalie A, Davila, Donna R, Dayton, Brian D, Ebert, Paige, Lesuisse, Philippe, Liguori, Michael J, Wetter, Jill M, Yang, Hyuna, Buck, Wayne R

“…Environmental enrichment in rodents may improve animal well-being but can affect neurologic development, immune system function, and aging. We tested the…”
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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 by 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

“…SAR studies for N-aryl- N′-benzyl urea class of TRPV1 antagonists have been extended to cover α-benzyl alkylation. Alkylated compounds showed weaker in vitro…”
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Discovery of 3-Methyl-N-(1-oxy-3‘,4‘,5‘,6‘-tetrahydro-2‘H-[2,4‘-bipyridine]-1‘-ylmethyl)benzamide (ABT-670), an Orally Bioavailable Dopamine D4 Agonist for the Treatment of Erectile Dysfunction by Patel, Meena V, Kolasa, Teodozyj, Mortell, Kathleen, Matulenko, Mark A, Hakeem, Ahmed A, Rohde, Jeffrey J, Nelson, Sherry L, Cowart, Marlon D, Nakane, Masaki, Miller, Loan N, Uchic, Marie E, Terranova, Marc A, El-Kouhen, Odile F, Donnelly-Roberts, Diana L, Namovic, Marian T, Hollingsworth, Peter R, Chang, Renjie, Martino, Brenda R, Wetter, Jill M, Marsh, Kennan C, Martin, Ruth, Darbyshire, John F, Gintant, Gary, Hsieh, Gin C, Moreland, Robert B, Sullivan, James P, Brioni, Jorge D, Stewart, Andrew O

“…The goal of this study was to identify a structurally distinct D4-selective agonist with superior oral bioavailability to our first-generation clinical…”
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Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: in vitro properties, drug-likeness, and behavioral activity by Cowart, Marlon, Gfesser, Gregory A, Browman, Kaitlin E, Faghih, Ramin, Miller, Thomas R, Milicic, Ivan, Baranowski, John L, Krueger, Kathleen M, Witte, David G, Molesky, Angela L, Komater, Victoria A, Buckley, Michael J, Diaz, Gilbert J, Gagne, Gerard D, Zhou, Deliang, Deng, Xiaoqing, Pan, Liping, Roberts, Ellen M, Diehl, Marilyn S, Wetter, Jill M, Marsh, Kennan C, Fox, Gerard B, Brioni, Jorge D, Esbenshade, Timothy A, Hancock, Arthur A

“…Three novel heterocyclic benzofurans A-688057 (1), A-687136 (2), and A-698418 (3) were profiled for their in vitro and in vivo properties as a new series of…”
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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 by 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

“…The synthesis and structure−activity relationship of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 (TRPV1) antagonists are…”
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Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists by Zheng, Guo Zhu, Bhatia, Pramila, Kolasa, Teodozyj, Patel, Meena, El Kouhen, Odile F., Chang, Renjie, Uchic, Marie E., Miller, Loan, Baker, Scott, Lehto, Sonya G., Honore, Prisca, Wetter, Jill M., Marsh, Kennan C., Moreland, Robert B., Brioni, Jorge D., Stewart, Andrew O.

“…We have discovered a novel, potent, and selective triazafluorenone series of metabotropic glutamate receptor 1 (mGluR1) antagonists with efficacy in various…”
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1-Aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one Oximes as Potent Dopamine D4 Receptor Agonists for the Treatment of Erectile Dysfunction by Kolasa, Teodozyj, Matulenko, Mark A, Hakeem, Ahmed A, Patel, Meena V, Mortell, Kathleen, Bhatia, Pramila, Henry, Rodger, Nakane, Masaki, Hsieh, Gin C, Terranova, Marc A, Uchic, Marie E, Miller, Loan N, Chang, Renje, Donnelly-Roberts, Diana L, Namovic, Marian T, Hollingsworth, Peter R, Martino, Brenda, El Kouhen, Odile, Marsh, Kennan C, Wetter, Jill M, Moreland, Robert B, Brioni, Jorge D, Stewart, Andrew O

“…A new series of dopamine D4 receptor agonists, 1-aryl-3-(4-pyridinepiperazin-1-yl)propanone oximes, was designed through the modification of known dopamine D4…”
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Structure–activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists by 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

“…Novel 5,6-fused heteroaromatic ureas were synthesized and evaluated for their activity as TRPV1 antagonists. It was found that 4-aminoindoles and indazoles are…”
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