Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia
Bonaventure, Pascal, Shelton, Jonathan, Yun, Sujin, Nepomuceno, Diane, Sutton, Steven, Aluisio, Leah, Fraser, Ian, Lord, Brian, Shoblock, James, Welty, Natalie, Chaplan, Sandra R, Aguilar, Zuleima, Halter, Robin, Ndifor, Anthony, Koudriakova, Tatiana, Rizzolio, Michele, Letavic, Michael, Carruthers, Nicholas I, Lovenberg, Timothy, Dugovic, Christine
Published in The Journal of pharmacology and experimental therapeutics (01.09.2015)
Published in The Journal of pharmacology and experimental therapeutics (01.09.2015)
Get full text
Journal Article
Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement
Shoblock, James R., Welty, Natalie, Aluisio, Leah, Fraser, Ian, Motley, S. Timothy, Morton, Kirsten, Palmer, James, Bonaventure, Pascal, Carruthers, Nicholas I., Lovenberg, Timothy W., Boggs, Jamin, Galici, Ruggero
Published in Psychopharmacologia (01.05.2011)
Published in Psychopharmacologia (01.05.2011)
Get full text
Journal Article
Blockade of Orexin-1 Receptors Attenuates Orexin-2 Receptor Antagonism-Induced Sleep Promotion in the Rat
Dugovic, Christine, Shelton, Jonathan E, Aluisio, Leah E, Fraser, Ian C, Jiang, Xiaohui, Sutton, Steven W, Bonaventure, Pascal, Yun, Sujin, Li, Xiaorong, Lord, Brian, Dvorak, Curt A, Carruthers, Nicholas I, Lovenberg, Timothy W
Published in The Journal of pharmacology and experimental therapeutics (01.07.2009)
Published in The Journal of pharmacology and experimental therapeutics (01.07.2009)
Get full text
Journal Article
Selective Blockade of the Capsaicin Receptor TRPV1 Attenuates Bone Cancer Pain
Ghilardi, Joseph R, Rohrich, Heidi, Lindsay, Theodore H, Sevcik, Molly A, Schwei, Matthew J, Kubota, Kazufumi, Halvorson, Kyle G, Poblete, Jeannie, Chaplan, Sandra R, Dubin, Adrienne E, Carruthers, Nicholas I, Swanson, Devin, Kuskowski, Michael, Flores, Christopher M, Julius, David, Mantyh, Patrick W
Published in The Journal of neuroscience (23.03.2005)
Published in The Journal of neuroscience (23.03.2005)
Get full text
Journal Article
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists
Ameriks, Michael K., Ao, Hong, Carruthers, Nicholas I., Lord, Brian, Ravula, Suchitra, Rech, Jason C., Savall, Brad M., Wall, Jessica L., Wang, Qi, Bhattacharya, Anindya, Letavic, Michael A.
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Get full text
Journal Article
JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats
Galici, Ruggero, Rezvani, Amir H., Aluisio, Leah, Lord, Brian, Levin, Edward D., Fraser, Ian, Boggs, Jamin, Welty, Natalie, Shoblock, James R., Motley, S. Timothy, Letavic, Michael A., Carruthers, Nicholas I., Dugovic, Christine, Lovenberg, Timothy W., Bonaventure, Pascal
Published in Psychopharmacologia (01.04.2011)
Published in Psychopharmacologia (01.04.2011)
Get full text
Journal Article
Identification and Biological Evaluation of 4-(3-Trifluoromethylpyridin-2-yl)piperazine-1-carboxylic Acid (5-Trifluoromethylpyridin-2-yl)amide, a High Affinity TRPV1 (VR1) Vanilloid Receptor Antagonist
Swanson, Devin M, Dubin, Adrienne E, Shah, Chandra, Nasser, Nadia, Chang, Leon, Dax, Scott L, Jetter, Michele, Breitenbucher, J. Guy, Liu, Changlu, Mazur, Curt, Lord, Brian, Gonzales, Lisa, Hoey, Kenway, Rizzolio, Michele, Bogenstaetter, Michael, Codd, Ellen E, Lee, Doo H, Zhang, Sui-Po, Chaplan, Sandra R, Carruthers, Nicholas I
Published in Journal of medicinal chemistry (24.03.2005)
Published in Journal of medicinal chemistry (24.03.2005)
Get full text
Journal Article
Copper-mediated synthesis of drug-like bicyclopentanes
Zhang, Xiaheng, Smith, Russell T, Le, Chip, McCarver, Stefan J, Shireman, Brock T, Carruthers, Nicholas I, MacMillan, David W C
Published in Nature (London) (01.04.2020)
Published in Nature (London) (01.04.2020)
Get full text
Journal Article
A New Class of Diamine-Based Human Histamine H3 Receptor Antagonists: 4-(Aminoalkoxy)benzylamines
Apodaca, Richard, Dvorak, Curt A, Xiao, Wei, Barbier, Ann J, Boggs, Jamin D, Wilson, Sandy J, Lovenberg, Timothy W, Carruthers, Nicholas I
Published in Journal of medicinal chemistry (28.08.2003)
Published in Journal of medicinal chemistry (28.08.2003)
Get full text
Journal Article
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling
BEMBENEK, Scott D, KEITH, John M, LETAVIC, Michael A, APODACA, Richard, BARBIER, Ann J, DVORAK, Lisa, ALUISIO, Leah, MILLER, Kirsten L, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I
Published in Bioorganic & medicinal chemistry (15.03.2008)
Published in Bioorganic & medicinal chemistry (15.03.2008)
Get full text
Journal Article
Pharmacological characterization of JNJ-28583867, a histamine H3 receptor antagonist and serotonin reuptake inhibitor
BARBIER, Ann J, ALUISIO, Leah, PUDIAK, Cindy, DUGOVIC, Christine, SHELTON, Jonathan, MAZUR, Curt, LETAVIC, Michael A, CARRUTHERS, Nicholas I, LOVENBERG, Timothy W, LORD, Brian, YING QU, WILSON, Sandy J, BOGGS, Jamin D, BONAVENTURE, Pascal, MILLER, Kirsten, FRASER, Ian, DVORAK, Lisa
Published in European journal of pharmacology (01.12.2007)
Published in European journal of pharmacology (01.12.2007)
Get full text
Journal Article
Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8
Maher, Michael P, Wu, Nyantsz, Ravula, Suchitra, Ameriks, Michael K, Savall, Brad M, Liu, Changlu, Lord, Brian, Wyatt, Ryan M, Matta, Jose A, Dugovic, Christine, Yun, Sujin, Ver Donck, Luc, Steckler, Thomas, Wickenden, Alan D, Carruthers, Nicholas I, Lovenberg, Timothy W
Published in The Journal of pharmacology and experimental therapeutics (01.05.2016)
Published in The Journal of pharmacology and experimental therapeutics (01.05.2016)
Get full text
Journal Article
A Dipolar Cycloaddition Reaction To Access 6‑Methyl-4,5,6,7-tetrahydro‑1H‑[1,2,3]triazolo[4,5‑c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate
Chrovian, Christa C, Soyode-Johnson, Akinola, Peterson, Alexander A, Gelin, Christine F, Deng, Xiaohu, Dvorak, Curt A, Carruthers, Nicholas I, Lord, Brian, Fraser, Ian, Aluisio, Leah, Coe, Kevin J, Scott, Brian, Koudriakova, Tatiana, Schoetens, Freddy, Sepassi, Kia, Gallacher, David J, Bhattacharya, Anindya, Letavic, Michael A
Published in Journal of medicinal chemistry (11.01.2018)
Published in Journal of medicinal chemistry (11.01.2018)
Get full text
Journal Article
Discovery of a Series of Substituted 1H‑((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators
Gelin, Christine F., Stenne, Brice, Coate, Heather, Hiscox, Afton, Soyode-Johnson, Akinola, Wall, Jessica L., Lord, Brian, Schoellerman, Jeffrey, Coe, Kevin J., Wang, Kai, Alcázar, Jesus, Chrovian, Christa C., Dvorak, Curt A., Carruthers, Nicholas I., Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A.
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
Get full text
Journal Article
Dual serotonin transporter/histamine H3 ligands : Optimization of the H3 pharmacophore
KEITH, John M, GOMEZ, Leslie A, MAZUR, Curt, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I, LETAVIC, Michael A, LY, Kiev S, JABLONOWSKI, Jill A, SEIERSTAD, Mark, BARBIER, Ann J, WILSON, Sandy J, BOGGS, Jamin D, FRASER, Ian C
Published in Bioorganic & medicinal chemistry letters (01.02.2007)
Published in Bioorganic & medicinal chemistry letters (01.02.2007)
Get full text
Journal Article
Discovery of a Series of Substituted 1 H -((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators
Gelin, Christine F, Stenne, Brice, Coate, Heather, Hiscox, Afton, Soyode-Johnson, Akinola, Wall, Jessica L, Lord, Brian, Schoellerman, Jeffrey, Coe, Kevin J, Wang, Kai, Alcázar, Jesus, Chrovian, Christa C, Dvorak, Curt A, Carruthers, Nicholas I, Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
Get full text
Journal Article
4‑Methyl-6,7-dihydro‑4H‑triazolo[4,5‑c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate
Letavic, Michael A, Savall, Brad M, Allison, Brett D, Aluisio, Leah, Andres, Jose Ignacio, De Angelis, Meri, Ao, Hong, Beauchamp, Derek A, Bonaventure, Pascal, Bryant, Stewart, Carruthers, Nicholas I, Ceusters, Marc, Coe, Kevin J, Dvorak, Curt A, Fraser, Ian C, Gelin, Christine F, Koudriakova, Tatiana, Liang, Jimmy, Lord, Brian, Lovenberg, Timothy W, Otieno, Monicah A, Schoetens, Freddy, Swanson, Devin M, Wang, Qi, Wickenden, Alan D, Bhattacharya, Anindya
Published in Journal of medicinal chemistry (08.06.2017)
Published in Journal of medicinal chemistry (08.06.2017)
Get full text
Journal Article
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT7/2 inhibitors leading to the identification of a clinical candidate
Dvorak, Curt A., Rudolph, Dale A., Nepomuceno, Diane, Dvorak, Lisa, Lord, Brian, Fraser, Ian, Bonaventure, Pascal, Lovenberg, Timothy, Carruthers, Nicholas I.
Published in Bioorganic & medicinal chemistry letters (01.01.2021)
Published in Bioorganic & medicinal chemistry letters (01.01.2021)
Get full text
Journal Article
Aplysamine-1 and related analogs as histamine H3 receptor antagonists
SWANSON, Devin M, WILSON, Sandy J, BOGGS, Jamin D, WEI XIAO, APODACA, Richard, BARBIER, Ann J, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I
Published in Bioorganic & medicinal chemistry letters (15.02.2006)
Published in Bioorganic & medicinal chemistry letters (15.02.2006)
Get full text
Journal Article
Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a Small Molecule Antagonist of the Neuropeptide Y Y2 Receptor
Bonaventure, Pascal, Nepomuceno, Diane, Mazur, Curt, Lord, Brian, Rudolph, Dale A, Jablonowski, Jill A, Carruthers, Nicholas I, Lovenberg, Timothy W
Published in The Journal of pharmacology and experimental therapeutics (01.03.2004)
Published in The Journal of pharmacology and experimental therapeutics (01.03.2004)
Get full text
Journal Article