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Pharmacologic characterization of JNJ-42226314, [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a reversible, selective and potent monoacylglycerol lipase inhibitor.

Wyatt RM, Fraser I, Welty N, Lord B, Wennerholm M, Sutton SW, Ameriks MK, Dugovic C, Yun S, White A, Nguyen L, Koudriakova T, Tian G, Suarez J, Szewczuk L, Bonnette W, Ahn K, Ghosh B, Flores CM, Connolly PJ, Zhu B, Macielag MJ, Brandt MR, Chevalier K, Zhang SP, Lovenberg TW, Bonaventure P.

J Pharmacol Exp Ther. 2019 Dec 9. pii: jpet.119.262139. doi: 10.1124/jpet.119.262139. [Epub ahead of print]


Integrative Analysis of DiseaseLand Omics Database for Disease Signatures and Treatments: A Bipolar Case Study.

Wu C, Huang BE, Chen G, Lovenberg TW, Pocalyko DJ, Yao X.

Front Genet. 2019 Apr 30;10:396. doi: 10.3389/fgene.2019.00396. eCollection 2019.


GPR139 and Dopamine D2 Receptor Co-express in the Same Cells of the Brain and May Functionally Interact.

Wang L, Lee G, Kuei C, Yao X, Harrington A, Bonaventure P, Lovenberg TW, Liu C.

Front Neurosci. 2019 Mar 26;13:281. doi: 10.3389/fnins.2019.00281. eCollection 2019.


Pharmacology of JNJ-28583113: A novel TRPM2 antagonist.

Fourgeaud L, Dvorak C, Faouzi M, Starkus J, Sahdeo S, Wang Q, Lord B, Coate H, Taylor N, He Y, Qin N, Wickenden A, Carruthers N, Lovenberg TW, Penner R, Bhattacharya A.

Eur J Pharmacol. 2019 Jun 15;853:299-307. doi: 10.1016/j.ejphar.2019.03.043. Epub 2019 Apr 6.


Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators.

Savall BM, Wu D, Swanson DM, Seierstad M, Wu N, Vives Martinez J, García Olmos B, Lord B, Coe K, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK.

ACS Med Chem Lett. 2018 Dec 26;10(3):267-272. doi: 10.1021/acsmedchemlett.8b00599. eCollection 2019 Mar 14.


Allosteric Modulation of Ionotropic Glutamate Receptors Special Issue.

Carruthers NI, Lovenberg TW, Traynelis SF.

ACS Med Chem Lett. 2019 Mar 14;10(3):226. doi: 10.1021/acsmedchemlett.9b00047. eCollection 2019 Mar 14. No abstract available.


Mutagenesis of GPR139 reveals ways to create gain or loss of function receptors.

Wang L, Lee G, Shih A, Kuei C, Nepomuceno D, Wennerholm M, Fan F, Wu J, Bonaventure P, Lovenberg TW, Liu C.

Pharmacol Res Perspect. 2019 Feb 7;7(1):e00466. doi: 10.1002/prp2.466. eCollection 2019 Feb.


Lead Optimization of 5-Aryl Benzimidazolone- and Oxindole-Based AMPA Receptor Modulators Selective for TARP γ-8.

Ravula S, Savall BM, Wu N, Lord B, Coe K, Wang K, Seierstad M, Swanson DM, Ziff J, Nguyen M, Leung P, Rynberg R, La D, Pippel DJ, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK.

ACS Med Chem Lett. 2018 Jul 13;9(8):821-826. doi: 10.1021/acsmedchemlett.8b00215. eCollection 2018 Aug 9.


Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia.

Bhattacharya A, Lord B, Grigoleit JS, He Y, Fraser I, Campbell SN, Taylor N, Aluisio L, O'Connor JC, Papp M, Chrovian C, Carruthers N, Lovenberg TW, Letavic MA.

Neuropsychopharmacology. 2018 Dec;43(13):2586-2596. doi: 10.1038/s41386-018-0141-6. Epub 2018 Jul 9.


Allosteric Modulation of Ionotropic Glutamate Receptors Special Issue.

Carruthers NI, Lovenberg TW, Traynelis SF.

ACS Med Chem Lett. 2018 May 10;9(5):398-399. doi: 10.1021/acsmedchemlett.8b00174. eCollection 2018 May 10.


Selective Inhibition of Orexin-2 Receptors Prevents Stress-Induced ACTH Release in Mice.

Yun S, Wennerholm M, Shelton JE, Bonaventure P, Letavic MA, Shireman BT, Lovenberg TW, Dugovic C.

Front Behav Neurosci. 2017 May 8;11:83. doi: 10.3389/fnbeh.2017.00083. eCollection 2017.


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 MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A.

J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25.


Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA.

J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8.


Reply to "A Comment on 'Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8'".

Maher MP, Ameriks MK, Savall BM, Carruthers NI, Lovenberg TW.

J Pharmacol Exp Ther. 2016 Sep;358(3):527. doi: 10.1124/jpet.116.234815. No abstract available.


Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8.

Maher MP, Wu N, Ravula S, Ameriks MK, Savall BM, Liu C, Lord B, Wyatt RM, Matta JA, Dugovic C, Yun S, Ver Donck L, Steckler T, Wickenden AD, Carruthers NI, Lovenberg TW.

J Pharmacol Exp Ther. 2016 May;357(2):394-414. doi: 10.1124/jpet.115.231712. Epub 2016 Mar 17.


Role of neuro-immunological factors in the pathophysiology of mood disorders.

Bhattacharya A, Derecki NC, Lovenberg TW, Drevets WC.

Psychopharmacology (Berl). 2016 May;233(9):1623-36. doi: 10.1007/s00213-016-4214-0. Epub 2016 Jan 23. Review.


Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists.

Ziff J, Rudolph DA, Stenne B, Koudriakova T, Lord B, Bonaventure P, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA, Shireman BT.

ACS Chem Neurosci. 2016 Apr 20;7(4):498-504. doi: 10.1021/acschemneuro.5b00304. Epub 2016 Jan 19.


A novel radioligand for the ATP-gated ion channel P2X7: [3H] JNJ-54232334.

Lord B, Ameriks MK, Wang Q, Fourgeaud L, Vliegen M, Verluyten W, Haspeslagh P, Carruthers NI, Lovenberg TW, Bonaventure P, Letavic MA, Bhattacharya A.

Eur J Pharmacol. 2015 Oct 15;765:551-9. doi: 10.1016/j.ejphar.2015.09.026. Epub 2015 Sep 18.


GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.

Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W, Yao X, Yieh L, Dvorak C, Carruthers N, Coate H, Yun S, Dugovic C, Harrington A, Lovenberg TW.

Mol Pharmacol. 2015 Nov;88(5):911-25. doi: 10.1124/mol.115.100412. Epub 2015 Sep 8.


Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.

Letavic MA, Bonaventure P, Carruthers NI, Dugovic C, Koudriakova T, Lord B, Lovenberg TW, Ly KS, Mani NS, Nepomuceno D, Pippel DJ, Rizzolio M, Shelton JE, Shah CR, Shireman BT, Young LK, Yun S.

J Med Chem. 2015 Jul 23;58(14):5620-36. doi: 10.1021/acs.jmedchem.5b00742. Epub 2015 Jul 8.


Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.

Letavic MA, Aluisio L, Apodaca R, Bajpai M, Barbier AJ, Bonneville A, Bonaventure P, Carruthers NI, Dugovic C, Fraser IC, Kramer ML, Lord B, Lovenberg TW, Li LY, Ly KS, Mcallister H, Mani NS, Morton KL, Ndifor A, Nepomuceno SD, Pandit CR, Sands SB, Shah CR, Shelton JE, Snook SS, Swanson DM, Xiao W.

ACS Med Chem Lett. 2015 Mar 13;6(4):450-4. doi: 10.1021/ml5005156. eCollection 2015 Apr 9.


Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432.

Lord B, Aluisio L, Shoblock JR, Neff RA, Varlinskaya EI, Ceusters M, Lovenberg TW, Carruthers N, Bonaventure P, Letavic MA, Deak T, Drinkenburg W, Bhattacharya A.

J Pharmacol Exp Ther. 2014 Dec;351(3):628-41. doi: 10.1124/jpet.114.218487. Epub 2014 Sep 30.


Orexin-1 receptor blockade dysregulates REM sleep in the presence of orexin-2 receptor antagonism.

Dugovic C, Shelton JE, Yun S, Bonaventure P, Shireman BT, Lovenberg TW.

Front Neurosci. 2014 Feb 14;8:28. doi: 10.3389/fnins.2014.00028. eCollection 2014.


Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567.

Bhattacharya A, Wang Q, Ao H, Shoblock JR, Lord B, Aluisio L, Fraser I, Nepomuceno D, Neff RA, Welty N, Lovenberg TW, Bonaventure P, Wickenden AD, Letavic MA.

Br J Pharmacol. 2013 Oct;170(3):624-40. doi: 10.1111/bph.12314.


The discovery of potent selective NPY Y(2) antagonists.

Chai W, Wong VD, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4141-4. doi: 10.1016/j.bmcl.2013.05.038. Epub 2013 May 22.


Identification of structural motifs critical for epstein-barr virus-induced molecule 2 function and homology modeling of the ligand docking site.

Zhang L, Shih AY, Yang XV, Kuei C, Wu J, Deng X, Mani NS, Mirzadegan T, Sun S, Lovenberg TW, Liu C.

Mol Pharmacol. 2012 Dec;82(6):1094-103. doi: 10.1124/mol.112.080275. Epub 2012 Aug 28.


Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.

Dvorak CA, Liu C, Shelton J, Kuei C, Sutton SW, Lovenberg TW, Carruthers NI.

ACS Med Chem Lett. 2012 Jun 11;3(8):637-9. doi: 10.1021/ml3000676. eCollection 2012 Aug 9.


Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder.

Bonaventure P, Dugovic C, Kramer M, De Boer P, Singh J, Wilson S, Bertelsen K, Di J, Shelton J, Aluisio L, Dvorak L, Fraser I, Lord B, Nepomuceno D, Ahnaou A, Drinkenburg W, Chai W, Dvorak C, Sands S, Carruthers N, Lovenberg TW.

J Pharmacol Exp Ther. 2012 Aug;342(2):429-40. doi: 10.1124/jpet.112.193995. Epub 2012 May 8.


3,5-Dihydroxybenzoic acid, a specific agonist for hydroxycarboxylic acid 1, inhibits lipolysis in adipocytes.

Liu C, Kuei C, Zhu J, Yu J, Zhang L, Shih A, Mirzadegan T, Shelton J, Sutton S, Connelly MA, Lee G, Carruthers N, Wu J, Lovenberg TW.

J Pharmacol Exp Ther. 2012 Jun;341(3):794-801. doi: 10.1124/jpet.112.192799. Epub 2012 Mar 20.


The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.

Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18.


Oxysterols direct B-cell migration through EBI2.

Liu C, Yang XV, Wu J, Kuei C, Mani NS, Zhang L, Yu J, Sutton SW, Qin N, Banie H, Karlsson L, Sun S, Lovenberg TW.

Nature. 2011 Jul 27;475(7357):519-23. doi: 10.1038/nature10226.


Pharmacological blockade of serotonin 5-HT₇ receptor reverses working memory deficits in rats by normalizing cortical glutamate neurotransmission.

Bonaventure P, Aluisio L, Shoblock J, Boggs JD, Fraser IC, Lord B, Lovenberg TW, Galici R.

PLoS One. 2011;6(6):e20210. doi: 10.1371/journal.pone.0020210. Epub 2011 Jun 20.


International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B).

Offermanns S, Colletti SL, Lovenberg TW, Semple G, Wise A, IJzerman AP.

Pharmacol Rev. 2011 Jun;63(2):269-90. doi: 10.1124/pr.110.003301. Epub 2011 Mar 31. Review.


Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement.

Shoblock JR, Welty N, Aluisio L, Fraser I, Motley ST, Morton K, Palmer J, Bonaventure P, Carruthers NI, Lovenberg TW, Boggs J, Galici R.

Psychopharmacology (Berl). 2011 May;215(1):191-203. doi: 10.1007/s00213-010-2127-x. Epub 2010 Dec 22.


Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT(7) antagonists.

Rudolph DA, Dvorak CA, Dvorak L, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):42-4. doi: 10.1016/j.bmcl.2010.11.078. Epub 2010 Nov 24.


The novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist, JNJ-31020028, tested in animal models of alcohol consumption, relapse, and anxiety.

Cippitelli A, Rezvani AH, Robinson JE, Eisenberg L, Levin ED, Bonaventure P, Motley ST, Lovenberg TW, Heilig M, Thorsell A.

Alcohol. 2011 Sep;45(6):567-76. doi: 10.1016/j.alcohol.2010.09.003. Epub 2010 Dec 10.


JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats.

Galici R, Rezvani AH, Aluisio L, Lord B, Levin ED, Fraser I, Boggs J, Welty N, Shoblock JR, Motley ST, Letavic MA, Carruthers NI, Dugovic C, Lovenberg TW, Bonaventure P.

Psychopharmacology (Berl). 2011 Apr;214(4):829-41. doi: 10.1007/s00213-010-2092-4. Epub 2010 Nov 18.


Indole- and benzothiophene-based histamine H3 antagonists.

Santillan A Jr, McClure KJ, Allison BD, Lord B, Boggs JD, Morton KL, Everson AM, Nepomuceno D, Letavic MA, Lee-Dutra A, Lovenberg TW, Carruthers NI, Grice CA.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6226-30. doi: 10.1016/j.bmcl.2010.08.103. Epub 2010 Aug 27.


Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

Letavic MA, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16.


In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor.

Shoblock JR, Welty N, Nepomuceno D, Lord B, Aluisio L, Fraser I, Motley ST, Sutton SW, Morton K, Galici R, Atack JR, Dvorak L, Swanson DM, Carruthers NI, Dvorak C, Lovenberg TW, Bonaventure P.

Psychopharmacology (Berl). 2010 Feb;208(2):265-77. doi: 10.1007/s00213-009-1726-x. Epub 2009 Dec 2.


Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.

Swanson DM, Shah CR, Lord B, Morton K, Dvorak LK, Mazur C, Apodaca R, Xiao W, Boggs JD, Feinstein M, Wilson SJ, Barbier AJ, Bonaventure P, Lovenberg TW, Carruthers NI.

Eur J Med Chem. 2009 Nov;44(11):4413-25. doi: 10.1016/j.ejmech.2009.06.007. Epub 2009 Jun 16.


Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.

Dvorak CA, Apodaca R, Xiao W, Jablonowski JA, Bonaventure P, Dugovic C, Shelton J, Lord B, Miller K, Dvorak LK, Lovenberg TW, Carruthers NI.

Eur J Med Chem. 2009 Oct;44(10):4098-106. doi: 10.1016/j.ejmech.2009.04.049. Epub 2009 May 13.


Relaxin family peptides and receptors in mammalian brain.

Gundlach AL, Ma S, Sang Q, Shen PJ, Piccenna L, Sedaghat K, Smith CM, Bathgate RA, Lawrence AJ, Tregear GW, Wade JD, Finkelstein DI, Bonaventure P, Liu C, Lovenberg TW, Sutton SW.

Ann N Y Acad Sci. 2009 Apr;1160:226-35. doi: 10.1111/j.1749-6632.2009.03956.x. Review.


Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat.

Dugovic C, Shelton JE, Aluisio LE, Fraser IC, Jiang X, Sutton SW, Bonaventure P, Yun S, Li X, Lord B, Dvorak CA, Carruthers NI, Lovenberg TW.

J Pharmacol Exp Ther. 2009 Jul;330(1):142-51. doi: 10.1124/jpet.109.152009. Epub 2009 Apr 10.


JNJ-10181457, a selective non-imidazole histamine H(3) receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition.

Galici R, Boggs JD, Aluisio L, Fraser IC, Bonaventure P, Lord B, Lovenberg TW.

Neuropharmacology. 2009 Jun;56(8):1131-7. doi: 10.1016/j.neuropharm.2009.03.011. Epub 2009 Apr 2.


Novel imidazole-based histamine H3 antagonists.

Jablonowski JA, Ly KS, Bogenstaetter M, Dvorak CA, Boggs JD, Dvorak LK, Lord B, Miller KL, Mazur C, Wilson SJ, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):903-7. doi: 10.1016/j.bmcl.2008.11.114. Epub 2008 Dec 6.


Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81.

Liu C, Wu J, Zhu J, Kuei C, Yu J, Shelton J, Sutton SW, Li X, Yun SJ, Mirzadegan T, Mazur C, Kamme F, Lovenberg TW.

J Biol Chem. 2009 Jan 30;284(5):2811-22. doi: 10.1074/jbc.M806409200. Epub 2008 Dec 1.


Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135).

Zhu J, Kuei C, Sutton S, Kamme F, Yu J, Bonaventure P, Atack J, Lovenberg TW, Liu C.

Eur J Pharmacol. 2008 Aug 20;590(1-3):43-52. doi: 10.1016/j.ejphar.2008.05.025. Epub 2008 May 27.


In-vitro and in-vivo characterization of JNJ-7925476, a novel triple monoamine uptake inhibitor.

Aluisio L, Lord B, Barbier AJ, Fraser IC, Wilson SJ, Boggs J, Dvorak LK, Letavic MA, Maryanoff BE, Carruthers NI, Bonaventure P, Lovenberg TW.

Eur J Pharmacol. 2008 Jun 10;587(1-3):141-6. doi: 10.1016/j.ejphar.2008.04.008. Epub 2008 Apr 10.


2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.

Shireman BT, Dvorak CA, Rudolph DA, Bonaventure P, Nepomuceno D, Dvorak L, Miller KL, Lovenberg TW, Carruthers NI.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2103-8. doi: 10.1016/j.bmcl.2008.01.090. Epub 2008 Jan 30. Erratum in: Bioorg Med Chem Lett. 2008 Jul 15;18(14):4253.


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