J&JPRD - La Jolla, CA - Publications
Home Related Links Contacts Sitemap
Community Research Pipeline Clinical Trials Careers Our R&D Partnerships Newsroom LocationsTransparency
spacer
La Jolla, CA Clinical Trials RESEARCH AND EARLY DEVELOPMENT spacer
spacer
 
spacer spacer
Search Jobs & Internships
Explore the career possibilities at a leading, global company. more
Partner With Us
Accessing external innovation that complements our existing internal research programs is an integral component of our overall R&D strategy for building a successful business. more
Selected Publications
Publication Authors Title Journal
1 Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth. Analg. (2009), 108(1), 316-329.
2 Lebsack AD, Branstetter BJ, Hack MD, Xiao W, Peterson ML, Nasser N, Maher MP, Ao H, Bhattacharya A, Kansagara M, Scott BP, Luo L, Rynberg R, Rizzolio M, Chaplan SR, Wickenden AD, Breitenbucher JG. Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists. Bioorg. Med. Chem. Lett. (2009), 19(1), 40-46.
3 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. Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81. J. Biol. Chem. (2009), 284(5), 2811-2822.
4 Sales ZS, Mani NS. An efficient intramolecular 1,3-dipolar cycloaddition involving 2-(1,2-dichlorovinyloxy)aryldiazomethanes: a one-pot synthesis of benzofuropyrazoles from salicylaldehydes. J. Org. Chem. (2009), 74(2), 891-894.
5 Xu XL, Kapoun AM. Heterogeneous activation of the TGFbeta pathway in glioblastomas identified by gene expression-based classification using TGFbeta-responsive genes. J. Transl. Med. (2009), 7:12, online.
6 Shelton J, Bonaventure P, Li X, Yun S, Lovenberg T, Dugovic C. 5-HT7 receptor deletion enhances REM sleep suppression induced by selective serotonin reuptake inhibitors, but not by direct stimulation of 5-HT1A receptor. Neuropharmacology (2009), 56(2), 448-454.
7 Bembenek SD, Keith JM, Letavic MA, Apodaca R, Barbier AJ, Dvorak L, Aluisio L, Miller KL, Lovenberg TW, Carruthers NI. Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling. Bioorg. Med. Chem. (2008), 16(6), 2968-2973.
8 Rosen MD, Hack MD, Allison BD, Phuong VK, Woods CR, Morton MF, Prendergast CE, Barrett TD, Schubert C, Li L, Wu X, Wu J, Freedman JM, Shankley NP, Rabinowitz MH. Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis. Bioorg. Med. Chem. (2008), 16(7), 3917-3925.
9 Shireman BT, Dvorak CA, Rudolph DA, Bonaventure P, Nepomuceno D, Dvorak L, Miller KL, Lovenberg TW, Carruthers NI. 2-Alkyl-4-aryl pyrimidine fused heterocycles as selective 5-HT2A antagonists. Bioorg. Med. Chem. Lett. (2008), 18(6), 2103-2108.
10 Timmons A, Seierstad M, Apodaca R, Epperson M, Pippel D, Brown S, Chang L, Scott B, Webb M, Chaplan SR, Breitenbucher JG. Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH). Bioorg. Med. Chem. Lett. (2008), 18(6), 2109-2113.
11 Wolin RL, Bembenek SD, Wei J, Crawford S, Lundeen K, Brunmark A, Karlsson L, Edwards JP, Blevitt JM. Dual binding site inhibitors of B-RAF kinase. Bioorg. Med. Chem. Lett. (2008), 18(9), 2825-2829.
12 Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG. Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. Bioorg. Med. Chem. Lett. (2008), 18(17), 4838-4843.
13 Barrett TD, Yan W, Freedman JM, Lagaud GJ, Breitenbucher JG, Shankley NP. Role of CCK and potential utility of CCK1 receptor antagonism in the treatment of pancreatitis induced by biliary tract obstruction. Br. J. Pharmacol. (2008), 153(8), 1650-1658.
14 Aluisio L, Lord B, Barbier AJ, Fraser IC, Wilson SJ, Boggs J, Dvorak LK, Letavic MA, Maryanoff BE, Carruthers NI, Bonaventure P, Lovenberg TW. In-vitro and in-vivo characterization of JNJ-7925476, a novel triple monoamine uptake inhibitor. Eur. J. Pharmacol. (2008), 587(1-3), 141-146.
15 Zhu J, Kuei C, Sutton S, Kamme F, Yu J, Bonaventure P, Atack J, Lovenberg TW, Liu C. Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135). Eur. J. Pharmacol. (2008), 590(1-3), 43-52.
16 Reynolds CH, Tounge BA, Bembenek SD. Ligand binding efficiency: trends, physical basis, and implications. J. Med. Chem. (2008), 51(8), 2432-2438.
17 Grice CA, Tays KL, Savall BM, Wei J, Butler CR, Axe FU, Bembenek SD, Fourie AM, Dunford PJ, Lundeen K, Coles F, Xue X, Riley JP, Williams KN, Karlsson L, Edwards JP. Identification of a potent, selective, and orally active leukotriene A4 hydrolase inhibitor with anti-inflammatory activity. J. Med. Chem. (2008), 51(14), 4150-4169.
18 Seierstad M, Breitenbucher JG. Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors. J. Med. Chem. (2008), 51(23), 7327-7343.
19 Keith JM. One-step conversion of heteroaromatic-N-oxides to imidazolo-heteroarenes. J. Org. Chem. (2008), 73(1), 327-330.
20 Deng X, Mani NS. Regioselective synthesis of 1,3,5-tri and 1,3,4,5-tetrasubstituted pyrazoles from N-arylhydrazones and nitroolefins. J. Org. Chem. (2008), 73(6), 2412-2415.
21 Liu J, Fitzgerald AE, Mani NS. Facile assembly of fused benzo[4,5]furo heterocycles. J. Org. Chem. (2008), 73(7), 2951-2954.
22 Crawford S, Belajic D, Wei J, Riley JP, Dunford PJ, Bembenek S, Fourie A, Edwards JP, Karlsson L, Brunmark A, Wolin RL, Blevitt JM. A novel B-RAF inhibitor blocks interleukin-8 (IL-8) synthesis in human melanoma xenografts, revealing IL-8 as a potential pharmacodynamic biomarker. Mol. Cancer Ther. (2008), 7(3), 492-499.
23 Maher M, Ao H, Banke T, Nasser N, Wu NT, Breitenbucher JG, Chaplan SR, Wickenden AD. Activation of TRPA1 by farnesyl thiosalicylic acid. Mol. Pharmacol. (2008), 73(4), 1225-1234.
24 Deng X, Mani NS. Base-mediated reaction of hydrazones and nitroolefins with a reversed regioselectivity: a novel synthesis of 1,3,4-trisubstituted pyrazoles. Org. Lett. (2008), 10(6), 1307-1310.
25 Deng X, Mani NS. Regioselective Synthesis of 1,3,5-Trisubstituted Pyrazoles by the Reaction of N-Monosubstituted Hydrazones with Nitroolefins. Org. Synth. (2008), 85, 179-188.
26 Wiener JJ, Gomez L, Venkatesan H, Santillan A Jr, Allison BD, Schwarz KL, Shinde S, Tang L, Hack MD, Morrow BJ, Motley ST, Goldschmidt RM, Shaw KJ, Jones TK, Grice CA. Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains. Bioorg. Med. Chem. Lett. (2007), 17(10), 2718-2722.
27 Gomez L, Hack MD, Wu J, Wiener JJ, Venkatesan H, Santillan A Jr, Pippel DJ, Mani N, Morrow BJ, Motley ST, Shaw KJ, Wolin R, Grice CA, Jones TK. Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis. Bioorg. Med. Chem. Lett. (2007), 17(10), 2723-2727.
28 Reynolds CH, Bembenek SD, Tounge BA. The role of molecular size in ligand efficiency. Bioorg. Med. Chem. Lett. (2007), 17(15), 4258-4261.
29 Wei J, Pio BA, Cai H, Meduna SP, Sun S, Gu Y, Jiang W, Thurmond RL, Karlsson L, Edwards JP. Pyrazole-based cathepsin S inhibitors with improved cellular potency. Bioorg. Med. Chem. Lett. (2007), 17(20), 5525-5528.
30 Neff DK, Lee-Dutra A, Blevitt JM, Axe FU, Hack MD, Buma JC, Rynberg R, Brunmark A, Karlsson L, Breitenbucher JG. 2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2. Bioorg. Med. Chem. Lett. (2007), 17(23), 6467-6471.
31 Gomez L, Hack MD, McClure K, Sehon C, Huang L, Morton M, Li L, Barrett TD, Shankley N, Breitenbucher JG. SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists. Bioorg. Med. Chem. Lett. (2007), 17(23), 6493-6498.
32 Woods CR, Hack MD, Allison BD, Phuong VK, Rosen MD, Morton MF, Prendergast CE, Barrett TD, Shankley NP, Rabinowitz MH. Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands. Bioorg. Med. Chem. Lett. (2007), 17(24), 6905-6909.
33 Dorai H, Li K, Huang CC, Bittner A, Galindo J, Carmen A. Genome-wide analysis of mouse myeloma cell lines expressing therapeutic antibodies. Biotechnol. Prog. (2007), 23(4), 911-920.
34 Barbier AJ, Aluisio L, Lord B, Qu Y, Wilson SJ, Boggs JD, Bonaventure P, Miller K, Fraser I, Dvorak C, Pudiak C, Dugovic C, Shelton J, Mazur C, Letavic M, Carruthers NI, Lovenberg TW. Pharmacological characterization of JNJ-28583867, a histamine H3 receptor antagonist and serotonin reuptake inhibitor. Eur. J. Pharmacol. (2007), 576(1-3), 43-54.
35 Tham CS, Whitaker J, Luo L, Webb M. Inhibition of microglial fatty acid amide hydrolase modulates LPS stimulated release of inflammatory mediators. FEBS Lett. (2007), 581(16), 2899-2904.
36 Dunford PJ, Williams KN, Desai PJ, Karlsson L, McQueen D, Thurmond RL. Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus. J. Allergy Clin. Immunol. (2007), 119(1), 176-183.
37 Kuei C, Sutton S, Bonaventure P, Pudiak C, Shelton J, Zhu J, Nepomuceno D, Wu J, Chen J, Kamme F, Seierstad M, Hack M, Bathgate RAD, Hossain MA, Wade JD, Atack J, Lovenberg TW, Liu C. R3(BDelta23 27)R/I5 Chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization. J. Biol. Chem. (2007), 282(35), 25425-25435.
38 Maher MP, Wu NT, Ao H. pH-Insensitive FRET voltage dyes. J. Biomol. Screen. (2007), 12(5), 656-667.
39 Agrafiotis DK, Alex S, Dai H, Derkinderen A, Farnum M, Gates P, Izrailev S, Jaeger EP, Konstant P, Leung A, Lobanov VS, Marichal P, Martin D, Rassokhin DN, Shemanarev M, Skalkin A, Stong J, Tabruyn T, Vermeiren M, Wan J, Xu XY, Yao X. Advanced biological and chemical discovery (ABCD): centralizing discovery knowledge in an inherently decentralized world. J. Chem. Inf. Model. (2007), 47(6), 1999-2014.
40 Romero FA, Du W, Hwang I, Rayl TJ, Kimball FS, Leung D, Hoover HS, Apodaca RL, Breitenbucher JG, Cravatt BF, Boger DL. Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. J. Med. Chem. (2007), 50(5), 1058-1068.
41 Pippel DJ, Mapes CM, Mani NS. Reactions between Weinreb amides and 2-magnesiated oxazoles: a simple and efficient preparation of 2-acyl oxazoles. J. Org. Chem. (2007), 72(15), 5828-5831.
42 Liang JT, Mani NS, Jones TK. Design of concise, scaleable route to a cholecystokinin 1 (CCK 1) receptor antagonist. J. Org. Chem. (2007), 72(22), 8243-8250.
43 Bonaventure P, Kelly L, Aluisio L, Shelton J, Lord B, Galici R, Miller K, Atack J, Lovenberg TW, Dugovic C. Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents. J. Pharmacol. Exp. Ther. (2007), 321(2), 690-698.
44 Rao NL, Dunford PJ, Xue X, Jiang X, Lundeen KA, Coles F, Riley JP, Williams KN, Grice CA, Edwards JP, Karlsson L, Fourie AM. Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton. J. Pharmacol. Exp. Ther. (2007), 321(3), 1154-1160.
45 Morton MF, Barrett TD, Yan W, Freedman JM, Lagaud G, Prendergast CE, Moreno V, Pyati J, Figueroa K, Li L, Wu X, Rizzolio M, Breitenbucher JG, McClure K, Shankley NP. 3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide. J. Pharmacol. Exp. Ther. (2007), 323(2), 562-569.
46 Bhattacharya A, Scott BP, Nasser N, Ao H, Maher MP, Dubin AE, Swanson DM, Shankley NP, Wickenden AD, Chaplan SR. Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J. Pharmacol. Exp. Ther. (2007), 323(2), 665-674.
47 Luo L, Chang L, Brown SM, Ao H, Lee DH, Higuera ES, Dubin AE, Chaplan SR. Role of peripheral hyperpolarization-activated cyclic nucleotide-modulated channel pacemaker channels in acute and chronic pain models in the rat. Neuroscience (2007), 144(4), 1477-1485.
48 Morrill C, Mani NS. Synthesis of 4-arylpiperidines from 1-benzyl-4-piperidone: application of the Shapiro reaction and alkenylsilane cross-coupling. Org. Lett. (2007), 9(8), 1505-1508.
49 Mapes CM, Mani NS. High-yielding syntheses of 1-piperidin-4-yl butyro- and valerolactams through a tandem reductive amination-lactamization (reductive lactamization). Org. Process Res. Dev. (2007), 11(3), 482-486.
50 Deng X, Liang JT, Liu J, McAllister H, Schubert C, Mani N. A practical synthesis of enantiopure 7-alkoxy-4-aryl-tetrahydroisoquinoline, a dual serotonin reuptake inhibitor/histamine H3 antagonist. Org. Process Res. Dev. (2007), 11(6), 1043-1050.
51 Letavic MA, Ly KS. Microwave assisted, palladium catalyzed aminocarbonylations of heteroaromatic bromides using solid Mo(CO)6 as the carbon monoxide source. Tetrahedron Lett. (2007), 48(13), 2339-2343.
52 Swanson DM, Wilson SJ, Boggs JD, Xiao W, Apodaca R, Barbier AJ, Lovenberg TW, Carruthers NI. Aplysamine-1 and related analogs as histamine H3 receptor antagonists. Bioorg. Med. Chem. Lett. (2006), 16(4), 897-900.
53 McClure KJ, Huang L, Arienti KL, Axe FU, Brunmark A, Blevitt J, Breitenbucher JG. Novel non-benzimidazole Chk2 kinase inhibitors. Bioorg. Med. Chem. Lett. (2006), 16(7) 1924-1928.
54 Grice CA, Tays K, Khatuya H, Gustin DJ, Butler CR, Wei J, Sehon CA, Sun S, Gu Y, Jiang W, Thurmond RL, Karlsson L, Edwards JP. The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors. Bioorg. Med. Chem. Lett. (2006), 16(8), 2209-2212.
55 Lee-Dutra A, Arienti KL, Buzard DJ, Hack MD, Khatuya H, Desai PJ, Nguyen S, Thurmond RL, Karlsson L, Edwards JP, Breitenbucher JG. Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands. Bioorg. Med. Chem. Lett. (2006), 16(23), 6043-6048.
56 Chang L, Luo L, Palmer JA, Sutton S, Wilson SJ, Barbier AJ, Breitenbucher JG, Chaplan SR, Webb M. Inhibition of fatty acid amide hydrolase produces analgesia by multiple mechanisms. Br. J. Pharmacol. (2006), 48(1), 102-113.
57 Seierstad M, Agrafiotis DK. A QSAR model of hERG binding using a large, diverse, and internally consistent training set. Chem. Biol. Drug Des. (2006), 67(4), 284-296.
58 Deng X, Mani NS. A facile, environmentally benign sulfonamide synthesis in water. Green Chem. (2006), 8, 835-839.
59 Sanjuan MA, Rao N, Lai K-T A, Gu Y, Sun S, Fuchs A, Fung-Leung W-P, Colonna M, Karlsson L. CpG-induced tyrosine phosphorylation occurs via a TLR9-independent mechanism and is required for cytokine secretion. J. Cell Biol. (2006), 172(7), 1057-1068.
60 Bembenek SD. Calculation of the surface tension of oxygen using molecular dynamics simulations. J. Chem. Phys. (2006), 124(1), 014709-1 - 014709-4.
61 Dunford PJ, O'Donnell N, Riley JP, Williams KN, Karlsson L, Thurmond RL. The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells. J. Immunol. (2006), 176(11), 7062-7070.
62 Lundeen KA, Sun B, Karlsson L, Fourie AM. Leukotriene B4 receptors BLT1 and BLT2: expression and function in human and murine mast cells. J. Immunol. (2006), 177(5), 3439-3447.
63 Allison BD, Phuong VK, McAtee LC, Rosen M, Morton M, Prendergast C, Barrett T, Lagaud G, Freedman J, Li L, Wu X, Venkatesan H, Pippel M, Woods C, Rizzolio M C, Hack M, Hoey K, Deng X, King C, Shankley NP, Rabinowitz MH. Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists. J. Med. Chem. (2006), 49(21), 6371-6390.
64 Axe FU, Bembenek SD, Szalma S. Three-dimensional models of histamine H3 receptor antagonist complexes and their pharmacophore. J. Mol. Graph. Model. (2006), 24(6), 456-464.
65 Mani NS, Mapes CM, Wu J, Deng X, Jones TK. Stereoselective synthesis of Z-alpha-aryl-alpha,beta-unsaturated esters. J. Org. Chem. (2006), 71(13), 5039-5042.
66 Xue X, Lai K-T A, Huang J-F, Gu Y, Karlsson L, Fourie A. Anti-inflammatory activity in vitro and in vivo of the protein farnesyltransferase inhibitor tipifarnib. J. Pharmacol. Exp. Ther. (2006), 317(1), 53-60.
67 Nie AY, McMillian M, Parker JB, Leone A, Bryant S, Yieh L, Bittner A, Nelson J, Carmen A, Wan J, Lord PG. Predictive toxicogenomics approaches reveal underlying molecular mechanisms of nongenotoxic carcinogenicity. Mol. Carcinog. (2006), 45(12), 914-933.
68 Airaksinen AJ, Jablonowski JA, van der Mey M, Barbier AJ, Klok RP, Verbeek J, Schuit R, Herscheid JDM, Leysen JE, Carruthers NI, Lammertsma AA, Windhorst AD. Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: evaluation of a potential PET ligand. Nucl. Med. Biol. (2006), 33(6), 801-810.
69 Deng X, Mani NS. An efficient route to 4-aryl-5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine. Org. Lett. (2006), 8(2), 269-272.
70 Deng X, Mani NS. Reaction of N-monosubstituted hydrazones with nitroolefins: a novel regioselective pyrazole synthesis. Org. Lett. (2006), 8(16), 3505-3508.
71 Deng X, Stephanek S, Pippel MCW, Mani NS. Oxidation of 4-halo-2-nitrotoluene with tetrabutylammonium permanganate in pyridine: development and safety evaluation. Org. Process Res. Dev. (2006), 10(6), 1287-1291.
72 Jones NA, Morton MF, Prendergast CE, Powell GL, Shankley NP, Hollingsworth SJ. Neuromedin U stimulates contraction of human long saphenous vein and gastrointestinal smooth muscle in vitro. Regul. Pept. (2006), 136(1-3), 109-116.
73 Breitenbucher JG, Chaplan SR, Carruthers NI. The TRPV1 vanilloid receptor: a target for therapeutic intervention. Annu. Rep. Med. Chem. (2005), 40 185-198.
74 Liu C, Kuei C, Sutton S, Chen J, Bonaventure P, Wu J, Nepomuceno D, Kamme F, Tran D-T, Zhu J, Wilkinson T, Bathgate R, Eriste E, Sillard R, Lovenberg TW. INSL5 is a high affinity specific agonist for GPCR142 (GPR100). J. Biol. Chem. (2005), 280(1), 292-300.
75 Dubin AE, Nasser N, Rohrbacher J, Hermans AN, Marrannes R, Grantham C, Van Rossem K, Cik M, Chaplan SR, Gallacher D, Xu J, Guia A, Byrne NG, Mathes C. Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp. J. Biomol. Screen. (2005), 10(2), 168-181.
76 Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI. 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. J. Med. Chem. (2005), 48(6), 1857-1872.
77 Ghilardi JR, Rohrich H, Lindsay TH, Sevcik MA, Schwei MJ, Kubota K, Halvorson KG, Poblete J, Chaplan SR, Dubin AE, Carruthers NI, Swanson D, Kuskowski M, Flores CM, Julius D, Mantyh PW. Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J. Neurosci. (2005), 25(12), 3126-3131.
78 Dvorak CA, Rudolph DA, Ma S, Carruthers NI. Palladium-catalyzed coupling of pyrazole triflates with arylboronic acids. J. Org. Chem. (2005), 70(10), 4188-4190.
79 Lee DH, Chang L, Sorkin LS, Chaplan SR. Hyperpolarization-activated, cation-nonselective, cyclic nucleotide-modulated channel blockade alleviates mechanical allodynia and suppresses ectopic discharge in spinal nerve ligated rats. J. Pain (2005), 6(7), 417-424.
80 Chen J, Kuei C, Sutton S, Wilson SJ, Yu J, Kamme F, Mazur C, Lovenberg TW, Liu C. Identification and pharmacological characterization of prokineticin for prokineticin receptor 1. Mol. Pharmacol. (2005), 67(6), 2070-2076.
81 Galindo J, Jones N, Lowell GL, Hollingsworth SJ, Shankley N. Advanced qRT-PCR technology allows detection of the cholecystokinin 1 receptor (CCK1R) expression in human pancreas. Pancreas (Hagerstown, MD, United States) (2005), 31(4), 325-331.
82 Deng X, Mani NS. Boron trifluoride etherate-assisted ring opening of ethylene oxide by a chiral organolithium: enantioselective synthesis of (R)-N-Boc-2-(2-hydroxyethyl)pyrrolidine. Tetrahedron: Asymmetry (2005), 16, 661-664.
83 McMillian MK, Nie A, Parker JB, Leone AM, Kemmerer M, Bryant S, Herlich J, Yieh L, Bittner A, Liu X, Wan J, Johnson MD, Lord P. Drug-induced oxidative stress in rat liver from a toxicogenomics perspective. Toxicol. Appl. Pharmacol. (2005), 207(2), 171-178.
84 McMillian MK, Nie AY, Parker JB, Leone AM, Kemmerer M, Bryant S, Herlich J, Yieh L, Bittner A, Liu X, Wan J, Johnson MD. Inverse gene expression patterns for macrophage activating hepatotoxicants and peroxisome proliferators in rat liver. Biochem. Pharmacol. (2004), 67(11), 2141-2165.
85 McMillian MK, Nie AY, Parker JB, Leone AM, Bryant S, Kemmerer M, Herlich J, Liu Y, Yieh L, Bittner A, Liu X, Wan J, Johnson MD. A gene expression signature for oxidant stress/reactive metabolites in rat liver. Biochem. Pharmacol. (2004), 68(11), 2249-2261.
86 Jablonowski JA, Chai W, Li X, Rudolph DA, Murray WV, Youngman MA, Dax SL, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI. Novel non-peptidic neuropeptide Y Y2 receptor antagonists. Bioorg. Med. Chem. Lett. (2004), 14(5), 1239-1242.
87 McAtee LC, Sutton SW, Rudolph DE, Li X, Aluisio LE, Phuong VK, Dvorak CA, Lovenberg TW, Carruthers NI, Jones TK. Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OXR2) antagonists. Bioorg. Med. Chem. Lett. (2004), 14(16), 4225-4229.
88 Li J, Mbow M, Sun L, Li L, Yang G, Griswold D, Schantz A, Shealy D, Goletz J, Wan J, Peritt D. Induction of dendritic cell maturation by IL-18. Cell Immunol. (2004), 227(2), 103-108.
89 Dai H, Tian B, Zhao WD, Leung A, Smith SR, Wan JS, Yao X. Dynamic integration of gene annotation and its application to microarray analysis. J. Bioinform. Comput. Biol. (2004), 1(4), 627-646.
90 Wu J, McAllster H. Hold-and-flush, a novel fraction collection method in semi-preparative subcritical and supercritical fluid chromatography. J. Chromatogr., A (2004), 1024, 169-172.
91 Mani NS, Jablonowski JA, Jones TK. A scalable synthesis of a histamine H3 receptor antagonist. J. Org. Chem. (2004), 69(23), 8115-8117.
92 Bonaventure P, Nepomuceno D, Mazur C, Lord B, Rudoloph D, Jablonowski JA, Carruthers NI, Lovenberg TW. Characterization of JNJ-5207787 (N-(1-acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]-acrylamide), a small molecule antagonist of the neuropeptide Y Y2 receptor. J. Pharmacol. Exp. Ther. (2004), 308(3), 1130-1137.
93 Prouty S, Nathan D, Ledwith J, Salisbury M, Lyon G, Messer A, Amaratunga D, Go O, Wan J, Ilyin S. Integrative tools for data analysis in pharmaceutical R&D. PharmaGenomics (2004), September, 28-32.
94 Liu C, Eriste E, Sutton S, Chen J, Roland B, Kuei C, Farmer N, Jornvall H, Sillard R, Lovenberg TW. Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G protein-coupled receptor GPCR135. J. Biol. Chem. (2003), 278(50), 50754-50764.
95 Van der Meij M, Carruthers NI, Herscheid JDM, Jablonowski JA, Leysen JE, Windhorst AD. Reductive N-alkylation of secondary amines with [2-11C]acetone. J. Labelled Compd. Radiopharm. (2003), 46(11), 1075-1085.
96 Wu J, McAllister H. Exact mass measurement on an electrospray ionization time-of-flight mass spectrometer: error distribution and selective averaging. J. Mass Spectrom. (2003), 38(10), 1043-1053.
97 Jablonowski JA, Grice CA, Chai W, Dvorak C, Venable JD, Kwok AK, Ly KS, Wei J, Baker SM, Desai PJ, Jiang W, Wilson SJ, Thurmond RL, Karlsson L, Edwards JP, Lovenberg TW, Carruthers NI. The first potent and selective non-imidazole human histamine H4 receptor antagonists. J. Med. Chem. (2003), 46(19), 3957-3960.
98 Chaplan SR, Guo HQ, Lee DH, Luo L, Liu C, Kuei C, Velumian AA, Butler MP, Brown SM, Dubin AE. Neuronal hyperpolarization-activated pacemaker channels drive neuropathic pain. J. Neurosci. (2003), 23(4), 1169-1178.
99 Chai W, Kwok A, Wong V, Carruthers NI, Wu J. A practical parallel synthesis of 2-substituted indolizines. Synlett (2003), 14(13), 2086-2088.
100 Liu C, Ma X-J, Jiang X, Wilson SJ, Hofstra CL, Blevitt J, Pyati J, Li X, Chai W, Carruthers N, Lovenberg TW. Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. (2001), 59(3), 420-426.
101 Lovenberg TW, Roland BL, Wilson SJ, Jiang X, Pyati J, Huvar A, Jackson MR, Erlander MG. Cloning and functional expression of the human histamine H3 receptor. Mol. Pharmacol. (1999), 55(6), 1101-1107.


Back to top
Back to La Jolla's main page

 
Community | Research Pipeline | Clinical Trials | Careers | Our R&D Partnerships | Newsroom | Locations | Transparency
Contacts | Sitemap | Legal Information | Privacy Policy | Safe Harbor Policy | Related Links
This site is published by Johnson & Johnson Pharmaceutical Research & Development, L.L.C. which is solely responsible for its contents. It is intended for visitors from Belgium, France, Spain, Switzerland, the United Kingdom, and the United States.

© JOHNSON & JOHNSON PHARMACEUTICAL RESEARCH & DEVELOPMENT, L.L.C. 2009-2010
No part of this Web site may be reproduced or transmitted in any form to individuals outside of Johnson & Johnson without prior permission of the publisher. All content on this Web site is licensed, controlled, or owned by Johnson & Johnson Pharmaceutical Research & Development, L.L.C., and is protected by worldwide copyright laws.

This page last updated on: May 29 2009 at 14:01:01 EDT.