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Items: 28

1.

Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure Based Drug Design.

Hobson AD, Judge RA, Aguirre AL, Brown BS, Cui Y, Ding P, Dominguez E, DiGiammarino E, Egan DA, Freiberg GM, Gopalakrishnan SM, Harris CM, Honore MP, Kage KL, Kapecki NJ, Ling C, Ma J, Mack H, Mamo M, Maurus S, McRae B, Moore NS, Mueller BK, Mueller R, Namovic MT, Patel K, Pratt SD, Putman CB, Queeney KL, Sarris KK, Schaffter LM, Stoll VS, Vasudevan A, Wang L, Wang L, Wirthl W, Yach K.

J Med Chem. 2018 Nov 1. doi: 10.1021/acs.jmedchem.8b01098. [Epub ahead of print]

PMID:
30384606
2.

Short-term oral gavage administration of adenine induces a model of fibrotic kidney disease in rats.

Zhu CZ, Doyle KJ, Nikkel AL, Olsen L, Namovic MT, Salte K, Widomski D, Su Z, Donnelly-Roberts DL, Gopalakrishnan MM, McGaraughty S.

J Pharmacol Toxicol Methods. 2018 Nov - Dec;94(Pt 1):34-43. doi: 10.1016/j.vascn.2018.04.003. Epub 2018 Apr 22.

PMID:
29684554
3.

Design of Aminobenzothiazole Inhibitors of Rho Kinases 1 and 2 by Using Protein Kinase A as a Structure Surrogate.

Judge RA, Vasudevan A, Scott VE, Simler GH, Pratt SD, Namovic MT, Putman CB, Aguirre A, Stoll VS, Mamo M, Swann SI, Cassar SC, Faltynek CR, Kage KL, Boyce-Rustay JM, Hobson AD.

Chembiochem. 2018 Mar 16;19(6):613-621. doi: 10.1002/cbic.201700547. Epub 2018 Jan 30.

PMID:
29314498
4.

High throughput functional assays for P2X receptors.

Namovic MT, Jarvis MF, Donnelly-Roberts D.

Curr Protoc Pharmacol. 2012 Jun;Chapter 9:Unit 9.15.. doi: 10.1002/0471141755.ph0915s57.

PMID:
22684723
5.

Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.

Perez-Medrano A, Donnelly-Roberts DL, Florjancic AS, Nelson DW, Li T, Namovic MT, Peddi S, Faltynek CR, Jarvis MF, Carroll WA.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3297-300. doi: 10.1016/j.bmcl.2011.04.024. Epub 2011 Apr 14.

PMID:
21536435
6.

Comparative analysis of inactivated-state block of N-type (Ca(v)2.2) calcium channels.

Vortherms TA, Swensen AM, Niforatos W, Limberis JT, Neelands TR, Janis RS, Thimmapaya R, Donnelly-Roberts DL, Namovic MT, Zhang D, Brent Putman C, Martin RL, Surowy CS, Jarvis MF, Scott VE.

Inflamm Res. 2011 Jul;60(7):683-93. doi: 10.1007/s00011-011-0322-9. Epub 2011 Mar 11.

PMID:
21394563
7.

Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.

Donnelly-Roberts DL, Namovic MT, Han P, Jarvis MF.

Br J Pharmacol. 2009 Aug;157(7):1203-14. doi: 10.1111/j.1476-5381.2009.00233.x. Epub 2009 Jun 22.

8.

Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.

Perez-Medrano A, Donnelly-Roberts DL, Honore P, Hsieh GC, Namovic MT, Peddi S, Shuai Q, Wang Y, Faltynek CR, Jarvis MF, Carroll WA.

J Med Chem. 2009 May 28;52(10):3366-76. doi: 10.1021/jm8015848.

PMID:
19397270
9.

[3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors.

Donnelly-Roberts DL, Namovic MT, Surber B, Vaidyanathan SX, Perez-Medrano A, Wang Y, Carroll WA, Jarvis MF.

Neuropharmacology. 2009 Jan;56(1):223-9. doi: 10.1016/j.neuropharm.2008.06.012. Epub 2008 Jun 17.

PMID:
18602931
10.

Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.

Nelson DW, Sarris K, Kalvin DM, Namovic MT, Grayson G, Donnelly-Roberts DL, Harris R, Honore P, Jarvis MF, Faltynek CR, Carroll WA.

J Med Chem. 2008 May 22;51(10):3030-4. doi: 10.1021/jm701516f. Epub 2008 Apr 26.

PMID:
18438986
11.

Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.

Florjancic AS, Peddi S, Perez-Medrano A, Li B, Namovic MT, Grayson G, Donnelly-Roberts DL, Jarvis MF, Carroll WA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2089-92. doi: 10.1016/j.bmcl.2008.01.095. Epub 2008 Jan 30.

PMID:
18272366
12.

Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.

Morytko MJ, Betschmann P, Woller K, Ericsson A, Chen H, Donnelly-Roberts DL, Namovic MT, Jarvis MF, Carroll WA, Rafferty P.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2093-6. doi: 10.1016/j.bmcl.2008.01.094. Epub 2008 Jan 30.

PMID:
18272365
13.

Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.

Carroll WA, Kalvin DM, Perez Medrano A, Florjancic AS, Wang Y, Donnelly-Roberts DL, Namovic MT, Grayson G, Honoré P, Jarvis MF.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):4044-8. Epub 2007 Apr 27.

PMID:
17482819
14.

P2X7-related modulation of pathological nociception in rats.

McGaraughty S, Chu KL, Namovic MT, Donnelly-Roberts DL, Harris RR, Zhang XF, Shieh CC, Wismer CT, Zhu CZ, Gauvin DM, Fabiyi AC, Honore P, Gregg RJ, Kort ME, Nelson DW, Carroll WA, Marsh K, Faltynek CR, Jarvis MF.

Neuroscience. 2007 Jun 8;146(4):1817-28. Epub 2007 May 3.

PMID:
17478048
15.

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.

Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO.

J Med Chem. 2006 Dec 14;49(25):7450-65.

PMID:
17149874
16.

A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat.

Honore P, Donnelly-Roberts D, Namovic MT, Hsieh G, Zhu CZ, Mikusa JP, Hernandez G, Zhong C, Gauvin DM, Chandran P, Harris R, Medrano AP, Carroll W, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85. Epub 2006 Sep 18.

PMID:
16982702
17.

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.

Kolasa T, Matulenko MA, Hakeem AA, Patel MV, Mortell K, Bhatia P, Henry R, Nakane M, Hsieh GC, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino B, El Kouhen O, Marsh KC, Wetter JM, Moreland RB, Brioni JD, Stewart AO.

J Med Chem. 2006 Aug 24;49(17):5093-109.

PMID:
16913699
18.

Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.

Nelson DW, Gregg RJ, Kort ME, Perez-Medrano A, Voight EA, Wang Y, Grayson G, Namovic MT, Donnelly-Roberts DL, Niforatos W, Honore P, Jarvis MF, Faltynek CR, Carroll WA.

J Med Chem. 2006 Jun 15;49(12):3659-66.

PMID:
16759108
19.

2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist.

Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR, Wetter JM, Marsh K, Stewart AO, Brioni JD, Moreland RB.

Neuropharmacology. 2005 Jul;49(1):112-21. Epub 2005 Apr 1.

PMID:
15992586
20.

Pharmacological characterization of P2X7 receptors in rat peritoneal cells.

Chen YW, Donnelly-Roberts DL, Namovic MT, Gintant GA, Cox BF, Jarvis MF, Harris RR.

Inflamm Res. 2005 Mar;54(3):119-26.

PMID:
15883745
21.

Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.

Matulenko MA, Surber B, Fan L, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Moreland RB, Brioni JD, Stewart AO.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5095-8.

PMID:
15380206
22.

ABT-963 [2-(3,4-difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one], a highly potent and selective disubstituted pyridazinone cyclooxgenase-2 inhibitor.

Harris RR, Black L, Surapaneni S, Kolasa T, Majest S, Namovic MT, Grayson G, Komater V, Wilcox D, King L, Marsh K, Jarvis MF, Nuss M, Nellans H, Pruesser L, Reinhart GA, Cox B, Jacobson P, Stewart A, Coghlan M, Carter G, Bell RL.

J Pharmacol Exp Ther. 2004 Dec;311(3):904-12. Epub 2004 Jul 26.

PMID:
15277581
23.

Comparative pharmacology of human dopamine D(2)-like receptor stable cell lines coupled to calcium flux through Galpha(qo5).

Moreland RB, Nakane M, Donnelly-Roberts DL, Miller LN, Chang R, Uchic ME, Terranova MA, Gubbins EJ, Helfrich RJ, Namovic MT, El-Kouhen OF, Masters JN, Brioni JD.

Biochem Pharmacol. 2004 Aug 15;68(4):761-72.

PMID:
15276084
24.

Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.

Cowart M, Latshaw SP, Bhatia P, Daanen JF, Rohde J, Nelson SL, Patel M, Kolasa T, Nakane M, Uchic ME, Miller LN, Terranova MA, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino BR, Lynch JJ 3rd, Sullivan JP, Hsieh GC, Moreland RB, Brioni JD, Stewart AO.

J Med Chem. 2004 Jul 15;47(15):3853-64.

PMID:
15239663
25.

Synthesis and functional activity of (2-aryl-1-piperazinyl)-N-(3-methylphenyl)acetamides: selective dopamine D4 receptor agonists.

Matulenko MA, Hakeem AA, Kolasa T, Nakane M, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Moreland RB, Brioni JD, Stewart AO.

Bioorg Med Chem. 2004 Jul 1;12(13):3471-83.

PMID:
15186832
26.

Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.

Stewart AO, Cowart MD, Moreland RB, Latshaw SP, Matulenko MA, Bhatia PA, Wang X, Daanen JF, Nelson SL, Terranova MA, Namovic MT, Donnelly-Roberts DL, Miller LN, Nakane M, Sullivan JP, Brioni JD.

J Med Chem. 2004 Apr 22;47(9):2348-55.

PMID:
15084133
27.

Mitogen-activated protein kinase and caspase signaling pathways are required for P2X7 receptor (P2X7R)-induced pore formation in human THP-1 cells.

Donnelly-Roberts DL, Namovic MT, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2004 Mar;308(3):1053-61. Epub 2003 Nov 21.

PMID:
14634045
28.

Pharmacological modulation of eosinophil influx into the lungs of Brown Norway rats.

Namovic MT, Walsh RE, Goodfellow C, Harris RR, Carter GW, Bell RL.

Eur J Pharmacol. 1996 Nov 7;315(1):81-8.

PMID:
8960868

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