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Items: 39

1.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR.

J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2.

PMID:
27077528
2.

Pharmacological properties and procognitive effects of ABT-288, a potent and selective histamine H3 receptor antagonist.

Esbenshade TA, Browman KE, Miller TR, Krueger KM, Komater-Roderwald V, Zhang M, Fox GB, Rueter L, Robb HM, Radek RJ, Drescher KU, Fey TA, Bitner RS, Marsh K, Polakowski JS, Zhao C, Cowart MD, Hancock AA, Sullivan JP, Brioni JD.

J Pharmacol Exp Ther. 2012 Oct;343(1):233-45. doi: 10.1124/jpet.112.194126. Epub 2012 Jul 19.

PMID:
22815533
3.

Antagonism of supraspinal histamine H3 receptors modulates spinal neuronal activity in neuropathic rats.

McGaraughty S, Chu KL, Cowart MD, Brioni JD.

J Pharmacol Exp Ther. 2012 Oct;343(1):13-20. doi: 10.1124/jpet.112.194761. Epub 2012 Jun 22.

PMID:
22729221
4.

Diaryldiamines with dual inhibition of the histamine H(3) 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.

Altenbach RJ, Black LA, Strakhova MI, Manelli AM, Carr TL, Marsh KC, Wetter JM, Wensink EJ, Hsieh GC, Honore P, Garrison TR, Brioni JD, Cowart MD.

J Med Chem. 2010 Nov 11;53(21):7869-73. doi: 10.1021/jm100666w.

PMID:
20945906
5.

Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease.

Brioni JD, Esbenshade TA, Garrison TR, Bitner SR, Cowart MD.

J Pharmacol Exp Ther. 2011 Jan;336(1):38-46. doi: 10.1124/jpet.110.166876. Epub 2010 Sep 23. Review.

PMID:
20864505
6.

Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems.

Hsieh GC, Honore P, Pai M, Wensink EJ, Chandran P, Salyers AK, Wetter JM, Zhao C, Liu H, Decker MW, Esbenshade TA, Cowart MD, Brioni JD.

Brain Res. 2010 Oct 1;1354:74-84. doi: 10.1016/j.brainres.2010.07.083. Epub 2010 Aug 1.

PMID:
20682302
7.

In vitro studies on a class of quinoline containing histamine H3 antagonists.

Liu H, Altenbach RJ, Diaz GJ, Manelli AM, Martin RL, Miller TR, Esbenshade TA, Brioni JD, Cowart MD.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3295-300. doi: 10.1016/j.bmcl.2010.04.045. Epub 2010 Apr 18.

PMID:
20457525
8.

H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats.

Hsieh GC, Chandran P, Salyers AK, Pai M, Zhu CZ, Wensink EJ, Witte DG, Miller TR, Mikusa JP, Baker SJ, Wetter JM, Marsh KC, Hancock AA, Cowart MD, Esbenshade TA, Brioni JD, Honore P.

Pharmacol Biochem Behav. 2010 Mar;95(1):41-50. doi: 10.1016/j.pbb.2009.12.004. Epub 2009 Dec 11.

PMID:
20004681
9.

Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.

Zhao C, Sun M, Bennani YL, Miller TR, Witte DG, Esbenshade TA, Wetter J, Marsh KC, Hancock AA, Brioni JD, Cowart MD.

J Med Chem. 2009 Aug 13;52(15):4640-9. doi: 10.1021/jm900480x.

PMID:
19588934
10.

In vitro and in vivo characterization of A-940894: a potent histamine H4 receptor antagonist with anti-inflammatory properties.

Strakhova MI, Cuff CA, Manelli AM, Carr TL, Witte DG, Baranowski JL, Vortherms TA, Miller TR, Rundell L, McPherson MJ, Adair RM, Brito AA, Bettencourt BM, Yao BB, Wetter JM, Marsh KC, Liu H, Cowart MD, Brioni JD, Esbenshade TA.

Br J Pharmacol. 2009 May;157(1):44-54. doi: 10.1111/j.1476-5381.2009.00236.x.

11.

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.

Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD.

J Med Chem. 2008 Nov 27;51(22):7094-8. doi: 10.1021/jm8007618.

PMID:
18983139
12.

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.

Cowart MD, Altenbach RJ, Liu H, Hsieh GC, Drizin I, Milicic I, Miller TR, Witte DG, Wishart N, Fix-Stenzel SR, McPherson MJ, Adair RM, Wetter JM, Bettencourt BM, Marsh KC, Sullivan JP, Honore P, Esbenshade TA, Brioni JD.

J Med Chem. 2008 Oct 23;51(20):6547-57. doi: 10.1021/jm800670r. Epub 2008 Sep 26.

PMID:
18817367
13.

Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.

Altenbach RJ, Adair RM, Bettencourt BM, Black LA, Fix-Stenzel SR, Gopalakrishnan SM, Hsieh GC, Liu H, Marsh KC, McPherson MJ, Milicic I, Miller TR, Vortherms TA, Warrior U, Wetter JM, Wishart N, Witte DG, Honore P, Esbenshade TA, Hancock AA, Brioni JD, Cowart MD.

J Med Chem. 2008 Oct 23;51(20):6571-80. doi: 10.1021/jm8005959. Epub 2008 Sep 24.

PMID:
18811133
14.

The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.

Zhao C, Sun M, Bennani YL, Gopalakrishnan SM, Witte DG, Miller TR, Krueger KM, Browman KE, Thiffault C, Wetter J, Marsh KC, Hancock AA, Esbenshade TA, Cowart MD.

J Med Chem. 2008 Sep 11;51(17):5423-30. doi: 10.1021/jm8003625. Epub 2008 Aug 7.

PMID:
18683917
15.

A robust and high-capacity [(35)S]GTPgammaS binding assay for determining antagonist and inverse agonist pharmacological parameters of histamine H(3) receptor ligands.

Miller TR, Baranowski JL, Estvander BR, Witte DG, Carr TL, Manelli AM, Krueger KM, Cowart MD, Brioni JD, Esbenshade TA.

Assay Drug Dev Technol. 2008 Jun;6(3):339-49. doi: 10.1089/adt.2007.118.

PMID:
18593375
16.

The histamine H3 receptor: an attractive target for the treatment of cognitive disorders.

Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD.

Br J Pharmacol. 2008 Jul;154(6):1166-81. doi: 10.1038/bjp.2008.147. Epub 2008 May 12. Review.

17.

Minimization of potential hERG liability in histamine H3 receptor antagonists.

Black LA, Liu H, Diaz GJ, Fox GB, Browman KE, Wetter J, Marsh KC, Miller TR, Esbenshade TA, Brioni J, Cowart MD.

Inflamm Res. 2008;57 Suppl 1:S45-6. doi: 10.1007/s00011-007-0622-2. No abstract available.

PMID:
18345496
18.

In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.

Nersesian DL, Black LA, Miller TR, Vortherms TA, Esbenshade TA, Hancock AA, Cowart MD.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.

PMID:
18077160
19.

Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.

Altenbach RJ, Liu H, Banfor PN, Browman KE, Fox GB, Fryer RM, Komater VA, Krueger KM, Marsh K, Miller TR, Pan JB, Pan L, Sun M, Thiffault C, Wetter J, Zhao C, Zhou D, Esbenshade TA, Hancock AA, Cowart MD.

J Med Chem. 2007 Nov 1;50(22):5439-48. Epub 2007 Oct 6.

PMID:
17918921
20.

An 80-amino acid deletion in the third intracellular loop of a naturally occurring human histamine H3 isoform confers pharmacological differences and constitutive activity.

Bongers G, Krueger KM, Miller TR, Baranowski JL, Estvander BR, Witte DG, Strakhova MI, van Meer P, Bakker RA, Cowart MD, Hancock AA, Esbenshade TA, Leurs R.

J Pharmacol Exp Ther. 2007 Dec;323(3):888-98. Epub 2007 Sep 12.

PMID:
17855474
21.

Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.

Muchmore SW, Smith RA, Stewart AO, Cowart MD, Gomtsyan A, Matulenko MA, Yu H, Severin JM, Bhagwat SS, Lee CH, Kowaluk EA, Jarvis MF, Jakob CL.

J Med Chem. 2006 Nov 16;49(23):6726-31.

PMID:
17154503
22.

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
23.

In vitro preclinical cardiac assessment of tolterodine and terodiline: multiple factors predict the clinical experience.

Martin RL, Su Z, Limberis JT, Palmatier JD, Cowart MD, Cox BF, Gintant GA.

J Cardiovasc Pharmacol. 2006 Nov;48(5):199-206.

PMID:
17110801
24.

Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety.

Basso AM, Bratcher NA, Gallagher KB, Cowart MD, Zhao C, Sun M, Esbenshade TA, Brune ME, Fox GB, Schmidt M, Collins CA, Souers AJ, Iyengar R, Vasudevan A, Kym PR, Hancock AA, Rueter LE.

Eur J Pharmacol. 2006 Jul 1;540(1-3):115-20. Epub 2006 May 6.

PMID:
16765941
25.

Histamine H3 receptor antagonists: preclinical promise for treating obesity and cognitive disorders.

Esbenshade TA, Fox GB, Cowart MD.

Mol Interv. 2006 Apr;6(2):77-88, 59. Review.

PMID:
16565470
26.

Distinctions and contradistinctions between antiobesity histamine H(3) receptor (H (3)R) antagonists compared to cognition-enhancing H (3) receptor antagonists.

Hancock AA, Bitner RS, Krueger KM, Otte S, Nikkel AL, Fey TA, Bush EN, Dickinson RW, Shapiro R, Knourek-Segel V, Droz BA, Brune ME, Jacobson PB, Cowart MD, Esbenshade TA.

Inflamm Res. 2006 Apr;55 Suppl 1:S42-4. No abstract available.

PMID:
16547814
27.

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
28.

Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy.

Hancock AA, Diehl MS, Fey TA, Bush EN, Faghih R, Miller TR, Krueger KM, Pratt JK, Cowart MD, Dickinson RW, Shapiro R, Knourek-Segel VE, Droz BA, McDowell CA, Krishna G, Brune ME, Esbenshade TA, Jacobson PB.

Inflamm Res. 2005 Apr;54 Suppl 1:S27-9. No abstract available.

PMID:
15928821
29.

Selective H3 receptor (H3R) blockade: broad efficacy in cognition and schizophrenia.

Fox GB, Esbenshade TA, Pan JB, Browman KE, Zhang M, Ballard ME, Radek RJ, Miner H, Bitner RS, Krueger KM, Yao BB, Faghih R, Rueter LE, Komater VA, Drescher KU, Buckley MJ, Sullivan JP, Cowart MD, Decker MW, Hancock AA.

Inflamm Res. 2005 Apr;54 Suppl 1:S23-4. No abstract available.

PMID:
15928819
30.

Structure-activity relationships of arylbenzofuran H3 receptor antagonists.

Gfesser GA, Faghih R, Bennani YL, Curtis MP, Esbenshade TA, Hancock AA, Cowart MD.

Bioorg Med Chem Lett. 2005 May 16;15(10):2559-63.

PMID:
15863316
31.

5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors.

Matulenko MA, Lee CH, Jiang M, Frey RR, Cowart MD, Bayburt EK, Didomenico S, Gfesser GA, Gomtsyan A, Zheng GZ, McKie JA, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Wismer CT, Mikusa J, Marsh KC, Snyder RD, Diehl MS, Kowaluk EA, Jarvis MF, Bhagwat SS.

Bioorg Med Chem. 2005 Jun 1;13(11):3705-20.

PMID:
15863000
32.

Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.

Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, Marsh K, Bennani YL, Cowart MD, Sullivan JP, Hancock AA.

J Pharmacol Exp Ther. 2005 Apr;313(1):165-75. Epub 2004 Dec 17.

PMID:
15608078
33.

Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist.

Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan JP, Cowart MD, Decker MW, Hancock AA.

J Pharmacol Exp Ther. 2005 Apr;313(1):176-90. Epub 2004 Dec 17.

PMID:
15608077
34.

In vitro optimization of structure activity relationships of analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists.

Hancock AA, Diehl MS, Faghih R, Bush EN, Krueger KM, Krishna G, Miller TR, Wilcox DM, Nguyen P, Pratt JK, Cowart MD, Esbenshade TA, Jacobson PB.

Basic Clin Pharmacol Toxicol. 2004 Sep;95(3):144-52.

35.

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
36.

Cognition enhancing effects of novel H(3) receptor (H(3)R) antagonists in several animal models.

Fox GB, Pan JB, Lewis AM, Browman KE, Komater VA, Buckley MJ, Curzon P, Radek RJ, Faghih R, Esbenshade TA, Cowart MD, Decker MW, Hancock AA.

Inflamm Res. 2004 Mar;53 Suppl 1:S49-50. Epub 2004 Mar 5. No abstract available.

PMID:
15054614
37.

Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.

Zheng GZ, Mao Y, Lee CH, Pratt JK, Koenig JR, Perner RJ, Cowart MD, Gfesser GA, McGaraughty S, Chu KL, Zhu C, Yu H, Kohlhaas K, Alexander KM, Wismer CT, Mikusa J, Jarvis MF, Kowaluk EA, Stewart AO.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3041-4.

PMID:
12941329
38.

Molecular recognition in aqueous media. Conformationally restricted water-soluble cyclophanes derived from 6H,12H-5,11-methanodibenzo[b,f][1,5]diazocine.

Cowart MD, Sucholeiki I, Bukownik RR, Wilcox CS.

J Am Chem Soc. 1988 Aug 1;110(18):6204-10. doi: 10.1021/ja00226a040. No abstract available.

PMID:
22148800

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