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Items: 1 to 50 of 98

1.

α7 Nicotinic receptor agonist enhances cognition in aged 3xTg-AD mice with robust plaques and tangles.

Medeiros R, Castello NA, Cheng D, Kitazawa M, Baglietto-Vargas D, Green KN, Esbenshade TA, Bitner RS, Decker MW, LaFerla FM.

Am J Pathol. 2014 Feb;184(2):520-9. doi: 10.1016/j.ajpath.2013.10.010. Epub 2013 Nov 19.

PMID:
24269557
2.

Assessment of the abuse liability of ABT-288, a novel histamine H₃ receptor antagonist.

Hudzik TJ, Basso A, Boyce-Rustay JM, Bracken W, Browman KE, Drescher K, Esbenshade TA, Loberg LI, Lynch JJ 3rd, Brioni JD.

Psychopharmacology (Berl). 2013 Jul;228(2):187-97. doi: 10.1007/s00213-013-3027-7. Epub 2013 Feb 28.

PMID:
23455597
3.

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
4.

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
5.

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
6.

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
7.

Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.

Koenig JR, Liu H, Drizin I, Witte DG, Carr TL, Manelli AM, Milicic I, Strakhova MI, Miller TR, Esbenshade TA, Brioni JD, Cowart M.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1900-4. doi: 10.1016/j.bmcl.2010.01.131. Epub 2010 Feb 1.

PMID:
20171098
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.

Use of the H3 receptor antagonist radioligand [3H]-A-349821 to reveal in vivo receptor occupancy of cognition enhancing H3 receptor antagonists.

Miller TR, Milicic I, Bauch J, Du J, Surber B, Browman KE, Marsh K, Cowart M, Brioni JD, Esbenshade TA.

Br J Pharmacol. 2009 May;157(1):139-49. doi: 10.1111/j.1476-5381.2009.00239.x.

11.

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.

12.

Localization of histamine H4 receptors in the central nervous system of human and rat.

Strakhova MI, Nikkel AL, Manelli AM, Hsieh GC, Esbenshade TA, Brioni JD, Bitner RS.

Brain Res. 2009 Jan 23;1250:41-8. doi: 10.1016/j.brainres.2008.11.018. Epub 2008 Nov 19.

PMID:
19046950
13.

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
14.

Cloning and characterization of the monkey histamine H3 receptor isoforms.

Strakhova MI, Fox GB, Carr TL, Witte DG, Vortherms TA, Manelli AM, Miller TR, Yao BB, Brioni JD, Esbenshade TA.

Eur J Pharmacol. 2008 Dec 28;601(1-3):8-15. doi: 10.1016/j.ejphar.2008.10.026. Epub 2008 Oct 21.

PMID:
18977214
15.

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
16.

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
17.

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
18.

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
19.

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.

20.

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
21.

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
22.

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
23.

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
24.

A new family of histamine H3 receptor antagonists based on a natural product: discovery, SAR, and properties of the series.

Cowart M, Sun M, Zhao C, Witte DG, Miller TR, Krueger KM, Browman K, Fox GB, Bennani YL, Esbenshade TA, Hancock AA.

Inflamm Res. 2007 Apr;56 Suppl 1:S47-8. No abstract available.

PMID:
17806176
25.

Pharmacological classification of histamine H3 receptor agents across species is attributable to transmembrane 3 sequence differences.

Esbenshade TA, Estvander BR, Miller TR, Baranowski JL, Sharma R, Hancock AA, Krueger KM.

Inflamm Res. 2007 Apr;56 Suppl 1:S45-6. No abstract available.

PMID:
17806175
26.

Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: in vitro properties, drug-likeness, and behavioral activity.

Cowart M, Gfesser GA, Browman KE, Faghih R, Miller TR, Milicic I, Baranowski JL, Krueger KM, Witte DG, Molesky AL, Komater VA, Buckley MJ, Diaz GJ, Gagne GD, Zhou D, Deng X, Pan L, Roberts EM, Diehl MS, Wetter JM, Marsh KC, Fox GB, Brioni JD, Esbenshade TA, Hancock AA.

Biochem Pharmacol. 2007 Apr 15;73(8):1243-55. Epub 2007 Feb 23.

PMID:
17371699
27.

4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.

Black LA, Nersesian DL, Sharma P, Ku YY, Bennani YL, Marsh KC, Miller TR, Esbenshade TA, Hancock AA, Cowart M.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1443-6. Epub 2006 Dec 1.

PMID:
17169555
28.

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
29.

Evidence for tolerance following repeated dosing in rats with ciproxifan, but not with A-304121.

Pan JB, Yao BB, Miller TR, Kroeger PE, Bennani YL, Komater VA, Esbenshade TA, Hancock AA, Decker MW, Fox GB.

Life Sci. 2006 Aug 29;79(14):1366-79. Epub 2006 Apr 26.

PMID:
16730751
30.

Detection of multiple H3 receptor affinity states utilizing [3H]A-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand.

Witte DG, Yao BB, Miller TR, Carr TL, Cassar S, Sharma R, Faghih R, Surber BW, Esbenshade TA, Hancock AA, Krueger KM.

Br J Pharmacol. 2006 Jul;148(5):657-70. Epub 2006 May 22.

31.

Fluorescent benzofuran histamine H(3) receptor antagonists with sub-nanomolar potency.

Cowart M, Gfesser GA, Bhatia K, Esser R, Sun M, Miller TR, Krueger K, Witte D, Esbenshade TA, Hancock AA.

Inflamm Res. 2006 Apr;55 Suppl 1:S47-8. No abstract available.

PMID:
16705379
32.

Differences in pharmacological properties of histamine H(3) receptor agonists and antagonists revealed at two human H (3) receptor isoforms.

Esbenshade TA, Krueger KM, Yao BB, Witte DG, Estvander BR, Baranowski JL, Miller TR, Hancock AA.

Inflamm Res. 2006 Apr;55 Suppl 1:S45-6. No abstract available.

PMID:
16705378
33.

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
34.

Differential CNS expression and functional activity of multiple human H(3) receptor isoforms.

Esbenshade TA, Strakhova MI, Carr TL, Sharma R, Witte DG, Yao BB, Miller TR, Hancock AA.

Inflamm Res. 2006 Apr;55 Suppl 1:S38-9. No abstract available.

PMID:
16547816
35.

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
36.

Histamine in cardiac sympathetic ganglia: a novel neurotransmitter?

Fryer RM, Reinhart GA, Esbenshade TA.

Mol Interv. 2006 Feb;6(1):14-9, 2.

PMID:
16507745
37.

Overview of signal transduction.

Esbenshade TA, Duzic E.

Curr Protoc Pharmacol. 2006 Jan;Chapter 2:Unit2.1. doi: 10.1002/0471141755.ph0201s31. Review.

PMID:
21953400
38.

Use of an inverse agonist radioligand [3H]A-317920 reveals distinct pharmacological profiles of the rat histamine H3 receptor.

Yao BB, Witte DG, Miller TR, Carr TL, Kang CH, Cassar S, Faghih R, Bennani YL, Surber BW, Hancock AA, Esbenshade TA.

Neuropharmacology. 2006 Mar;50(4):468-78. Epub 2005 Nov 28.

PMID:
16316670
39.

Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.

Sun M, Zhao C, Gfesser GA, Thiffault C, Miller TR, Marsh K, Wetter J, Curtis M, Faghih R, Esbenshade TA, Hancock AA, Cowart M.

J Med Chem. 2005 Oct 6;48(20):6482-90. Erratum in: J Med Chem. 2012 Jan 12;55(1):563.

PMID:
16190774
40.

Use of novel, non-imidazole inverse agonist radioligands to define histamine H3 receptor pharmacology.

Esbenshade TA, Yao BB, Witte DG, Carr TL, Sharma R, Baranowski JL, Krueger KM, Miller TR, Surber BW, Faghih R, Hancock AA.

Inflamm Res. 2005 Apr;54 Suppl 1:S46-7. No abstract available.

PMID:
15928830
41.

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
42.

Achievement of behavioral efficacy and improved potency in new heterocyclic analogs of benzofuran H3 antagonists.

Cowart M, Faghih R, Gfesser G, Curtis M, Sun M, Zhao C, Bennani Y, Wetter J, Marsh K, Miller TR, Krueger K, Pan JB, Drescher K, Fox GB, Esbenshade TA, Hancock AA.

Inflamm Res. 2005 Apr;54 Suppl 1:S25-6. No abstract available.

PMID:
15928820
43.

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
44.

Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs.

Zhang M, Ballard ME, Pan L, Roberts S, Faghih R, Cowart M, Esbenshade TA, Fox GB, Decker MW, Hancock AA, Rueter LE.

Brain Res. 2005 May 31;1045(1-2):142-9. Epub 2005 Apr 20.

PMID:
15910772
45.

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
46.

G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations.

Krueger KM, Witte DG, Ireland-Denny L, Miller TR, Baranowski JL, Buckner S, Milicic I, Esbenshade TA, Hancock AA.

J Pharmacol Exp Ther. 2005 Jul;314(1):271-81. Epub 2005 Apr 8.

PMID:
15821027
47.

4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.

Cowart M, Faghih R, Curtis MP, Gfesser GA, Bennani YL, Black LA, Pan L, Marsh KC, Sullivan JP, Esbenshade TA, Fox GB, Hancock AA.

J Med Chem. 2005 Jan 13;48(1):38-55.

PMID:
15634000
48.

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
49.

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
50.

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.

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