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Items: 1 to 50 of 112

1.

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
2.

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
3.

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
4.

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
5.

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
6.

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
7.

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
8.

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
9.

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
10.

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
11.

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
12.

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
13.

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
14.

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
15.

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.

16.

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
17.

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
18.

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
19.

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
20.
21.

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
22.

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
23.

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
24.

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
25.

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
26.

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
27.

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
28.

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
29.

Assessment of pharmacology and potential anti-obesity properties of H3 receptor antagonists/inverse agonists.

Hancock AA, Brune ME.

Expert Opin Investig Drugs. 2005 Mar;14(3):223-41. Review.

PMID:
15833055
30.

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
31.

Effects of histamine H3 receptor antagonists in two models of spatial learning.

Komater VA, Buckley MJ, Browman KE, Pan JB, Hancock AA, Decker MW, Fox GB.

Behav Brain Res. 2005 Apr 30;159(2):295-300. Epub 2004 Dec 10.

PMID:
15817192
32.

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
33.

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
34.

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
35.

Medicinal chemistry and biological properties of non-imidazole histamine H3 antagonists.

Cowart M, Altenbach R, Black L, Faghih R, Zhao C, Hancock AA.

Mini Rev Med Chem. 2004 Nov;4(9):979-92. Review.

PMID:
15544558
36.

Perspectives on cognitive domains, H3 receptor ligands and neurological disease.

Hancock AA, Fox GB.

Expert Opin Investig Drugs. 2004 Oct;13(10):1237-48. Review.

PMID:
15461554
37.

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.

38.

Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.

Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB, Faghih R, Bennani YL, Williams M, Hancock AA.

Biochem Pharmacol. 2004 Sep 1;68(5):933-45.

PMID:
15294456
39.

Enhancement of prepulse inhibition of startle in mice by the H3 receptor antagonists thioperamide and ciproxifan.

Browman KE, Komater VA, Curzon P, Rueter LE, Hancock AA, Decker MW, Fox GB.

Behav Brain Res. 2004 Aug 12;153(1):69-76.

PMID:
15219708
40.

Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.

Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3220-35.

PMID:
15163201
41.

D-amino acid homopiperazine amides: discovery of A-320436, a potent and selective non-imidazole histamine H(3)-receptor antagonist.

Curtis MP, Dwight W, Pratt J, Cowart M, Esbenshade TA, Krueger KM, Fox GB, Pan JB, Pagano TG, Hancock AA, Faghih R, Bennani YL.

Arch Pharm (Weinheim). 2004 Apr;337(4):219-29.

PMID:
15146898
42.

Structure-activity relationships of A-331440: a new histamine-3 antagonist with anti-obesity properties.

Faghih R, Esbenshade TA, Krueger KM, Yao BB, Witte DG, Miller TM, Kang CH, Fox GB, Cowart M, Bennani YL, Hancock AA.

Inflamm Res. 2004 Mar;53 Suppl 1:S79-80. Epub 2004 Mar 5. No abstract available.

PMID:
15054629
43.

Molecular and pharmacological characterization of the monkey histamine H(3) receptor.

Yao BB, Sharma R, Cassar S, Faghih R, Bennani Y, Esbenshade TA, Hancock AA.

Inflamm Res. 2004 Mar;53 Suppl 1:S75-6. Epub 2004 Mar 5. No abstract available.

PMID:
15054627
44.

The medicinal chemistry of novel H(3) antagonists.

Cowart M, Faghih R, Gfesser G, Curtis M, Pratt JK, Bennani Y, Fox GB, Esbenshade TA, Hancock AA.

Inflamm Res. 2004 Mar;53 Suppl 1:S69-70. Epub 2004 Mar 5. No abstract available.

PMID:
15054624
45.

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
46.

Histamine H(3) antagonists in models of obesity.

Hancock AA, Bush EN, Jacobson PB, Faghih R, Esbenshade TA.

Inflamm Res. 2004 Mar;53 Suppl 1:S47-8. Epub 2004 Mar 5. No abstract available.

PMID:
15054613
47.

Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.

Hancock AA, Bennani YL, Bush EN, Esbenshade TA, Faghih R, Fox GB, Jacobson P, Knourek-Segel V, Krueger KM, Nuss ME, Pan JB, Shapiro R, Witte DG, Yao BB.

Eur J Pharmacol. 2004 Mar 8;487(1-3):183-97.

PMID:
15033391
48.

A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.

Cowart M, Pratt JK, Stewart AO, Bennani YL, Esbenshade TA, Hancock AA.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):689-93.

PMID:
14741270
49.

Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.

Gfesser GA, Zhang H, Dinges J, Fox GB, Pan JB, Esbenshade TA, Yao BB, Witte D, Miller TR, Kang CH, Krueger KM, Bennani YL, Hancock AA, Faghih R.

Bioorg Med Chem Lett. 2004 Feb 9;14(3):673-6.

PMID:
14741266
50.

An efficient multigram synthesis of the potent histamine H3 antagonist GT-2331 and the reassessment of the absolute configuration.

Liu H, Kerdesky FA, Black LA, Fitzgerald M, Henry R, Esbenshade TA, Hancock AA, Bennani YL.

J Org Chem. 2004 Jan 9;69(1):192-4.

PMID:
14703397

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