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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.


Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.

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

J Pharmacol Exp Ther. 2003 Jun;305(3):887-96. Epub 2003 Feb 20.


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.


GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.

Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB, Davis RK, Davis RP, Dawson LA, Foley AG, Gartlon J, Gonzalez MI, Heslop T, Hirst WD, Jennings C, Jones DN, Lacroix LP, Martyn A, Ociepka S, Ray A, Regan CM, Roberts JC, Schogger J, Southam E, Stean TO, Trail BK, Upton N, Wadsworth G, Wald JA, White T, Witherington J, Woolley ML, Worby A, Wilson DM.

J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. Epub 2007 Feb 27.


Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats.

Medhurst AD, Briggs MA, Bruton G, Calver AR, Chessell I, Crook B, Davis JB, Davis RP, Foley AG, Heslop T, Hirst WD, Medhurst SJ, Ociepka S, Ray A, Regan CM, Sargent B, Schogger J, Stean TO, Trail BK, Upton N, White T, Orlek B, Wilson DM.

Biochem Pharmacol. 2007 Apr 15;73(8):1182-94. Epub 2007 Jan 7.


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.


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.


Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687).

McLeod RL, Rizzo CA, West RE Jr, Aslanian R, McCormick K, Bryant M, Hsieh Y, Korfmacher W, Mingo GG, Varty L, Williams SM, Shih NY, Egan RW, Hey JA.

J Pharmacol Exp Ther. 2003 Jun;305(3):1037-44. Epub 2003 Mar 20.


Studies on the pharmacology of the novel histamine H3 receptor agonist Sch 50971.

Hey JA, Aslanian R, Bolser DC, Chapman RW, Egan RW, Rizzo CA, Shih NY, Fernandez X, McLeod RL, West R, Kreutner W.

Arzneimittelforschung. 1998 Sep;48(9):881-8.


SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue.

Scott C, Soffin EM, Hill M, Atkinson PJ, Langmead CJ, Wren PB, Faedo S, Gordon LJ, Price GW, Bromidge S, Johnson CN, Hagan JJ, Watson J.

Eur J Pharmacol. 2006 Apr 24;536(1-2):54-61. Epub 2006 Feb 28.


Two novel and selective nonimidazole H3 receptor antagonists A-304121 and A-317920: II. In vivo behavioral and neurophysiological characterization.

Fox GB, Pan JB, Radek RJ, Lewis AM, Bitner RS, Esbenshade TA, Faghih R, Bennani YL, Williams M, Yao BB, Decker MW, Hancock AA.

J Pharmacol Exp Ther. 2003 Jun;305(3):897-908. Epub 2003 Feb 20.


Histamine H3-receptor inverse agonists as novel antipsychotics.

Ito C.

Cent Nerv Syst Agents Med Chem. 2009 Jun;9(2):132-6. Review.


Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.

Ligneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J.

J Pharmacol Exp Ther. 1998 Nov;287(2):658-66.


Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors.

Rouleau A, Ligneau X, Tardivel-Lacombe J, Morisset S, Gbahou F, Schwartz JC, Arrang JM.

Br J Pharmacol. 2002 Jan;135(2):383-92.


Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.

Yates SL, Phillips JG, Gregory R, Pawlowski GP, Fadnis L, Khan MA, Ali SM, Tedford CE.

J Pharmacol Exp Ther. 1999 May;289(2):1151-9.


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.


H3 receptor-mediated inhibition of intestinal acetylcholine release: pharmacological characterization of signal transduction pathways.

Blandizzi C, Colucci R, Tognetti M, De Paolis B, Del Tacca M.

Naunyn Schmiedebergs Arch Pharmacol. 2001 Feb;363(2):193-202.


Ciproxifan and chemically related compounds are highly potent and selective histamine H3-receptor antagonists.

Kathmann M, Schlicker E, Marr I, Werthwein S, Stark H, Schunack W.

Naunyn Schmiedebergs Arch Pharmacol. 1998 Dec;358(6):623-7.


Development of FUB 181, a selective histamine H3-receptor antagonist of high oral in vivo potency with 4-(omega-(arylalkyloxy)alkyl)-1H-imidazole structure.

Stark H, Hüls A, Ligneau X, Purand K, Pertz H, Arrang JM, Schwartz JC, Schunack W.

Arch Pharm (Weinheim). 1998 Jun;331(6):211-8.


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