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Results: 1 to 20 of 102

1.

Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.

Moree WJ, Li BF, Zamani-Kord S, Yu J, Coon T, Huang C, Marinkovic D, Tucci FC, Malany S, Bradbury MJ, Hernandez LM, Wen J, Wang H, Hoare SR, Petroski RE, Jalali K, Yang C, Sacaan A, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5874-8. doi: 10.1016/j.bmcl.2010.07.117. Epub 2010 Aug 3.

PMID:
20800486
[PubMed - indexed for MEDLINE]
2.

Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

Moree WJ, Li BF, Jovic F, Coon T, Yu J, Gross RS, Tucci F, Marinkovic D, Zamani-Kord S, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G.

J Med Chem. 2009 Sep 10;52(17):5307-10. doi: 10.1021/jm900933k.

PMID:
19663387
[PubMed - indexed for MEDLINE]
3.

Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.

Huang C, Moree WJ, Zamani-Kord S, Li BF, Tucci FC, Malany S, Wen J, Wang H, Hoare SR, Yang C, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):947-51. doi: 10.1016/j.bmcl.2010.12.053. Epub 2010 Dec 16.

PMID:
21232954
[PubMed - indexed for MEDLINE]
4.

Novel benzothiophene H1-antihistamines for the treatment of insomnia.

Moree WJ, Jovic F, Coon T, Yu J, Li BF, Tucci FC, Marinkovic D, Gross RS, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2316-20. doi: 10.1016/j.bmcl.2010.01.134. Epub 2010 Feb 2.

PMID:
20188547
[PubMed - indexed for MEDLINE]
5.

Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

Li BF, Moree WJ, Yu J, Coon T, Zamani-Kord S, Malany S, Jalali K, Wen J, Wang H, Yang C, Hoare SR, Petroski RE, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2629-33. doi: 10.1016/j.bmcl.2010.02.055. Epub 2010 Feb 18.

PMID:
20227880
[PubMed - indexed for MEDLINE]
6.

Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors.

Malany S, Hernandez LM, Smith WF, Crowe PD, Hoare SR.

J Recept Signal Transduct Res. 2009;29(2):84-93. doi: 10.1080/10799890902721339.

PMID:
19308787
[PubMed - indexed for MEDLINE]
7.

The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.

Lavrador-Erb K, Ravula SB, Yu J, Zamani-Kord S, Moree WJ, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 May 1;20(9):2916-9. doi: 10.1016/j.bmcl.2010.03.027. Epub 2010 Mar 10.

PMID:
20347297
[PubMed - indexed for MEDLINE]
8.

Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.

Böhme TM, Keim C, Kreutzmann K, Linder M, Dingermann T, Dannhardt G, Mutschler E, Lambrecht G.

J Med Chem. 2003 Feb 27;46(5):856-67.

PMID:
12593665
[PubMed - indexed for MEDLINE]
9.

Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

Coon T, Moree WJ, Li B, Yu J, Zamani-Kord S, Malany S, Santos MA, Hernandez LM, Petroski RE, Sun A, Wen J, Sullivan S, Haelewyn J, Hedrick M, Hoare SJ, Bradbury MJ, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4380-4. doi: 10.1016/j.bmcl.2009.05.086. Epub 2009 May 27.

PMID:
19553115
[PubMed - indexed for MEDLINE]
10.

Interaction of terfenadine and its primary metabolites with cytochrome P450 2D6.

Jones BC, Hyland R, Ackland M, Tyman CA, Smith DA.

Drug Metab Dispos. 1998 Sep;26(9):875-82.

PMID:
9733666
[PubMed - indexed for MEDLINE]
Free Article
11.

Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H₁-antihistamines for insomnia.

Ravula SB, Yu J, Tran JA, Arellano M, Tucci FC, Moree WJ, Li BF, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):421-6. doi: 10.1016/j.bmcl.2011.10.115. Epub 2011 Nov 15.

PMID:
22153347
[PubMed - indexed for MEDLINE]
12.

The expanding role of H1 antihistamines: a patent survey of selective and dual activity compounds 2005-2010.

Beaton G, Moree WJ.

Expert Opin Ther Pat. 2010 Sep;20(9):1197-218. doi: 10.1517/13543776.2010.510516. Review.

PMID:
20716024
[PubMed - indexed for MEDLINE]
13.

Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines.

Stahl SM.

CNS Spectr. 2008 Dec;13(12):1027-38. Review.

PMID:
19179941
[PubMed - indexed for MEDLINE]
14.

CYP2D6 is the principal cytochrome P450 responsible for metabolism of the histamine H1 antagonist promethazine in human liver microsomes.

Nakamura K, Yokoi T, Inoue K, Shimada N, Ohashi N, Kume T, Kamataki T.

Pharmacogenetics. 1996 Oct;6(5):449-57.

PMID:
8946477
[PubMed - indexed for MEDLINE]
15.

Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.

Procopiou PA, Browning C, Gore PM, Lynn SM, Richards SA, Slack RJ, Sollis SL.

Bioorg Med Chem. 2012 Oct 15;20(20):6097-108. doi: 10.1016/j.bmc.2012.08.032. Epub 2012 Aug 31.

PMID:
22985961
[PubMed - indexed for MEDLINE]
16.

Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.

Aslanian R, Mutahi Mw, Shih NY, Piwinski JJ, West R, Williams SM, She S, Wu RL, Hey JA.

Bioorg Med Chem Lett. 2003 Jun 16;13(12):1959-61.

PMID:
12781173
[PubMed - indexed for MEDLINE]
17.

Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes.

Nakamura K, Yokoi T, Kodama T, Inoue K, Nagashima K, Shimada N, Shimizu T, Kamataki T.

J Pharmacol Exp Ther. 1998 Feb;284(2):437-42.

PMID:
9454781
[PubMed - indexed for MEDLINE]
Free Article
18.

Studies on the novel antiallergic agent HSR-609: its penetration into the central nervous system in mice and guinea pigs and its selectivity for the histamine H1-receptor.

Kakiuchi M, Ohashi T, Musoh K, Kawamura K, Morikawa K, Kato H.

Jpn J Pharmacol. 1997 Apr;73(4):291-8.

PMID:
9165365
[PubMed - indexed for MEDLINE]
Free Article
19.

In silico binding characteristics between human histamine H1 receptor and antagonists.

Wang X, Yang Q, Li M, Yin D, You Q.

J Mol Model. 2010 Sep;16(9):1529-37. doi: 10.1007/s00894-010-0666-z. Epub 2010 Feb 24.

PMID:
20179978
[PubMed - indexed for MEDLINE]
20.

Review of the histamine system and the clinical effects of H1 antagonists: basis for a new model for understanding the effects of insomnia medications.

Krystal AD, Richelson E, Roth T.

Sleep Med Rev. 2013 Aug;17(4):263-72. doi: 10.1016/j.smrv.2012.08.001. Epub 2013 Jan 26. Review.

PMID:
23357028
[PubMed - indexed for MEDLINE]

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