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Items: 1 to 20 of 210

1.

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
2.

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
3.

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
4.

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
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
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
8.

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
9.

Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene.

Nicholson AN, Pascoe PA, Turner C, Ganellin CR, Greengrass PM, Casy AF, Mercer AD.

Br J Pharmacol. 1991 Sep;104(1):270-6.

10.

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
11.

Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent.

Mandhane SN, Ayer UB, Midha AS, Rao CT, Rajamannar T.

Drugs R D. 2008;9(2):93-112.

PMID:
18298128
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
13.

The discovery of CCR3/H1 dual antagonists with reduced hERG risk.

Bahl A, Barton P, Bowers K, Brough S, Evans R, Luckhurst CA, Mochel T, Perry MW, Rigby A, Riley RJ, Sanganee H, Sisson A, Springthorpe B.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6688-93. doi: 10.1016/j.bmcl.2012.08.124. Epub 2012 Sep 15.

PMID:
23031591
14.

Are over-the-counter sleep medications effective? All-night EEG studies.

Kales J, Tan TL, Swearingen C, Kales A.

Curr Ther Res Clin Exp. 1971 Mar;13(3):143-51. No abstract available.

PMID:
4397942
15.

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
16.

Effects of second-generation histamine H1 receptor antagonists on the sleep-wakefulness cycle in rats.

Shigemoto Y, Shinomiya K, Mio M, Azuma N, Kamei C.

Eur J Pharmacol. 2004 Jun 28;494(2-3):161-5.

PMID:
15212970
17.

Effect time-course of the inhibition of histamine induced skin reactions by orally applied dimethindene maleate.

Rehn D, Geissler H, Schuster O, Lukas H, Hennings G.

Agents Actions. 1991 May;33(1-2):221-4.

PMID:
1680275
18.
19.

[H1-antihistaminics of the first generation].

Bennack E, Holzgrabe U.

Pharm Unserer Zeit. 2007;36(3):202-4. Review. German. No abstract available.

PMID:
17555056
20.

Effect-time-relation of the H1-receptor antagonist dimethindene maleate following intravenous injection.

Rehn D, Geissler H, Schönbrunn U, Lukas H, Hennings G.

Agents Actions. 1990 Apr;30(1-2):178-81.

PMID:
1973583

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