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Items: 1 to 50 of 93

1.

Toreforant, an orally active histamine H4-receptor antagonist, in patients with active rheumatoid arthritis despite methotrexate: mechanism of action results from a phase 2, multicenter, randomized, double-blind, placebo-controlled synovial biopsy study.

Boyle DL, DePrimo SE, Calderon C, Chen D, Dunford PJ, Barchuk W, Firestein GS, Thurmond RL.

Inflamm Res. 2019 Apr;68(4):261-274. doi: 10.1007/s00011-019-01218-y. Epub 2019 Feb 9.

PMID:
30739130
3.

A phase 2a study of toreforant, a histamine H4 receptor antagonist, in eosinophilic asthma.

Kollmeier AP, Barnathan ES, O'Brien C, Chen B, Xia YK, Zhou B, Loza MJ, Silkoff PE, Ge M, Thurmond RL.

Ann Allergy Asthma Immunol. 2018 Nov;121(5):568-574. doi: 10.1016/j.anai.2018.08.001. Epub 2018 Aug 11.

PMID:
30102965
4.

Phase 2a, randomized, double-blind, placebo-controlled, multicentre, parallel-group study of an H4 R-antagonist (JNJ-39758979) in adults with uncontrolled asthma.

Kollmeier AP, Greenspan A, Xu XL, Silkoff PE, Barnathan ES, Loza MJ, Jiang J, Zhou B, Chen B, Thurmond RL.

Clin Exp Allergy. 2018 Aug;48(8):957-969. doi: 10.1111/cea.13154. Epub 2018 Jun 6.

PMID:
29682796
5.

Histamine H4 receptor antagonism prevents the progression of diabetic nephropathy in male DBA2/J mice.

Pini A, Grange C, Veglia E, Argenziano M, Cavalli R, Guasti D, Calosi L, Ghè C, Solarino R, Thurmond RL, Camussi G, Chazot PL, Rosa AC.

Pharmacol Res. 2018 Feb;128:18-28. doi: 10.1016/j.phrs.2018.01.002. Epub 2018 Jan 6.

PMID:
29309903
6.

Clinical Development of Histamine H4 Receptor Antagonists.

Thurmond RL, Venable J, Savall B, La D, Snook S, Dunford PJ, Edwards JP.

Handb Exp Pharmacol. 2017;241:301-320. doi: 10.1007/164_2016_130. Review.

PMID:
28233185
7.

Behavioural phenotype of histamine H4 receptor knockout mice: Focus on central neuronal functions.

Sanna MD, Ghelardini C, Thurmond RL, Masini E, Galeotti N.

Neuropharmacology. 2017 Mar 1;114:48-57. doi: 10.1016/j.neuropharm.2016.11.023. Epub 2016 Nov 27.

PMID:
27899280
8.

Toreforant, A Histamine H4 Receptor Antagonist, in Patients with Active Rheumatoid Arthritis Despite Methotrexate Therapy: Results of 2 Phase II Studies.

Thurmond RL, Greenspan A, Radziszewski W, Xu XL, Miao Y, Chen B, Ge T, Zhou B, Baker DG, Pavlova D, Ritchlin CT, Tanaka Y, Takeuchi T, Smolen JS.

J Rheumatol. 2016 Sep;43(9):1637-42. doi: 10.3899/jrheum.160164. Epub 2016 Jul 15.

PMID:
27422891
9.

Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy.

Genovese MC, Hsia E, Belkowski SM, Chien C, Masterson T, Thurmond RL, Manthey CL, Yan XD, Ge T, Franks C, Greenspan A.

J Rheumatol. 2015 Oct;42(10):1752-60. doi: 10.3899/jrheum.141580. Epub 2015 Aug 1.

10.

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

Panula P, Chazot PL, Cowart M, Gutzmer R, Leurs R, Liu WL, Stark H, Thurmond RL, Haas HL.

Pharmacol Rev. 2015 Jul;67(3):601-55. doi: 10.1124/pr.114.010249. Review.

11.

Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.

Tichenor MS, Thurmond RL, Venable JD, Savall BM.

J Med Chem. 2015 Sep 24;58(18):7119-27. doi: 10.1021/acs.jmedchem.5b00516. Epub 2015 Jun 3. Review.

PMID:
25993395
12.

The histamine H4 receptor: from orphan to the clinic.

Thurmond RL.

Front Pharmacol. 2015 Mar 31;6:65. doi: 10.3389/fphar.2015.00065. eCollection 2015. Review.

13.

Antihistamines and itch.

Thurmond RL, Kazerouni K, Chaplan SR, Greenspan AJ.

Handb Exp Pharmacol. 2015;226:257-90. doi: 10.1007/978-3-662-44605-8_15. Review.

PMID:
25861785
14.

Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.

Savall BM, Meduna SP, Tays K, Cai H, Thurmond RL, McGovern P, Gaul M, Zhao BP, Edwards JP.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):956-9. doi: 10.1016/j.bmcl.2014.12.027. Epub 2014 Dec 23.

PMID:
25595684
15.

Phase 2a, randomized, double-blind, placebo-controlled, multicenter, parallel-group study of a H4 R-antagonist (JNJ-39758979) in Japanese adults with moderate atopic dermatitis.

Murata Y, Song M, Kikuchi H, Hisamichi K, Xu XL, Greenspan A, Kato M, Chiou CF, Kato T, Guzzo C, Thurmond RL, Ohtsuki M, Furue M.

J Dermatol. 2015 Feb;42(2):129-39. doi: 10.1111/1346-8138.12726. Epub 2014 Dec 9.

PMID:
25491792
16.

The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.

Savall BM, Meduna SP, Venable J, Wei J, Smith RC, Hack MD, Thurmond RL, McGovern P, Edwards JP.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5489-92. doi: 10.1016/j.bmcl.2014.10.013. Epub 2014 Oct 13.

PMID:
25455490
17.

Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment.

Rosa AC, Pini A, Lucarini L, Lanzi C, Veglia E, Thurmond RL, Stark H, Masini E.

J Pharmacol Exp Ther. 2014 Nov;351(2):308-16. doi: 10.1124/jpet.114.215152. Epub 2014 Sep 2.

PMID:
25185215
18.

Peripheral Neuronal Mechanism of Itch: Histamine and Itch.

Thurmond RL, Kazerouni K, Chaplan SR, Greenspan AJ.

In: Carstens E, Akiyama T, editors. Itch: Mechanisms and Treatment. Boca Raton (FL): CRC Press/Taylor & Francis; 2014. Chapter 10.

19.

The histamine H₄ receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects.

Kollmeier A, Francke K, Chen B, Dunford PJ, Greenspan AJ, Xia Y, Xu XL, Zhou B, Thurmond RL.

J Pharmacol Exp Ther. 2014 Jul;350(1):181-7. doi: 10.1124/jpet.114.215749. Epub 2014 May 9.

PMID:
24817035
20.

The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils.

Dib K, Perecko T, Jenei V, McFarlane C, Comer D, Brown V, Katebe M, Scheithauer T, Thurmond RL, Chazot PL, Ennis M.

J Leukoc Biol. 2014 Sep;96(3):411-8. doi: 10.1189/jlb.2AB0813-432RR. Epub 2014 May 5.

21.

Histamine H4-receptors inhibit mast cell renin release in ischemia/reperfusion via protein kinase C ε-dependent aldehyde dehydrogenase type-2 activation.

Aldi S, Takano K, Tomita K, Koda K, Chan NY, Marino A, Salazar-Rodriguez M, Thurmond RL, Levi R.

J Pharmacol Exp Ther. 2014 Jun;349(3):508-17. doi: 10.1124/jpet.114.214122. Epub 2014 Apr 2.

22.

Clinical and preclinical characterization of the histamine H(4) receptor antagonist JNJ-39758979.

Thurmond RL, Chen B, Dunford PJ, Greenspan AJ, Karlsson L, La D, Ward P, Xu XL.

J Pharmacol Exp Ther. 2014 May;349(2):176-84. doi: 10.1124/jpet.113.211714. Epub 2014 Feb 18.

PMID:
24549371
23.

Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.

Savall BM, Chavez F, Tays K, Dunford PJ, Cowden JM, Hack MD, Wolin RL, Thurmond RL, Edwards JP.

J Med Chem. 2014 Mar 27;57(6):2429-39. doi: 10.1021/jm401727m. Epub 2014 Feb 21.

PMID:
24495018
24.

The histamine H4 receptor mediates inflammation and Th17 responses in preclinical models of arthritis.

Cowden JM, Yu F, Banie H, Farahani M, Ling P, Nguyen S, Riley JP, Zhang M, Zhu J, Dunford PJ, Thurmond RL.

Ann Rheum Dis. 2014 Mar;73(3):600-8. doi: 10.1136/annrheumdis-2013-203832. Epub 2013 Oct 14.

25.

Histamine synthesis is required for granule maturation in murine mast cells.

Nakazawa S, Sakanaka M, Furuta K, Natsuhara M, Takano H, Tsuchiya S, Okuno Y, Ohtsu H, Nishibori M, Thurmond RL, Hirasawa N, Nakayama K, Ichikawa A, Sugimoto Y, Tanaka S.

Eur J Immunol. 2014 Jan;44(1):204-14. doi: 10.1002/eji.201343838. Epub 2013 Oct 1.

26.

Antagonism of the histamine H4 receptor reduces LPS-induced TNF production in vivo.

Cowden JM, Yu F, Challapalli M, Huang JF, Kim S, Fung-Leung WP, Ma JY, Riley JP, Zhang M, Dunford PJ, Thurmond RL.

Inflamm Res. 2013 Jun;62(6):599-607. doi: 10.1007/s00011-013-0612-5. Epub 2013 Mar 27.

27.

Histamine down-regulates IL-27 production in antigen-presenting cells.

Gschwandtner M, Bunk H, Köther B, Thurmond RL, Kietzmann M, Werfel T, Bäumer W, Gutzmer R.

J Leukoc Biol. 2012 Jul;92(1):21-9. doi: 10.1189/jlb.0111017. Epub 2012 Mar 2.

PMID:
22389321
28.

Histamine H4 receptor optimizes T regulatory cell frequency and facilitates anti-inflammatory responses within the central nervous system.

del Rio R, Noubade R, Saligrama N, Wall EH, Krementsov DN, Poynter ME, Zachary JF, Thurmond RL, Teuscher C.

J Immunol. 2012 Jan 15;188(2):541-7. doi: 10.4049/jimmunol.1101498. Epub 2011 Dec 5.

29.

Tricyclic aminopyrimidine histamine H4 receptor antagonists.

Savall BM, Gomez L, Chavez F, Curtis M, Meduna SP, Kearney A, Dunford P, Cowden J, Thurmond RL, Grice C, Edwards JP.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6577-81. doi: 10.1016/j.bmcl.2011.08.014. Epub 2011 Aug 19.

PMID:
21920744
30.

Histamine H₄ receptor activation enhances LPS-induced IL-6 production in mast cells via ERK and PI3K activation.

Desai P, Thurmond RL.

Eur J Immunol. 2011 Jun;41(6):1764-73. doi: 10.1002/eji.201040932. Epub 2011 May 25.

31.

Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.

Meduna SP, Savall BM, Cai H, Edwards JP, Thurmond RL, McGovern PM.

Bioorg Med Chem Lett. 2011 May 15;21(10):3113-6. doi: 10.1016/j.bmcl.2011.03.017. Epub 2011 Mar 30.

PMID:
21458260
32.

Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines.

Cowden JM, Riley JP, Ma JY, Thurmond RL, Dunford PJ.

Respir Res. 2010 Jun 24;11:86. doi: 10.1186/1465-9921-11-86.

33.

Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors.

Ameriks MK, Bembenek SD, Burdett MT, Choong IC, Edwards JP, Gebauer D, Gu Y, Karlsson L, Purkey HE, Staker BL, Sun S, Thurmond RL, Zhu J.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4060-4. doi: 10.1016/j.bmcl.2010.05.086. Epub 2010 May 25.

PMID:
20541404
34.

Structural requirements for inverse agonism and neutral antagonism of indole-, benzimidazole-, and thienopyrrole-derived histamine H4 receptor ligands.

Schneider EH, Strasser A, Thurmond RL, Seifert R.

J Pharmacol Exp Ther. 2010 Aug;334(2):513-21. doi: 10.1124/jpet.110.165977. Epub 2010 May 18.

PMID:
20484153
35.

Recent advances in the design of cathepsin S inhibitors.

Wiener JJ, Sun S, Thurmond RL.

Curr Top Med Chem. 2010;10(7):717-32. Review.

PMID:
20337580
36.

Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors.

Wiener DK, Lee-Dutra A, Bembenek S, Nguyen S, Thurmond RL, Sun S, Karlsson L, Grice CA, Jones TK, Edwards JP.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2379-82. doi: 10.1016/j.bmcl.2010.01.103. Epub 2010 Feb 8.

PMID:
20188543
37.

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.

Lee-Dutra A, Wiener DK, Arienti KL, Liu J, Mani N, Ameriks MK, Axe FU, Gebauer D, Desai PJ, Nguyen S, Randal M, Thurmond RL, Sun S, Karlsson L, Edwards JP, Jones TK, Grice CA.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2370-4. doi: 10.1016/j.bmcl.2010.01.108. Epub 2010 Jan 28.

PMID:
20153648
38.

Molecular determinants of ligand binding to H4R species variants.

Lim HD, de Graaf C, Jiang W, Sadek P, McGovern PM, Istyastono EP, Bakker RA, de Esch IJ, Thurmond RL, Leurs R.

Mol Pharmacol. 2010 May;77(5):734-43. doi: 10.1124/mol.109.063040. Epub 2010 Jan 26.

PMID:
20103609
39.

The future antihistamines: histamine H3 and H4 receptor ligands.

Yu F, Bonaventure P, Thurmond RL.

Adv Exp Med Biol. 2010;709:125-40. Review.

PMID:
21618893
40.

Histamine inflammation. Preface.

Thurmond RL.

Adv Exp Med Biol. 2010;709:vii-viii. No abstract available.

PMID:
21618881
41.

Phosphoinositide 3-kinase gamma (PI3Kgamma) inhibitors for the treatment of inflammation and autoimmune disease.

Venable JD, Ameriks MK, Blevitt JM, Thurmond RL, Fung-Leung WP.

Recent Pat Inflamm Allergy Drug Discov. 2010 Jan;4(1):1-15. Review.

PMID:
20017720
42.

The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation.

Cowden JM, Zhang M, Dunford PJ, Thurmond RL.

J Invest Dermatol. 2010 Apr;130(4):1023-33. doi: 10.1038/jid.2009.358. Epub 2009 Nov 12.

43.

Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency.

Ameriks MK, Cai H, Edwards JP, Gebauer D, Gleason E, Gu Y, Karlsson L, Nguyen S, Sun S, Thurmond RL, Zhu J.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6135-9. doi: 10.1016/j.bmcl.2009.09.013. Epub 2009 Sep 10.

PMID:
19783435
44.

Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements.

Ameriks MK, Axe FU, Bembenek SD, Edwards JP, Gu Y, Karlsson L, Randal M, Sun S, Thurmond RL, Zhu J.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6131-4. doi: 10.1016/j.bmcl.2009.09.014. Epub 2009 Sep 10.

PMID:
19773165
45.

A selective H4R antagonist prevents antigen-induced asthma-like reaction and airway inflammation in guinea pigs.

Masini E, Ragazzo E, Vinci MC, Nistri S, Cinci L, Mastroianni R, Thurmond RL, Salvemini D.

Inflamm Res. 2009 Apr;58 Suppl 1:9-10. doi: 10.1007/s00011-009-0643-0. No abstract available.

PMID:
19274434
46.

The histamine H4 receptor antagonist JNJ7777120 induces increases in the histamine content of the rat conjunctiva.

Zampeli E, Thurmond RL, Tiligada E.

Inflamm Res. 2009 Jun;58(6):285-91. doi: 10.1007/s00011-009-8245-4.

PMID:
19184344
47.

Cutting edge: histamine receptor H4 activation positively regulates in vivo IL-4 and IFN-gamma production by invariant NKT cells.

Leite-de-Moraes MC, Diem S, Michel ML, Ohtsu H, Thurmond RL, Schneider E, Dy M.

J Immunol. 2009 Feb 1;182(3):1233-6.

48.

Cloning and pharmacological characterization of the dog histamine H4 receptor.

Jiang W, Lim HD, Zhang M, Desai P, Dai H, Colling PM, Leurs R, Thurmond RL.

Eur J Pharmacol. 2008 Sep 11;592(1-3):26-32. doi: 10.1016/j.ejphar.2008.06.095. Epub 2008 Jul 2.

PMID:
18639542
49.

The new biology of histamine receptors.

Huang JF, Thurmond RL.

Curr Allergy Asthma Rep. 2008 Mar;8(1):21-7. Review.

PMID:
18377770
50.

The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines.

Thurmond RL, Gelfand EW, Dunford PJ.

Nat Rev Drug Discov. 2008 Jan;7(1):41-53. doi: 10.1038/nrd2465. Review.

PMID:
18172439

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