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Items: 31

1.

The Selective Sphingosine 1-Phosphate Receptor Modulator Etrasimod Regulates Lymphocyte Trafficking and Alleviates Experimental Colitis.

Al-Shamma H, Lehmann-Bruinsma K, Carroll C, Solomon M, Komori HK, Peyrin-Biroulet L, Adams J.

J Pharmacol Exp Ther. 2019 Jun;369(3):311-317. doi: 10.1124/jpet.118.254268. Epub 2019 Mar 14.

PMID:
30872391
2.

Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain.

Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH, Barden J, Sadeque A, Usmani A, Chen C, Semple G, Grottick AJ, Al-Shamma H, Christopher R, Jones RM.

ACS Med Chem Lett. 2017 Nov 30;8(12):1309-1313. doi: 10.1021/acsmedchemlett.7b00396. eCollection 2017 Dec 14.

3.

(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.

Buzard DJ, Lopez L, Moody J, Kawasaki A, Schrader TO, Kasem M, Johnson B, Zhu X, Thoresen L, Kim SH, Gharbaoui T, Sengupta D, Calvano L, Krishnan A, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Usmani K, Chen C, Sadeque A, Chen W, Christopher RJ, Thatte J, Fu L, Solomon M, Whelan K, Al-Shamma H, Gatlin J, Gaidarov I, Anthony T, Le M, Unett DJ, Stirn S, Blackburn A, Behan DP, Jones RM.

ACS Med Chem Lett. 2014 Nov 25;5(12):1334-9. doi: 10.1021/ml500422m. eCollection 2014 Dec 11.

4.

Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.

Buzard DJ, Kim SH, Lopez L, Kawasaki A, Zhu X, Moody J, Thoresen L, Calderon I, Ullman B, Han S, Lehmann J, Gharbaoui T, Sengupta D, Calvano L, Montalban AG, Ma YA, Sage C, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Chen W, Usmani K, Chen C, Sadeque A, Christopher RJ, Thatte J, Fu L, Solomon M, Mills D, Whelan K, Al-Shamma H, Gatlin J, Le M, Gaidarov I, Anthony T, Unett DJ, Blackburn A, Rueter J, Stirn S, Behan DP, Jones RM.

ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7. doi: 10.1021/ml500389m. eCollection 2014 Dec 11.

5.

Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.

Han S, Thoresen L, Zhu X, Narayanan S, Jung JK, Strah-Pleynet S, Decaire M, Choi K, Xiong Y, Yue D, Semple G, Thatte J, Solomon M, Fu L, Whelan K, Al-Shamma H, Gatlin J, Chen R, Dang H, Pride C, Gaidarov I, Unett DJ, Behan DP, Sadeque A, Usmani KA, Chen C, Edwards J, Morgan M, Jones RM.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):322-6. doi: 10.1016/j.bmcl.2014.11.040. Epub 2014 Nov 26.

PMID:
25488844
6.

Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists.

Buzard DJ, Kim SH, Lehmann J, Han S, Calderon I, Wong A, Kawasaki A, Narayanan S, Bhat R, Gharbaoui T, Lopez L, Yue D, Whelan K, Al-Shamma H, Unett DJ, Shu HH, Tung SF, Chang S, Chuang CF, Morgan M, Sadeque A, Chu ZL, Leonard JN, Jones RM.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-5. doi: 10.1016/j.bmcl.2014.06.071. Epub 2014 Jul 3.

PMID:
25088191
7.

Fused tricyclic indoles as S1P₁ agonists with robust efficacy in animal models of autoimmune disease.

Buzard DJ, Han S, Lopez L, Kawasaki A, Moody J, Thoresen L, Ullman B, Lehmann J, Calderon I, Zhu X, Gharbaoui T, Sengupta D, Krishnan A, Gao Y, Edwards J, Barden J, Morgan M, Usmani K, Chen C, Sadeque A, Thatte J, Solomon M, Fu L, Whelan K, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4404-9. doi: 10.1016/j.bmcl.2012.04.129. Epub 2012 May 7.

PMID:
22633692
8.

Diet-induced models of obesity (DIO) in rodents.

Bagnol D, Al-Shamma HA, Behan D, Whelan K, Grottick AJ.

Curr Protoc Neurosci. 2012 Apr;Chapter 9:Unit 9.38.1-13. doi: 10.1002/0471142301.ns0938s59.

PMID:
22470151
9.

Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.

Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Feichtinger K, Frazer JM, Yoon WH, Whelan K, Sanabria EK, Grottick AJ, Al-Shamma H, Semple G.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1870-3. doi: 10.1016/j.bmcl.2012.01.080. Epub 2012 Jan 28.

PMID:
22325948
10.

Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.

Semple G, Lehmann J, Wong A, Ren A, Bruce M, Shin YJ, Sage CR, Morgan M, Chen WC, Sebring K, Chu ZL, Leonard JN, Al-Shamma H, Grottick AJ, Du F, Liang Y, Demarest K, Jones RM.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5. doi: 10.1016/j.bmcl.2011.12.092. Epub 2011 Dec 30.

PMID:
22264481
11.

Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P₁ agonists.

Buzard D, Han S, Thoresen L, Moody J, Lopez L, Kawasaki A, Schrader T, Sage C, Gao Y, Edwards J, Barden J, Thatte J, Fu L, Solomon M, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):6013-8. doi: 10.1016/j.bmcl.2011.05.110. Epub 2011 Jun 6.

PMID:
21852130
12.

Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.

Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM.

Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13.

PMID:
21444206
13.

Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.

Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Dosa PI, Feichtinger K, Teegarden BR, Frazer JM, Yoon WH, Shan Y, Whelan K, Hauser EK, Grottick AJ, Semple G, Al-Shamma H.

J Med Chem. 2010 Aug 12;53(15):5696-706. doi: 10.1021/jm100479q.

PMID:
20684606
14.

Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.

Xiong Y, Teegarden BR, Choi JS, Strah-Pleynet S, Decaire M, Jayakumar H, Dosa PI, Casper MD, Pham L, Feichtinger K, Ullman B, Adams J, Yuskin D, Frazer J, Morgan M, Sadeque A, Chen W, Webb RR, Connolly DT, Semple G, Al-Shamma H.

J Med Chem. 2010 Jun 10;53(11):4412-21. doi: 10.1021/jm100044a.

PMID:
20455563
15.

Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia.

Teegarden BR, Li H, Jayakumar H, Strah-Pleynet S, Dosa PI, Selaya SD, Kato N, Elwell KH, Davidson J, Cheng K, Saldana H, Frazer JM, Whelan K, Foster J, Espitia S, Webb RR, Beeley NR, Thomsen W, Morairty SR, Kilduff TS, Al-Shamma HA.

J Med Chem. 2010 Mar 11;53(5):1923-36. doi: 10.1021/jm9007328.

PMID:
20143782
16.

Targeted inhibition of the serotonin 5HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis.

Przyklenk K, Frelinger AL 3rd, Linden MD, Whittaker P, Li Y, Barnard MR, Adams J, Morgan M, Al-Shamma H, Michelson AD.

J Thromb Haemost. 2010 Feb;8(2):331-40. doi: 10.1111/j.1538-7836.2009.03693.x. Epub 2009 Nov 17.

17.

Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia.

Al-Shamma HA, Anderson C, Chuang E, Luthringer R, Grottick AJ, Hauser E, Morgan M, Shanahan W, Teegarden BR, Thomsen WJ, Behan D.

J Pharmacol Exp Ther. 2010 Jan;332(1):281-90. doi: 10.1124/jpet.109.160994. Epub 2009 Oct 19.

PMID:
19841476
18.

APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology.

Adams JW, Ramirez J, Shi Y, Thomsen W, Frazer J, Morgan M, Edwards JE, Chen W, Teegarden BR, Xiong Y, Al-Shamma H, Behan DP, Connolly DT.

J Pharmacol Exp Ther. 2009 Oct;331(1):96-103. doi: 10.1124/jpet.109.153189. Epub 2009 Jul 23.

PMID:
19628629
19.

5-HT(2A) inverse-agonists for the treatment of insomnia.

Teegarden BR, Al Shamma H, Xiong Y.

Curr Top Med Chem. 2008;8(11):969-76.

PMID:
18673166
20.

Anti-thrombotic and vascular effects of AR246686, a novel 5-HT2A receptor antagonist.

Adams JW, Ramirez J, Ortuno D, Shi Y, Thomsen W, Richman JG, Morgan M, Dosa P, Teegarden BR, Al-Shamma H, Behan DP, Connolly DT.

Eur J Pharmacol. 2008 May 31;586(1-3):234-43. doi: 10.1016/j.ejphar.2007.11.056. Epub 2007 Dec 3.

PMID:
18358471
21.

Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization.

Thomsen WJ, Grottick AJ, Menzaghi F, Reyes-Saldana H, Espitia S, Yuskin D, Whelan K, Martin M, Morgan M, Chen W, Al-Shamma H, Smith B, Chalmers D, Behan D.

J Pharmacol Exp Ther. 2008 May;325(2):577-87. doi: 10.1124/jpet.107.133348. Epub 2008 Feb 5.

PMID:
18252809
22.

G protein-coupled receptors as therapeutic targets for obesity and type 2 diabetes.

Bjenning C, Al-Shamma H, Thomsen W, Leonard J, Behan D.

Curr Opin Investig Drugs. 2004 Oct;5(10):1051-62. Review.

PMID:
15535426
23.

Apoptosis induction and potent antiestrogen receptor-negative breast cancer activity in vivo by a retinoid antagonist.

Fanjul AN, Piedrafita FJ, Al-Shamma H, Pfahl M.

Cancer Res. 1998 Oct 15;58(20):4607-10.

24.

Brain-derived neurotrophic factor regulates expression of androgen receptors in perineal motoneurons.

Al-Shamma HA, Arnold AP.

Proc Natl Acad Sci U S A. 1997 Feb 18;94(4):1521-6.

26.
27.

The sexually dimorphic vasopressin innervation of the brain as a model for steroid modulation of neuropeptide transmission.

De Vries GJ, al-Shamma HA, Zhou L.

Ann N Y Acad Sci. 1994 Nov 14;743:95-120. Review. No abstract available.

PMID:
7802421
28.
29.

Gonadal steroid modulation of vasopressin pathways.

De Vries GJ, Crenshaw BJ, al-Shamma HA.

Ann N Y Acad Sci. 1992 Jun 12;652:387-96. Review. No abstract available.

PMID:
1626838
31.

Sex differences in hormonal responses of vasopressin pathways in the rat brain.

De Vries GJ, al-Shamma HA.

J Neurobiol. 1990 Jul;21(5):686-93.

PMID:
2394985

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