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Items: 1 to 50 of 88

1.

B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor.

Post-Munson DJ, Pieschl RL, Molski TF, Graef JD, Hendricson AW, Knox RJ, McDonald IM, Olson RE, Macor JE, Weed MR, Bristow LJ, Kiss L, Ahlijanian MK, Herrington J.

Eur J Pharmacol. 2017 Mar 15;799:16-25. doi: 10.1016/j.ejphar.2017.01.037. Epub 2017 Jan 26.

PMID:
28132910
2.

Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.

Ahuja VT, Hartz RA, Molski TF, Mattson GK, Lentz KA, Grace JE Jr, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 May 1;26(9):2184-7. doi: 10.1016/j.bmcl.2016.03.067. Epub 2016 Mar 17.

PMID:
27020524
3.

Biochemical and behavioral effects of PDE10A inhibitors: Relationship to target site occupancy.

Li YW, Seager MA, Wojcik T, Heman K, Molski TF, Fernandes A, Langdon S, Pendri A, Gerritz S, Tian Y, Hong Y, Gallagher L, Merritt JR, Zhang C, Westphal R, Zaczek R, Macor JE, Bronson JJ, Lodge NJ.

Neuropharmacology. 2016 Mar;102:121-35. doi: 10.1016/j.neuropharm.2015.10.037. Epub 2015 Oct 30.

PMID:
26522433
4.

Discovery of D1 Dopamine Receptor Positive Allosteric Modulators: Characterization of Pharmacology and Identification of Residues that Regulate Species Selectivity.

Lewis MA, Hunihan L, Watson J, Gentles RG, Hu S, Huang Y, Bronson J, Macor JE, Beno BR, Ferrante M, Hendricson A, Knox RJ, Molski TF, Kong Y, Cvijic ME, Rockwell KL, Weed MR, Cacace AM, Westphal RS, Alt A, Brown JM.

J Pharmacol Exp Ther. 2015 Sep;354(3):340-9. doi: 10.1124/jpet.115.224071. Epub 2015 Jun 24.

5.

Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.

Lodge NJ, Li YW, Chin FT, Dischino DD, Zoghbi SS, Deskus JA, Mattson RJ, Imaizumi M, Pieschl R, Molski TF, Fujita M, Dulac H, Zaczek R, Bronson JJ, Macor JE, Innis RB, Pike VW.

Nucl Med Biol. 2014 Jul;41(6):524-35. doi: 10.1016/j.nucmedbio.2014.03.005. Epub 2014 Mar 29.

6.

NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.

Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ.

Neuropharmacology. 2013 Oct;73:232-40. doi: 10.1016/j.neuropharm.2013.05.038. Epub 2013 Jun 12.

PMID:
23770339
7.

Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.

Ditta JL, Denhart DJ, Deskus JA, Epperson JR, Meng Z, Gao Q, Mattson GK, Lapaglia MA, Taber MT, Molski TF, Lodge NJ, Mattson RJ, Macor JE.

Bioorg Med Chem Lett. 2013 May 15;23(10):2948-50. doi: 10.1016/j.bmcl.2013.03.045. Epub 2013 Mar 26.

PMID:
23578689
8.

[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.

Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA, Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7.

PMID:
23010264
9.

Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.

Dzierba CD, Sielecki TM, Arvanitis AG, Galka A, Johnson TL, Takvorian AG, Rafalski M, Kasireddy-Polam P, Vig S, Dasgupta B, Zhang G, Molski TF, Wong H, Zaczek RC, Lodge NJ, Combs AP, Gilligan PJ, Trainor GL, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4986-9. doi: 10.1016/j.bmcl.2012.06.034. Epub 2012 Jun 16.

PMID:
22749422
10.

Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.

King HD, Meng Z, Deskus JA, Sloan CP, Gao Q, Beno BR, Kozlowski ES, Lapaglia MA, Mattson GK, Molski TF, Taber MT, Lodge NJ, Mattson RJ, Macor JE.

J Med Chem. 2010 Nov 11;53(21):7564-72. doi: 10.1021/jm100515z.

PMID:
20949929
11.

5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.

Schmitz WD, Brenner AB, Bronson JJ, Ditta JL, Griffin CR, Li YW, Lodge NJ, Molski TF, Olson RE, Zhuo X, Macor JE.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3579-83. doi: 10.1016/j.bmcl.2010.04.121. Epub 2010 May 17.

PMID:
20483614
12.

Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Schmitz WD, Molski TF, Mattson GK, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1890-4. doi: 10.1016/j.bmcl.2010.01.129. Epub 2010 Feb 1.

PMID:
20176478
13.

Synthesis and hSERT activity of homotryptamine analogs. Part 6: [3+2] dipolar cycloaddition of 3-vinylindoles.

Marcin LR, Mattson RJ, Gao Q, Wu D, Molski TF, Mattson GK, Lodge NJ.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1027-30. doi: 10.1016/j.bmcl.2009.12.043. Epub 2009 Dec 16.

PMID:
20034793
14.

A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.

Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ.

J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v.

PMID:
19954247
15.

Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors.

Denhart DJ, Deskus JA, Ditta JL, Gao Q, Dalton King H, Kozlowski ES, Meng Z, LaPaglia MA, Mattson GK, Molski TF, Taber MT, Lodge NJ, Mattson RJ, Macor JE.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4031-3. doi: 10.1016/j.bmcl.2009.06.026. Epub 2009 Jun 13.

PMID:
19560923
16.

Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y.

PMID:
19552437
17.

In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19552436
18.

Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.

Dalton King H, Denhart DJ, Deskus JA, Ditta JL, Epperson JR, Higgins MA, Kung JE, Marcin LR, Sloan CP, Mattson GK, Molski TF, Krause RG, Bertekap RL Jr, Lodge NJ, Mattson RJ, Macor JE.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5647-51. Epub 2007 Aug 22.

PMID:
17766113
19.

Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.

Dzierba CD, Tebben AJ, Wilde RG, Takvorian AG, Rafalski M, Kasireddy-Polam P, Klaczkiewicz JD, Pechulis AD, Davis AL, Sweet MP, Woo AM, Yang Z, Ebeltoft SM, Molski TF, Zhang G, Zaczek RC, Trainor GL, Combs AP, Gilligan PJ.

J Med Chem. 2007 May 3;50(9):2269-72. Epub 2007 Apr 3.

PMID:
17402721
20.

Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.

Deskus JA, Epperson JR, Sloan CP, Cipollina JA, Dextraze P, Qian-Cutrone J, Gao Q, Ma B, Beno BR, Mattson GK, Molski TF, Krause RG, Taber MT, Lodge NJ, Mattson RJ.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3099-104. Epub 2007 Mar 16.

PMID:
17391962
21.

Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies.

Stark AD, Jordan S, Allers KA, Bertekap RL, Chen R, Mistry Kannan T, Molski TF, Yocca FD, Sharp T, Kikuchi T, Burris KD.

Psychopharmacology (Berl). 2007 Feb;190(3):373-82. Epub 2006 Nov 25.

PMID:
17242925
22.

Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.

Mattson RJ, Catt JD, Denhart DJ, Deskus JA, Ditta JL, Higgins MA, Marcin LR, Sloan CP, Beno BR, Gao Q, Cunningham MA, Mattson GK, Molski TF, Taber MT, Lodge NJ.

J Med Chem. 2005 Sep 22;48(19):6023-34.

PMID:
16162005
23.

Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).

Schmitz WD, Denhart DJ, Brenner AB, Ditta JL, Mattson RJ, Mattson GK, Molski TF, Macor JE.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1619-21.

PMID:
15745809
24.

Neurochemical, pharmacokinetic, and behavioral effects of the novel selective serotonin reuptake inhibitor BMS-505130.

Taber MT, Wright RN, Molski TF, Clarke WJ, Brassil PJ, Denhart DJ, Mattson RJ, Lodge NJ.

Pharmacol Biochem Behav. 2005 Mar;80(3):521-8.

PMID:
15740795
25.

Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.

Dzierba CD, Takvorian AG, Rafalski M, Kasireddy-Polam P, Wong H, Molski TF, Zhang G, Li YW, Lelas S, Peng Y, McElroy JF, Zaczek RC, Taub RA, Combs AP, Gilligan PJ, Trainor GL.

J Med Chem. 2004 Nov 4;47(23):5783-90.

PMID:
15509177
26.

Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.

Hartz RA, Nanda KK, Ingalls CL, Ahuja VT, Molski TF, Zhang G, Wong H, Peng Y, Kelley M, Lodge NJ, Zaczek R, Gilligan PJ, Trainor GL.

J Med Chem. 2004 Sep 9;47(19):4741-54.

PMID:
15341489
27.

Synthesis and SAR exploration of dinapsoline analogues.

Sit SY, Xie K, Jacutin-Porte S, Boy KM, Seanz J, Taber MT, Gulwadi AG, Korpinen CD, Burris KD, Molski TF, Ryan E, Xu C, Verdoorn T, Johnson G, Nichols DE, Mailman RB.

Bioorg Med Chem. 2004 Feb 15;12(4):715-34.

PMID:
14759732
28.

(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.

Sit SY, Xie K, Jacutin-Porte S, Taber MT, Gulwadi AG, Korpinen CD, Burris KD, Molski TF, Ryan E, Xu C, Wong H, Zhu J, Krishnananthan S, Gao Q, Verdoorn T, Johnson G.

J Med Chem. 2002 Aug 15;45(17):3660-8.

PMID:
12166939
29.

Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors.

Burris KD, Molski TF, Xu C, Ryan E, Tottori K, Kikuchi T, Yocca FD, Molinoff PB.

J Pharmacol Exp Ther. 2002 Jul;302(1):381-9.

30.

Phosphorylation of cytosolic phospholipase A2 and the release of arachidonic acid in human neutrophils.

Syrbu SI, Waterman WH, Molski TF, Nagarkatti D, Hajjar JJ, Sha'afi RI.

J Immunol. 1999 Feb 15;162(4):2334-40.

32.
33.

Stimulation of intestinal Na+/H+ exchange by cell volume changes during fasting and refeeding in rats.

Hajjar JJ, Aziz W, Molski TF, Sha'afi RI.

Proc Soc Exp Biol Med. 1995 Sep;209(4):354-9.

PMID:
7638242
34.

Effect of lipopolysaccharide on mitogen-activated protein kinases and cytosolic phospholipase A2.

Fouda SI, Molski TF, Ashour MS, Sha'afi RI.

Biochem J. 1995 Jun 15;308 ( Pt 3):815-22.

35.
37.

Phorbol ester inhibits granulocyte-macrophage colony-stimulating factor binding and tyrosine phosphorylation.

Gomez-Cambronero J, Huang CK, Yamazaki M, Wang E, Molski TF, Becker EL, Sha'afi RI.

Am J Physiol. 1992 Feb;262(2 Pt 1):C276-81.

PMID:
1539618
38.

Modulation of leukotriene B4 and platelet-activating factor binding to neutrophils.

Yamazaki M, Molski TF, Stevens T, Huang CK, Becker EL, Sha'afi RI.

Am J Physiol. 1991 Sep;261(3 Pt 1):C515-20.

PMID:
1653524
39.

Role of ion movements in neutrophil activation.

Sha'afi RI, Molski TF.

Annu Rev Physiol. 1990;52:365-79. Review. No abstract available.

PMID:
2184760
40.
41.

Phorbol 12-myristate 13-acetate inhibits binding of leukotriene B4 and platelet-activating factor and the responses they induce in neutrophils: site of action.

Yamazaki M, Gomez-Cambronero J, Durstin M, Molski TF, Becker EL, Sha'afi RI.

Proc Natl Acad Sci U S A. 1989 Aug;86(15):5791-4.

42.
43.

Granulocyte-macrophage colony-stimulating factor and human neutrophils: role of guanine nucleotide regulatory proteins.

Gomez-Cambronero J, Yamazaki M, Metwally F, Molski TF, Bonak VA, Huang CK, Becker EL, Sha'afi RI.

Proc Natl Acad Sci U S A. 1989 May;86(10):3569-73.

44.

Characterization of the membrane-associated GTPase activity: effects of chemotactic factors and toxins.

Pelz C, Matsumoto T, Molski TF, Becker EL, Sha'afi RI.

J Cell Biochem. 1989 Feb;39(2):197-206.

PMID:
2541143
45.

Arachidonic acid release in rabbit neutrophils.

Tao W, Molski TF, Sha'afi RI.

Biochem J. 1989 Feb 1;257(3):633-7.

46.

Actions of the protease inhibitor phenylmethylsulfonyl fluoride on neutrophil granule enzyme secretion and superoxide production induced by fMet-Leu-Phe and phorbol 12-myristate-13-acetate.

Gomez-Cambronero J, Mege JL, Molski TF, Naccache PH, Becker EL, Sha'afi RI.

Int Arch Allergy Appl Immunol. 1989;89(4):362-8.

PMID:
2551825
47.

Diacylglycerol kinase inhibitor R59022 and stimulated neutrophil responses.

Mege JL, Tao W, Molski TF, Gomez-Cambronero J, Huang CK, Becker EL, Sha'afi RI.

Am J Physiol. 1988 Nov;255(5 Pt 1):C589-94.

PMID:
2847534
48.

Effect of cholera toxin on histamine release from bone marrow-derived mouse mast cells.

Saito H, Okajima F, Molski TF, Sha'afi RI, Ui M, Ishizaka T.

Proc Natl Acad Sci U S A. 1988 Apr;85(8):2504-8.

49.
50.

Activation of the neutrophil.

Sha'afi RI, Molski TF.

Prog Allergy. 1988;42:1-64. Review. No abstract available.

PMID:
3140244

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