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Items: 32

1.

eIF2B activator prevents neurological defects caused by a chronic integrated stress response.

Wong YL, LeBon L, Basso AM, Kohlhaas KL, Nikkel AL, Robb HM, Donnelly-Roberts DL, Prakash J, Swensen AM, Rubinstein ND, Krishnan S, McAllister FE, Haste NV, O'Brien JJ, Roy M, Ireland A, Frost JM, Shi L, Riedmaier S, Martin K, Dart MJ, Sidrauski C.

Elife. 2019 Jan 9;8. pii: e42940. doi: 10.7554/eLife.42940.

2.

Identification and Characterization of Novel CFTR Potentiators.

Gees M, Musch S, Van der Plas S, Wesse AS, Vandevelde A, Verdonck K, Mammoliti O, Hwang TC, Sonck K, Stouten P, Swensen AM, Jans M, Van der Schueren J, Nelles L, Andrews M, Conrath K.

Front Pharmacol. 2018 Oct 26;9:1221. doi: 10.3389/fphar.2018.01221. eCollection 2018.

3.

Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis.

Wang X, Liu B, Searle X, Yeung C, Bogdan A, Greszler S, Singh A, Fan Y, Swensen AM, Vortherms T, Balut C, Jia Y, Desino K, Gao W, Yong H, Tse C, Kym P.

J Med Chem. 2018 Feb 22;61(4):1436-1449. doi: 10.1021/acs.jmedchem.7b01339. Epub 2018 Jan 5.

PMID:
29251932
4.

Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.

Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24.

PMID:
27839686
5.

Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.

Tang H, Zhu Y, Teumelsan N, Walsh SP, Shahripour A, Priest BT, Swensen AM, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Pai LY, Hampton C, Corona A, Hernandez M, Metzger J, Forrest M, Zhou X, Owens K, Tong V, Parmee E, Roy S, Kaczorowski GJ, Yang L, Alonso-Galicia M, Garcia ML, Pasternak A.

ACS Med Chem Lett. 2016 May 12;7(7):697-701. doi: 10.1021/acsmedchemlett.6b00122. eCollection 2016 Jul 14.

6.

Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.

Walsh SP, Shahripour A, Tang H, de Jesus RK, Teumelsan N, Zhu Y, Frie J, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A.

Bioorg Med Chem Lett. 2016 May 1;26(9):2339-43. doi: 10.1016/j.bmcl.2016.03.035. Epub 2016 Mar 12.

PMID:
27017115
7.

Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.

Walsh SP, Shahripour A, Tang H, Teumelsan N, Frie J, Zhu Y, Priest BT, Swensen AM, Liu J, Margulis M, Visconti R, Weinglass A, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Alonso-Galicia M, Zhou X, Pai LY, Corona A, Hampton C, Hernandez M, Bentley R, Chen J, Shah K, Metzger J, Forrest M, Owens K, Tong V, Ha S, Roy S, Kaczorowski GJ, Yang L, Parmee E, Garcia ML, Sullivan K, Pasternak A.

ACS Med Chem Lett. 2015 May 7;6(7):747-52. doi: 10.1021/ml500440u. eCollection 2015 Jul 9.

8.

Characterization of the triazine, T4, a representative from a novel series of CaV2 inhibitors with strong state-dependence, poor use-dependence, and distinctively fast kinetics.

Swensen AM, Niforatos W, Lee CH, Jarvis MF, McGaraughty S.

Eur J Pharmacol. 2014 Dec 15;745:234-42. doi: 10.1016/j.ejphar.2014.10.037. Epub 2014 Oct 30.

PMID:
25446431
9.

Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.

Shao PP, Ye F, Chakravarty PK, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL.

ACS Med Chem Lett. 2013 Sep 8;4(11):1064-8. doi: 10.1021/ml4002612. eCollection 2013 Nov 14.

10.

Mechanistic insights into the analgesic efficacy of A-1264087, a novel neuronal Ca(2+) channel blocker that reduces nociception in rat preclinical pain models.

Zhu CZ, Vortherms TA, Zhang M, Xu J, Swensen AM, Niforatos W, Neelands T, Milicic I, Lewis LG, Zhong C, Gauvin D, Mikusa J, Zhan C, Pai M, Roderwald V, Chu KL, Cole EE, Bespalov A, Searle XB, McGaraughty S, Bitner RS, Jarvis MF, Bannon AW, Joshi SK, Scott VE, Lee CH.

J Pain. 2014 Apr;15(4):387.e1-14. doi: 10.1016/j.jpain.2013.12.002. Epub 2013 Dec 25.

PMID:
24374196
11.

Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl)ethyl)isobenzofuran-1(3H)-one.

Tang H, de Jesus RK, Walsh SP, Zhu Y, Yan Y, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5829-32. doi: 10.1016/j.bmcl.2013.08.104. Epub 2013 Sep 6.

PMID:
24075732
12.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.

Beebe X, Yeung CM, Darczak D, Shekhar S, Vortherms TA, Miller L, Milicic I, Swensen AM, Zhu CZ, Banfor P, Wetter JM, Marsh KC, Jarvis MF, Scott VE, Schrimpf MR, Lee CH.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074. Epub 2013 Jul 4.

PMID:
23876987
13.

Establishment of a secondary screening assay for P/Q-type calcium channel blockers.

Hermann D, Mezler M, Swensen AM, Bruehl C, Obergru├čerger A, Wicke K, Schoemaker H, Gross G, Draguhn A, Nimmrich V.

Comb Chem High Throughput Screen. 2013 Mar;16(3):233-43.

PMID:
23228050
14.

Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.

Shao PP, Ye F, Chakravarty PK, Varughese DJ, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL.

J Med Chem. 2012 Nov 26;55(22):9847-55. doi: 10.1021/jm301056k. Epub 2012 Nov 12.

PMID:
23098566
15.

An automated electrophysiological assay for differentiating Ca(v)2.2 inhibitors based on state dependence and kinetics.

Swensen AM, Niforatos W, Vortherms TA, Perner RJ, Li T, Schrimpf MR, Scott VE, Lee L, Jarvis MF, McGaraughty S.

Assay Drug Dev Technol. 2012 Dec;10(6):542-50. doi: 10.1089/adt.2011.437. Epub 2012 Mar 19.

PMID:
22428804
16.

Development and validation of a fluorescence-based HTS assay for the identification of P/Q-type calcium channel blockers.

Mezler M, Hermann D, Swensen AM, Draguhn A, Terstappen GC, Gross G, Schoemaker H, Freiberg G, Pratt S, Gopalakrishnan SM, Nimmrich V.

Comb Chem High Throughput Screen. 2012 Jun 1;15(5):372-85.

PMID:
22272661
17.

Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels.

Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, Smith MM, Warren VA, Arneric SP, Eduljee C, Parker D, Snutch TP, Hoyt SB, London C, Duffy JL, Kaczorowski GJ, McManus OB.

Mol Pharmacol. 2012 Mar;81(3):488-97. doi: 10.1124/mol.111.075226. Epub 2011 Dec 21.

PMID:
22188924
18.

A-1048400 is a novel, orally active, state-dependent neuronal calcium channel blocker that produces dose-dependent antinociception without altering hemodynamic function in rats.

Scott VE, Vortherms TA, Niforatos W, Swensen AM, Neelands T, Milicic I, Banfor PN, King A, Zhong C, Simler G, Zhan C, Bratcher N, Boyce-Rustay JM, Zhu CZ, Bhatia P, Doherty G, Mack H, Stewart AO, Jarvis MF.

Biochem Pharmacol. 2012 Feb 1;83(3):406-18. doi: 10.1016/j.bcp.2011.10.019. Epub 2011 Nov 16.

PMID:
22153861
19.

Comparative analysis of inactivated-state block of N-type (Ca(v)2.2) calcium channels.

Vortherms TA, Swensen AM, Niforatos W, Limberis JT, Neelands TR, Janis RS, Thimmapaya R, Donnelly-Roberts DL, Namovic MT, Zhang D, Brent Putman C, Martin RL, Surowy CS, Jarvis MF, Scott VE.

Inflamm Res. 2011 Jul;60(7):683-93. doi: 10.1007/s00011-011-0322-9. Epub 2011 Mar 11.

PMID:
21394563
20.

A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.

Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21.

PMID:
21195616
21.

A pharmacologically validated, high-capacity, functional thallium flux assay for the human Ether-à-go-go related gene potassium channel.

Schmalhofer WA, Swensen AM, Thomas BS, Felix JP, Haedo RJ, Solly K, Kiss L, Kaczorowski GJ, Garcia ML.

Assay Drug Dev Technol. 2010 Dec;8(6):714-26. doi: 10.1089/adt.2010.0351.

PMID:
21158686
22.

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker.

Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL.

J Pharmacol Exp Ther. 2010 Aug;334(2):545-55. doi: 10.1124/jpet.110.166363. Epub 2010 May 3.

PMID:
20439438
23.

A high-capacity membrane potential FRET-based assay for the sodium-coupled glucose co-transporter SGLT1.

Weinglass AB, Swensen AM, Liu J, Schmalhofer W, Thomas A, Williams B, Ross L, Hashizume K, Kohler M, Kaczorowski GJ, Garcia ML.

Assay Drug Dev Technol. 2008 Apr;6(2):255-62. doi: 10.1089/adt.2008.125.

PMID:
18471079
24.

A high-throughput assay for evaluating state dependence and subtype selectivity of Cav2 calcium channel inhibitors.

Dai G, Haedo RJ, Warren VA, Ratliff KS, Bugianesi RM, Rush A, Williams ME, Herrington J, Smith MM, McManus OB, Swensen AM.

Assay Drug Dev Technol. 2008 Apr;6(2):195-212. doi: 10.1089/adt.2008.136.

PMID:
18471074
25.

Novel CaV2.1 clone replicates many properties of Purkinje cell CaV2.1 current.

Richards KS, Swensen AM, Lipscombe D, Bommert K.

Eur J Neurosci. 2007 Nov;26(10):2950-61.

PMID:
18001290
26.

Automated electrophysiology in drug discovery.

Priest BT, Swensen AM, McManus OB.

Curr Pharm Des. 2007;13(23):2325-37. Review.

PMID:
17692004
28.

Ionic mechanisms of burst firing in dissociated Purkinje neurons.

Swensen AM, Bean BP.

J Neurosci. 2003 Oct 22;23(29):9650-63.

29.

Modulators with convergent cellular actions elicit distinct circuit outputs.

Swensen AM, Marder E.

J Neurosci. 2001 Jun 1;21(11):4050-8.

30.

The roles of co-transmission in neural network modulation.

Nusbaum MP, Blitz DM, Swensen AM, Wood D, Marder E.

Trends Neurosci. 2001 Mar;24(3):146-54. Review.

PMID:
11182454
31.
32.

GABA and responses to GABA in the stomatogastric ganglion of the crab Cancer borealis.

Swensen AM, Golowasch J, Christie AE, Coleman MJ, Nusbaum MP, Marder E.

J Exp Biol. 2000 Jul;203(Pt 14):2075-92.

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