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Items: 22

1.

Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222.

Singh AK, Fan Y, Balut C, Alani S, Manelli AM, Swensen AM, Jia Y, Neelands TR, Vortherms TA, Liu B, Searle XB, Wang X, Gao W, Hwang TC, Ren HY, Cyr D, Kym PR, Conrath K, Tse C.

J Pharmacol Exp Ther. 2020 Jan;372(1):107-118. doi: 10.1124/jpet.119.261800. Epub 2019 Nov 15.

PMID:
31732698
2.

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
3.

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
4.

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
5.

Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.

Doherty GA, Bhatia P, Vortherms TA, Marsh KC, Wetter JM, Mack H, Scott VE, Jarvis MF, Stewart AO.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1716-8. doi: 10.1016/j.bmcl.2011.12.100. Epub 2012 Jan 8.

PMID:
22277280
6.

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
7.

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
8.

In vitro and in vivo characterization of A-940894: a potent histamine H4 receptor antagonist with anti-inflammatory properties.

Strakhova MI, Cuff CA, Manelli AM, Carr TL, Witte DG, Baranowski JL, Vortherms TA, Miller TR, Rundell L, McPherson MJ, Adair RM, Brito AA, Bettencourt BM, Yao BB, Wetter JM, Marsh KC, Liu H, Cowart MD, Brioni JD, Esbenshade TA.

Br J Pharmacol. 2009 May;157(1):44-54. doi: 10.1111/j.1476-5381.2009.00236.x.

9.

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.

Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD.

J Med Chem. 2008 Nov 27;51(22):7094-8. doi: 10.1021/jm8007618.

PMID:
18983139
10.

Cloning and characterization of the monkey histamine H3 receptor isoforms.

Strakhova MI, Fox GB, Carr TL, Witte DG, Vortherms TA, Manelli AM, Miller TR, Yao BB, Brioni JD, Esbenshade TA.

Eur J Pharmacol. 2008 Dec 28;601(1-3):8-15. doi: 10.1016/j.ejphar.2008.10.026. Epub 2008 Oct 21.

PMID:
18977214
11.

Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.

Altenbach RJ, Adair RM, Bettencourt BM, Black LA, Fix-Stenzel SR, Gopalakrishnan SM, Hsieh GC, Liu H, Marsh KC, McPherson MJ, Milicic I, Miller TR, Vortherms TA, Warrior U, Wetter JM, Wishart N, Witte DG, Honore P, Esbenshade TA, Hancock AA, Brioni JD, Cowart MD.

J Med Chem. 2008 Oct 23;51(20):6571-80. doi: 10.1021/jm8005959. Epub 2008 Sep 24.

PMID:
18811133
12.

In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.

Nersesian DL, Black LA, Miller TR, Vortherms TA, Esbenshade TA, Hancock AA, Cowart MD.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):355-9. Epub 2007 Oct 24.

PMID:
18077160
13.
14.

Salvinorin A: from natural product to human therapeutics.

Vortherms TA, Roth BL.

Mol Interv. 2006 Oct;6(5):257-65. Review.

PMID:
17035666
15.

D2 dopamine receptor-induced sensitization of adenylyl cyclase type 1 is G alpha(s) independent.

Vortherms TA, Nguyen CH, Bastepe M, J├╝ppner H, Watts VJ.

Neuropharmacology. 2006 Apr;50(5):576-84. Epub 2005 Dec 27.

PMID:
16376953
16.

Autoxidation of salvinorin A under basic conditions.

Munro TA, Goetchius GW, Roth BL, Vortherms TA, Rizzacasa MA.

J Org Chem. 2005 Nov 25;70(24):10057-61.

17.

Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.

Yan F, Mosier PD, Westkaemper RB, Stewart J, Zjawiony JK, Vortherms TA, Sheffler DJ, Roth BL.

Biochemistry. 2005 Jun 21;44(24):8643-51.

PMID:
15952771
18.

Receptorome screening for CNS drug discovery.

Vortherms TA, Roth BL.

IDrugs. 2005 Jun;8(6):491-6. Review.

PMID:
15906196
19.

Nigrostriatal dopaminergic deficits and hypokinesia caused by inactivation of the familial Parkinsonism-linked gene DJ-1.

Goldberg MS, Pisani A, Haburcak M, Vortherms TA, Kitada T, Costa C, Tong Y, Martella G, Tscherter A, Martins A, Bernardi G, Roth BL, Pothos EN, Calabresi P, Shen J.

Neuron. 2005 Feb 17;45(4):489-96.

20.

Using molecular tools to dissect the role of Galphas in sensitization of AC1.

Vortherms TA, Nguyen CH, Berlot CH, Watts VJ.

Mol Pharmacol. 2004 Dec;66(6):1617-24. Epub 2004 Sep 10.

PMID:
15361543
21.

Sensitization of neuronal A2A adenosine receptors after persistent D2 dopamine receptor activation.

Vortherms TA, Watts VJ.

J Pharmacol Exp Ther. 2004 Jan;308(1):221-7. Epub 2003 Oct 17.

PMID:
14566008
22.

Adrenergic agonists induce heterologous sensitization of adenylate cyclase in NS20Y-D(2L) cells.

Johnston CA, Cumbay MG, Vortherms TA, Watts VJ.

FEBS Lett. 2001 May 25;497(2-3):85-9.

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