Thomas Erker

Thomas Erker

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Thomas Erker

Thomas Erker

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Functional characterization of novel bumetanide derivatives for epilepsy treatment.

Neuropharmacology 2020 01 30;162:107754. Epub 2019 Aug 30.

Department of Pharmacology, Medical University of Innsbruck, Peter-Mayr-Str. 1a, 6020, Innsbruck, Austria. Electronic address:

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http://dx.doi.org/10.1016/j.neuropharm.2019.107754DOI Listing
January 2020

Impaired chloride homeostasis in epilepsy: Molecular basis, impact on treatment, and current treatment approaches.

Pharmacol Ther 2020 01 15;205:107422. Epub 2019 Oct 15.

Department of Pharmacology, Medical University of Innsbruck, Peter-Mayr-Str. 1a, 6020 Innsbruck, Austria. Electronic address:

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http://dx.doi.org/10.1016/j.pharmthera.2019.107422DOI Listing
January 2020

Multiple blood-brain barrier transport mechanisms limit bumetanide accumulation, and therapeutic potential, in the mammalian brain.

Neuropharmacology 2017 05 10;117:182-194. Epub 2017 Feb 10.

Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine Hannover, Germany; Center for Systems Neuroscience, Hannover, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.neuropharm.2017.02.006DOI Listing
May 2017

The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A.

Epilepsy Behav 2016 06 15;59:42-9. Epub 2016 Apr 15.

Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine Hannover, Germany; Center for Systems Neuroscience, Hannover, Germany. Electronic address:

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http://dx.doi.org/10.1016/j.yebeh.2016.03.021DOI Listing
June 2016

The bumetanide prodrug BUM5, but not bumetanide, potentiates the antiseizure effect of phenobarbital in adult epileptic mice.

Epilepsia 2016 05 27;57(5):698-705. Epub 2016 Feb 27.

Department of Pharmacology, Toxicology and Pharmacy, University of Veterinary Medicine Hannover, Hannover, Germany.

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http://dx.doi.org/10.1111/epi.13346DOI Listing
May 2016

Drug trapping in hERG K channels: (not) a matter of drug size?

Medchemcomm 2016 Mar 22;7(3):512-518. Epub 2015 Dec 22.

Department of Pharmacology and Toxicology , University of Vienna , Austria . Email:

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http://dx.doi.org/10.1039/c5md00443hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5292991PMC
March 2016

Antiproliferative and Pro-apoptotic Activities of a Novel Resveratrol Prodrug Against Jurkat CD4+ T-Cells.

Anticancer Res 2016 Feb;36(2):683-9

Department for Pharmaceutical Chemistry, University of Vienna, Vienna, Austria.

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February 2016

Structure-activity relationships of bumetanide derivatives: correlation between diuretic activity in dogs and inhibition of the human NKCC2A transporter.

Br J Pharmacol 2015 Sep 4;172(18):4469-4480. Epub 2015 Aug 4.

Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine Hannover, Hannover, Germany.

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http://dx.doi.org/10.1111/bph.13231DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4562508PMC
September 2015

Discovery of small molecules with vasodilating characteristics and adjustable hydrolytic behavior.

Bioorg Med Chem 2015 Aug 5;23(15):4710-8. Epub 2015 Jun 5.

Department of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.05.049DOI Listing
August 2015

Hydrogen sulphide induces HIF-1α and Nrf2 in THP-1 macrophages.

Biochimie 2015 May 18;112:187-95. Epub 2015 Mar 18.

Center of Pathobiochemistry and Genetics, Department of Medical Chemistry and Pathobiochemistry, Medical University of Vienna, Vienna, Austria. Electronic address:

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http://dx.doi.org/10.1016/j.biochi.2015.03.009DOI Listing
May 2015

Enhanced Antiproliferative and Pro-apoptotic Activities of a Novel Curcumin-related Compound in Jurkat Leukemia T-Cells.

Anticancer Res 2015 May;35(5):2675-80

Ludwig Boltzmann Institute for Rheumatology and Balneology, Cluster Rheumatology, Balneology and Rehabilitation, Vienna, Austria

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May 2015

SAR-guided development and characterization of a potent antitumor compound toward B-cell neoplasms with no detectable cytotoxicity toward healthy cells.

J Med Chem 2015 Feb 20;58(3):1244-53. Epub 2015 Jan 20.

Department of Medicinal Chemistry, University of Vienna , Althanstrasse 14, 1090 Vienna, Austria.

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http://dx.doi.org/10.1021/jm501848mDOI Listing
February 2015

Bumetanide is not capable of terminating status epilepticus but enhances phenobarbital efficacy in different rat models.

Eur J Pharmacol 2015 Jan 11;746:78-88. Epub 2014 Nov 11.

Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine Hannover, Germany; Center for Systems Neuroscience, Hannover, Germany. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00142999140076
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http://dx.doi.org/10.1016/j.ejphar.2014.10.056DOI Listing
January 2015

Efficient modulation of γ-aminobutyric acid type A receptors by piperine derivatives.

J Med Chem 2014 Jul 27;57(13):5602-19. Epub 2014 Jun 27.

Department of Pharmacology and Toxicology and §Division of Drug Design and Medicinal Chemistry, Department of Pharmaceutical Chemistry, University of Vienna , Althanstrasse 14, A-1090 Vienna, Austria.

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http://dx.doi.org/10.1021/jm5002277DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4106271PMC
July 2014

Synthesis, biological evaluation and 3D-QSAR studies of new chalcone derivatives as inhibitors of human P-glycoprotein.

Bioorg Med Chem 2014 Apr 15;22(7):2311-9. Epub 2014 Feb 15.

University of Vienna, Department of Medicinal Chemistry, Althanstrasse 14, 1090 Vienna, Austria. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2014.02.005DOI Listing
April 2014

A novel prodrug-based strategy to increase effects of bumetanide in epilepsy.

Ann Neurol 2014 Apr 2;75(4):550-62. Epub 2014 Apr 2.

Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine, Hannover, Germany; Center for Systems Neuroscience, Hannover, Germany.

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http://dx.doi.org/10.1002/ana.24124DOI Listing
April 2014

Foam cell specific LXRα ligand.

PLoS One 2013 25;8(2):e57311. Epub 2013 Feb 25.

Otto Warburg Laboratory, Max Planck Institute for Molecular Genetics, Berlin, Germany.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0057311PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3581588PMC
September 2013

GABAA receptor modulation by piperine and a non-TRPV1 activating derivative.

Biochem Pharmacol 2013 Jun 25;85(12):1827-36. Epub 2013 Apr 25.

Department of Pharmacology and Toxicology, University of Vienna, Althanstraße 14, A-1090 Wien, Austria.

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http://dx.doi.org/10.1016/j.bcp.2013.04.017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3776227PMC
June 2013

Tariquidar and elacridar are dose-dependently transported by P-glycoprotein and Bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study.

Drug Metab Dispos 2013 Apr 10;41(4):754-62. Epub 2013 Jan 10.

Department of Pharmacology, Toxicology, and Pharmacy, University of Veterinary Medicine, and Center for Systems Neuroscience, Hannover, Germany.

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http://dx.doi.org/10.1124/dmd.112.049148DOI Listing
April 2013

The exploration of thienothiazines as selective butyrylcholinesterase inhibitors.

Eur J Pharm Sci 2012 Aug 6;47(1):190-205. Epub 2012 Jun 6.

Department of Biosciences, Pharmaceutical Sciences, Abo Akademi University, BioCity, Tykistökatu 6 A, FI-20520 Turku, Finland.

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http://dx.doi.org/10.1016/j.ejps.2012.05.014DOI Listing
August 2012

Identification and characterization of diarylimidazoles as hybrid inhibitors of butyrylcholinesterase and amyloid beta fibril formation.

Eur J Pharm Sci 2012 Jan 16;45(1-2):169-83. Epub 2011 Nov 16.

Pharmaceutical Sciences, Department of Biosciences, Abo Akademi University, BioCity, Artillerigatan 6A, FI-20520 Turku, Finland.

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http://dx.doi.org/10.1016/j.ejps.2011.11.004DOI Listing
January 2012

PET and SPECT radiotracers to assess function and expression of ABC transporters in vivo.

Curr Drug Metab 2011 Oct;12(8):774-92

Health and Environment Department, Molecular Medicine, AIT Austrian Institute of Technology GmbH, 2444 Seibersdorf, Austria.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3691789PMC
http://dx.doi.org/10.2174/138920011798356980DOI Listing
October 2011

Using structural and mechanistic information to design novel inhibitors/substrates of P-glycoprotein.

Curr Top Med Chem 2010 ;10(17):1769-74

University of Vienna, Department of Medicinal Chemistry, Althanstrasse 14, 1090 Wien, Austria.

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http://dx.doi.org/10.2174/156802610792928004DOI Listing
January 2011

Synthesis, spasmolytic activity and structure-activity relationship study of a series of polypharmacological thiobenzanilides.

Eur J Pharm Sci 2011 Jan 20;42(1-2):37-44. Epub 2010 Oct 20.

Department of Medicinal Chemistry, University of Vienna, Althanstraße 14, Vienna, Austria.

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http://dx.doi.org/10.1016/j.ejps.2010.10.005DOI Listing
January 2011

A journey from benzanilides to dithiobenzanilides: Synthesis of selective spasmolytic compounds.

Bioorg Med Chem 2011 Jan 25;19(2):994-1001. Epub 2010 Nov 25.

Department of Medicinal Chemistry, University of Vienna, Austria.

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http://dx.doi.org/10.1016/j.bmc.2010.11.043DOI Listing
January 2011

Synthesis of new acridone derivatives, inhibitors of NS3 helicase, which efficiently and specifically inhibit subgenomic HCV replication.

J Med Chem 2010 Apr;53(8):3117-26

Institute of Biochemistry and Biophysics, PAS, Pawinskiego 5a, 02-106 Warsaw, Poland.

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http://dx.doi.org/10.1021/jm901741pDOI Listing
April 2010

Antitumor effects of KITC, a new resveratrol derivative, in AsPC-1 and BxPC-3 human pancreatic carcinoma cells.

Invest New Drugs 2009 Oct 8;27(5):393-401. Epub 2008 Oct 8.

Clinical Institute of Medical and Chemical Laboratory Diagnostics, General Hospital of Vienna, Medical University of Vienna, Waehringer Guertel 18-20, A-1090, Vienna, Austria.

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http://link.springer.com/10.1007/s10637-008-9183-7
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http://dx.doi.org/10.1007/s10637-008-9183-7DOI Listing
October 2009

Pros and cons of using resazurin staining for quantification of viable Staphylococcus aureus biofilms in a screening assay.

J Microbiol Methods 2009 Jul 8;78(1):104-6. Epub 2009 May 8.

Division of Pharmacy, Department of Biochemistry and Pharmacy, Abo Akademi University, Turku, Finland.

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http://dx.doi.org/10.1016/j.mimet.2009.04.014DOI Listing
July 2009

Benzanilides with spasmolytic activity: chemistry, pharmacology, and SAR.

Bioorg Med Chem 2008 Jun 26;16(11):5974-81. Epub 2008 Apr 26.

Department of Pharmaceutical Chemistry, University of Vienna, A-1090 Vienna, Althanstrasse 14, Austria.

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http://dx.doi.org/10.1016/j.bmc.2008.04.057DOI Listing
June 2008

Synthesis and biological activity of thienodiltiazem in isolated heart muscle preparations of guinea pigs.

Arzneimittelforschung 2007 ;57(12):757-61

Department of Pharmaceutical and Medicinal Chemistry, University of Vienna, Vienna, Austria.

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http://dx.doi.org/10.1055/s-0031-1296676DOI Listing
May 2008

No evidence for modulation of endothelial nitric oxide synthase by the olive oil polyphenol hydroxytyrosol in human endothelial cells.

Atherosclerosis 2007 Nov 30;195(1):e58-64. Epub 2007 Mar 30.

Department of Pharmacognosy, University of Vienna, A-1090 Vienna, Austria.

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http://dx.doi.org/10.1016/j.atherosclerosis.2007.02.024DOI Listing
November 2007

Novel resveratrol derivatives induce apoptosis and cause cell cycle arrest in prostate cancer cell lines.

Anticancer Res 2007 Sep-Oct;27(5A):3459-64

Clinical Institute of Medical and Chemical Laboratory Diagnostics, Waehringer Guertel 18-20, A-1090, Vienna, Austria.

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November 2007

'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.

Bioorg Med Chem 2007 Sep 20;15(18):6109-18. Epub 2007 Jun 20.

Department of Medicinal Chemistry, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria.

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http://dx.doi.org/10.1016/j.bmc.2007.06.030DOI Listing
September 2007

Synthesis of novel curcumin analogues and their evaluation as selective cyclooxygenase-1 (COX-1) inhibitors.

Chem Pharm Bull (Tokyo) 2007 Jan;55(1):64-71

Department of Medicinal Chemistry, University of Vienna, Vienna, Austria.

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http://dx.doi.org/10.1248/cpb.55.64DOI Listing
January 2007

Cytotoxic and biochemical effects of 3,3',4,4',5,5'-hexahydroxystilbene, a novel resveratrol analog in HL-60 human promyelocytic leukemia cells.

Exp Hematol 2006 Oct;34(10):1377-84

Clinical Institute of Medical and Chemical Laboratory Diagnostics, General Hospital of Vienna, Medical University of Vienna, Vienna, Austria.

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http://dx.doi.org/10.1016/j.exphem.2006.05.018DOI Listing
October 2006

Antioxidant activity of resveratrol, piceatannol and 3,3',4,4',5,5'-hexahydroxy-trans-stilbene in three leukemia cell lines.

Oncol Rep 2006 Sep;16(3):617-24

Department of Mutagenesis and Carcinogenesis, Cancer Research Institute, Slovak Academy of Sciences, 833 91 Bratislava, Slovak Republic.

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September 2006

Cyclooxygenase-1 and cyclooxygenase-2 inhibition of novel 1,2-disubstituted imidazoles.

Arch Pharm (Weinheim) 2005 Dec;338(12):602-4

Department of Medicinal Chemistry, University of Vienna, Vienna, Austria.

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http://dx.doi.org/10.1002/ardp.200500178DOI Listing
December 2005

Synthesis and pharmacological profile of non-peptide vasopressin antagonists.

Eur J Pharm Sci 2005 Apr;24(5):421-31

Department of Medicinal/Pharmaceutical Chemistry, University of Vienna, A-1090 Vienna, Althanstrasse 14, Austria.

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http://dx.doi.org/10.1016/j.ejps.2004.12.008DOI Listing
April 2005

Synergistic action of resveratrol, an ingredient of wine, with Ara-C and tiazofurin in HL-60 human promyelocytic leukemia cells.

Exp Hematol 2005 Mar;33(3):329-35

Clinical Institute of Medical and Chemical Laboratory Diagnostics, General Hospital of Vienna, Medical University of Vienna, Vienna, Austria.

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http://dx.doi.org/10.1016/j.exphem.2004.11.009DOI Listing
March 2005

Antioxidant, prooxidant and cytotoxic activity of hydroxylated resveratrol analogues: structure-activity relationship.

Biochem Pharmacol 2005 Mar;69(6):903-12

Institute of Pharmaceutical Chemistry, University of Vienna, A-1090 Vienna, Austria.

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http://dx.doi.org/10.1016/j.bcp.2004.12.001DOI Listing
March 2005

Resveratrol analogues as selective cyclooxygenase-2 inhibitors: synthesis and structure-activity relationship.

Bioorg Med Chem 2004 Nov;12(21):5571-8

Institute of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria.

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http://dx.doi.org/10.1016/j.bmc.2004.08.008DOI Listing
November 2004

Effects of novel synthesized pyridothiazines on various guinea pig heart muscle preparations.

Biol Pharm Bull 2004 Sep;27(9):1364-70

Department of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria.

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http://dx.doi.org/10.1248/bpb.27.1364DOI Listing
September 2004

Synthesis and multidrug-resistance modulating activity of a series of thienothiazines.

Arch Pharm (Weinheim) 2002 May;335(5):223-8

Institute of Medical Chemistry, University of Vienna, Wien, Austria.

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http://dx.doi.org/10.1002/1521-4184(200205)335:5<223::AID-ARDP223>3.0.CO;2-DDOI Listing
May 2002