Petrine Wellendorph

Search results

• 2024

  Deficient brain GABA metabolism leads to widespread impairments of astrocyte and oligodendrocyte function

  Andersen, J. V., Marian, O. C., Qvist, F. L., Westi, E. W., Aldana, B. I., Schousboe, A., Don, A. S., Skotte, N. H. & Wellendorph, P., 2024, In: Glia. 72, 10, p. 1821-1839

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• Deletion of CaMKIIα disrupts glucose metabolism, glutamate uptake, and synaptic energetics in the cerebral cortex

  Andersen, J. V., Westi, E. W., Griem-Krey, N., Skotte, N. H., Schousboe, A., Aldana, B. I. & Wellendorph, P., 2024, In: Journal of Neurochemistry. 168, 5, p. 704-718

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  2 Citations (Scopus)

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• Gender balance in the editorial room: BCPT as model journal?

  Wellendorph, P. & Tveden-Nyborg, P., 2024, In: Basic and Clinical Pharmacology and Toxicology. 134, 6, p. 767-769

  Research output: Contribution to journal › Editorial › Research › peer-review

• Ligand-induced CaMKIIα hub Trp403 flip, hub domain stacking, and modulation of kinase activity

  Narayanan, D., Larsen, A. S. G., Gauger, S. J., Adafia, R., Hammershøi, R. B., Hamborg, L., Bruus-Jensen, J., Griem-Krey, N., Gee, C. L., Frølund, B., Stratton, M. M., Kuriyan, J., Kastrup, J. S., Langkilde, A. E., Wellendorph, P. & Solbak, S. M. Ø., 2024, In: Protein science : a publication of the Protein Society. 33, 10, 17 p., e5152.

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• Rational Search for Betaine/GABA Transporter 1 Inhibitors─In Vitro Evaluation of Selected Hit Compound

  Łątka, K., Kickinger, S., Rzepka, Z., Zaręba, P., Latacz, G., Siwek, A., Wolak, M., Stary, D., Marcinkowska, M., Wellendorph, P., Wrześniok, D. & Bajda, M., 2024, In: ACS Chemical Neuroscience. 15, 21, p. 4046–4054

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• Rodent ischemic stroke models and their relevance in preclinical research

  Thaysen, M., Westi, E. W., N. Clarkson, A., Wellendorph, P. & Kristensen, M., 2024, (E-pub ahead of print) In: Neuroprotection.

  Research output: Contribution to journal › Journal article › Research › peer-review

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• Transmembrane transporter proteins: Capturing transport in motion

  Loland, C. J., Wellendorph, P., Pedersen, S. F. & Gether, U., 2024, In: Basic and Clinical Pharmacology and Toxicology. 134, 2, p. 203-205 3 p.

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• Ways of modulating GABA transporters to treat neurological disease

  Mortensen, J. S., Mikkelsen, A. N. L. & Wellendorph, P., 2024, In: Expert Opinion On Therapeutic Targets. 28, 7, p. 529-543

  Research output: Contribution to journal › Review › Research › peer-review

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• 2023

  Astrocytes regulate inhibitory neurotransmission through GABA uptake, metabolism, and recycling

  Andersen, J. V., Schousboe, A. & Wellendorph, P., 2023, In: Essays in Biochemistry. 67, 1, p. 77-91

  Research output: Contribution to journal › Journal article › Research › peer-review
  18 Citations (Scopus)

• CaMK2 modulators and their use in medicine

  Frølund, B., Shehata, M. A., Wellendorph, P., Gauger, S. J., Kuriyan, J., McSpadden, E. D., Poulsen, L. B., Fougiaxis, V. & Daraj, K., 2023, IPC No. A61K31/4164, A61K31/4178, A61P25/00, C07D277/06, C07D277/12, C07D277/56, C07D417/04, C07D417/10, Patent No. WO2023170024A1, 1 Jan 1970, Priority No. US202263318852P

  Research output: Patent

  Open Access

• Functional modulation of a pH-sensitive ion channel by a transporter family

  Poulsen, M. H., Xue, F., Maurya, S. R., Kickinger, S., Usher, S., Wellendorph, P., Lundby, A. & Pless, S. A., 2023, In: Biophysical Journal. 122, 3 Suppl. 1, p. 249a

  Research output: Contribution to journal › Conference abstract in journal › Research › peer-review

• GABA transport cycle: beyond a GAT feeling

  Shahsavar, A. & Wellendorph, P., 2023, In: Nature Structural and Molecular Biology. 30, p. pages863–865

  Research output: Contribution to journal › Comment/debate › Research › peer-review
  2 Citations (Scopus)

• Non-invasive detection of narcolepsy type I phenotypical features and disease progression by continuous home-cage monitoring of activity in two mouse models: the HCRT-KO and DTA model

  Piilgaard, L., Rose, L., Justinussen, J. L., Hviid, C. G., Lemcke, R., Wellendorph, P. & Kornum, B. R., 2023, In: Sleep. 46, 9, 15 p., zsad144.

  Research output: Contribution to journal › Journal article › Research › peer-review
  2 Citations (Scopus)

• N-Terminomic Changes in Neurons During Excitotoxicity Reveal Proteolytic Events Associated With Synaptic Dysfunctions and Potential Targets for Neuroprotection

  Ameen, S. S., Griem-Krey, N., Dufour, A., Hossain, M. I., Hoque, A., Sturgeon, S., Nandurkar, H., Draxler, D. F., Medcalf, R. L., Kamaruddin, M. A., Lucet, I. S., Leeming, M. G., Liu, D., Dhillon, A., Lim, J. P., Basheer, F., Zhu, H. J., Bokhari, L., Roulston, C. L., Paradkar, P. N. & 7 others, Kleifeld, O., Clarkson, A. N., Wellendorph, P., Ciccotosto, G. D., Williamson, N. A., Ang, C. S. & Cheng, H. C., 2023, In: Molecular & cellular proteomics : MCP. 22, 5, 100543.

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• Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine

  Bavo, F., Kickinger, S., Lie, M. E. K., Avgerinos, C., Wilhelmsen, K. S., Wellendorph, P. & Frølund, B., 2023, In: Medicinal Chemistry Research. 32, p. 2299–2324

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• The GHB analogue HOCPCA improves deficits in cognition and sensorimotor function after MCAO via CaMKIIα

  Griem-Krey, N., Klein, A. B., Clausen, B. H., Namini, M. R. J., Nielsen, P. V., Bhuiyan, M., Nagaraja, R. Y., De Silva, T. M., Sobey, C. G., Cheng, H. C., Orset, C., Vivien, D., Lambertsen, K. L., Clarkson, A. N. & Wellendorph, P., 2023, In: Journal of Cerebral Blood Flow and Metabolism. 43, 8, p. 1419-1434

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  2 Citations (Scopus)

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• 2022

  CaMKIIα as a Promising Drug Target for Ischemic Grey Matter

  Griem-Krey, N., Clarkson, A. N. & Wellendorph, P., 2022, In: Brain Sciences. 12, 12, 21 p., 1639.

  Research output: Contribution to journal › Review › Research › peer-review

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  4 Citations (Scopus)

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• Development of a medium throughput whole-cell microtiter plate Thr286 autophosphorylation assay for CaMKIIα using ELISA

  Palmelund, L. B., van Woerden, G. M., Bräuner-Osborne, H. & Wellendorph, P., 2022, In: Journal of Pharmacological and Toxicological Methods. 118, 8 p., 107226.

  Research output: Contribution to journal › Journal article › Research › peer-review

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• Discovery and Optimization of 5-Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain

  Tian, Y., Shehata, M. A., Gauger, S. J., Ng, C. K. L., Solbak, S., Thiesen, L., Bruus-Jensen, J., Krall, J., Bundgaard, C., Gibson, K. M., Wellendorph, P. & Frølund, B., 2022, In: Journal of Medicinal Chemistry. 65, 9, p. 6656-6676

  Research output: Contribution to journal › Journal article › Research › peer-review
  4 Citations (Scopus)

• Elucidating Pathway and Anesthetic Mechanism of Action of Clove Oil Nanoformulations in Fish

  Kheawfu, K., Pikulkaew, S., Wellendorph, P., Jørgensen, L. V. G., Rades, T., Mullertz, A. & Okonogi, S., 2022, In: Pharmaceutics. 14, 5, 13 p., 919.

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  10 Citations (Scopus)

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• Exploring the NCS-382 Scaffold for CaMKII alpha Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKII alpha Hub Domain

  Tian, Y., Shehata, M. A., Gauger, S. J., Veronesi, C., Hamborg, L., Thiesen, L., Bruus-Jensen, J., Royssen, J. S., Leurs, U., Larsen, A. S. G., Krall, J., Solbak, S. M. O., Wellendorph, P. & Frolund, B., 2022, In: Journal of Medicinal Chemistry. 65, 22, p. 15066–15084

  Research output: Contribution to journal › Journal article › Research › peer-review
  4 Citations (Scopus)

• Synthesis of gamma-Aminobutyric Acid (GABA) Analogues Conformationally Restricted by Bicyclo[3.1.0]hexane/hexene or [4.1.0]Heptane/heptene Backbones as Potent Betaine/GABA Transporter Inhibitors

  Mitsui, K., Lie, M. E. K., Saito, N., Fujiwara, K., Watanabe, M., Wellendorph, P. & Shuto, S., 2022, In: Organic Letters. 24, 23, p. 4151-4154

  Research output: Contribution to journal › Journal article › Research › peer-review
  2 Citations (Scopus)

• The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABA(A) Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform

  Khumpirapang, N., Suknuntha, K., Wongrattanakamon, P., Jiranusornkul, S., Anuchapreeda, S., Wellendorph, P., Mullertz, A., Rades, T. & Okonogi, S., 2022, In: Pharmaceutics. 14, 3, 15 p., 650.

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  2 Citations (Scopus)

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• The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction

  Griem-Krey, N., Gauger, S. J., Gowing, E. K., Thiesen, L., Frølund, B., Clarkson, A. N. & Wellendorph, P., 2022, In: Biomedicine and Pharmacotherapy. 156, 10 p., 113895.

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  4 Citations (Scopus)

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• 2021

  GABAA receptor β1-subunit knock-out mice show increased delta power in NREM sleep and decreased theta power in REM sleep

  Lie, M. E. K., Falk-Petersen, C. B., Petersen, L. P., Griem-Krey, N., Wellendorph, P. & Kornum, B. R., 2021, In: European Journal of Neuroscience. 54, 2, p. 4445-4455 11 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  5 Citations (Scopus)

• GHB analogs confer neuroprotection through specific interaction with the CaMKIIα hub domain

  Leurs, U., Klein, A. B., McSpadden, E. D., Griem-Krey, N., Solbak, S. M. Ø., Houlton, J., Villumsen, I. S., Vogensen, S. B., Hamborg, L., Gauger, S. J., Palmelund, L. B., Larsen, A. S. G., Shehata, M. A., Kelstrup, C. D., Olsen, J. V., Bach, A., Burnie, R. O., Kerr, D. S., Gowing, E. K., Teurlings, S. M. W. & 9 others, Chi, C. C., Gee, C. L., Frølund, B., Kornum, B. R., van Woerden, G. M., Clausen, R. P., Kuriyan, J., Clarkson, A. N. & Wellendorph, P., 2021, In: Proceedings of the National Academy of Sciences of the United States of America. 118, 31, 9 p., e2108079118.

  Research output: Contribution to journal › Journal article › Research › peer-review

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  28 Citations (Scopus)

• Molecular Determinants and Pharmacological Analysis for a Class of Competitive Non-transported Bicyclic Inhibitors of the Betaine/GABA Transporter BGT1

  Kickinger, S., Lie, M. E. K., Suemasa, A., Al-Khawaja, A., Fujiwara, K., Watanabe, M., Wilhelmsen, K. S., Falk-Petersen, C. B., Frølund, B., Shuto, S., Ecker, G. F. & Wellendorph, P., 2021, In: Frontiers in Chemistry. 9, 13 p., 736457.

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• Molecular Determinants underlying Delta Selective Compound 2 (DS2) Activity at δ-Containing GABAA Receptors

  Falk-Petersen, C. B., Rostrup, F., Löffler, R., Buchleihtner, S., Harpsøe, K., Gloriam, D. E., Frølund, B. & Wellendorph, P., 2021, In: Molecular Pharmacology. 100, 1, p. 46-56

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• Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology

  Griem-Krey, N., Frolund, B., Marek, A. & Wellendorph, P., 2021, In: Journal of Labelled Compounds and Radiopharmaceuticals. 64, 2, 77 p.

  Research output: Contribution to journal › Journal article › Research › peer-review

• Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors

  Rostrup, F., Falk-petersen, C. B., Harpsøe, K., Buchleithner, S., Conforti, I., Jung, S., Gloriam, D. E., Schirmeister, T., Wellendorph, P. & Frølund, B., 22 Apr 2021, In: Journal of Medicinal Chemistry. 64, 8, p. 4730-4743 14 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  7 Citations (Scopus)

• Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based ?-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect

  Bavo, F., De-Jong, H., Petersen, J., Falk-Petersen, C. B., Löffler, R., Sparrow, E., Rostrup, F., Eliasen, J. N., Wilhelmsen, K. S., Barslund, K., Bundgaard, C., Nielsen, B., Kristiansen, U., Wellendorph, P., Bogdanov, Y. & Frølund, B., 2021, In: Journal of Medicinal Chemistry. 64, 24, p. 17795-17812

  Research output: Contribution to journal › Journal article › Research › peer-review
  3 Citations (Scopus)
• 2020

  A CLASS OF SMALL-MOLECULE COMPOUNDS AND THEIR PRODRUGS FOR INTERVENTION WITH CAMK2A, AND THEIR USE IN ACUTE BRAIN INJURIES AND CENTRAL HYPERSOMNIAS

  Frølund, B., Wellendorph, P. & Kornum, B. R., 2020, Patent No. WO2020151795, 30 Jul 2020, Priority date 21 Jan 2019, Priority No. DK2019PA70040 20190121

  Research output: Patent

• Compounds for the treatment of acute brain injury

  Klein, A. B., Leurs, U., Houlton, J., Clausen, R. P., Frølund, B., Clarkson, A. & Wellendorph, P., 2020, Patent No. CN111989094, 24 Nov 2020, Priority date 1 Feb 2019, Priority No. PCT/DK2019/050041

  Research output: Patent

• Discovery of a new class of orthosteric antagonists with nanomolar potency at extrasynaptic GABA_A receptors

  Falk-Petersen, C. B., Tsonkov, T. M., Nielsen, M. S., Harpsøe, K., Bundgaard, C., Frølund, B., Kristiansen, U., Gloriam, D. E. & Wellendorph, P., 22 Jun 2020, In: Scientific Reports. 10, 1, 12 p., 10078.

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  10 Citations (Scopus)

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• Exploring the molecular determinants for subtype-selectivity of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid analogs as betaine/GABA transporter 1 (BGT1) substrate-inhibitors

  Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, F., Loeffler, R., Damgaard, M., Ecker, G. F., Frolund, B. & Wellendorph, P., 2020, In: Scientific Reports. 10, 1, 15 p., 12992.

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  5 Citations (Scopus)

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• Extensive astrocyte metabolism of γ-aminobutyric acid (GABA) sustains glutamine synthesis in the mammalian cerebral cortex

  Andersen, J. V., Jakobsen, E., Westi, E. W., Lie, M. E. K., Voss, C. M., Aldana, B. I., Schousboe, A., Wellendorph, P., Bak, L. K., Pinborg, L. H. & Waagepetersen, H. S., 2020, In: Glia. 68, 12, p. 2601-2612

  Research output: Contribution to journal › Journal article › Research › peer-review
  35 Citations (Scopus)

• Pharmacological Characterization of a Betaine/GABA Transporter 1 (BGT1) Inhibitor Displaying an Unusual Biphasic Inhibition Profile and Anti-seizure Effects

  Lie, M. E. K., Kickinger, S., Skovgaard-Petersen, J., Ecker, G. F., Clausen, R. P., Schousboe, A., White, H. S. & Wellendorph, P., 2020, In: Neurochemical Research. 45, p. 1551–1565

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  9 Citations (Scopus)

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• Silencing of spontaneous activity at α4β1/3δ GABAA receptors in hippocampal granule cells reveals different ligand pharmacology

  Dalby, N. O., Falk-Petersen, C. B., Leurs, U., Scholze, P., Krall, J., Frølund, B. & Wellendorph, P., 2020, In: British Journal of Pharmacology. 177, 17, p. 3975-3990

  Research output: Contribution to journal › Journal article › Research › peer-review

  Open Access
  9 Citations (Scopus)

• The γ-hydroxybutyric acid (GHB) analogue NCS-382 is a substrate for both monocarboxylate transporters subtypes 1 and 4

  Thiesen, L., Belew, Z. M., Griem-Krey, N., Pedersen, S. F., Crocoll, C., Nour-Eldin, H. H. & Wellendorph, P., 15 Feb 2020, In: European Journal of Pharmaceutical Sciences. 143, p. 1-9 105203.

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  4 Citations (Scopus)

• TREATMENT OF CNS DISORDERS WITH SLEEP DISTURBANCES

  Wellendorph, P., Kornum, B. R. & Frølund, B., 2020, Patent No. WO2020259787 , 30 Dec 2020, Priority date 28 Jun 2019, Priority No. DK2019PA70415 20190628

  Research output: Patent

• Unraveling the Molecular Determinants for GABA Transporter Subtype Selectivity

  Kickinger, S., Al-Khawaja, A., Haugaard, A. S., Lie, M. E. K., Bavo, F., Loffler, R., Damgaard, M., Frolund, B., Ecker, G. F. & Wellendorph, P., 2020, p. 130A-130A.

  Research output: Contribution to conference › Conference abstract for conference › Research › peer-review
• 2019

  Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets

  Griem-Krey, N., Klein, A. B., Herth, M. & Wellendorph, P., 12 Mar 2019, In: Journal of visualized experiments : JoVE. 145, 11 p., e58879.

  Research output: Contribution to journal › Journal article › Communication
  24 Citations (Scopus)

• Discovery of 2-(Imidazo[1,2-b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites

  Krall, J., Bavo, F., Falk-Petersen, C. B., Jensen, C. H., Nielsen, J. O., Tian, Y., Anglani, V., Kongstad, K. T., Piilgaard, L., Nielsen, B., Gloriam, D. E., Kehler, J., Jensen, A. A., Harpsøe, K., Wellendorph, P. & Frølund, B., 14 Mar 2019, In: Journal of Medicinal Chemistry. 62, 5, p. 2798-2813

  Research output: Contribution to journal › Journal article › Research › peer-review
  13 Citations (Scopus)

• Five-membered N-heterocyclic Scaffolds as Novel Amino Bioisosteres at gamma-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters

  Giraudo, A., Krall, J., Bavo, F., Nielsen, B., Kongstad, K. T., Rolando, B., De Blasio, R., Gloriam, D. E., Löffler, R., Thiesen, L., Harpsøe, K., Frydenvang, K., Boschi, D., Wellendorph, P., Lolli, M. L., Jensen, A. A. & Frølund, B., 27 Jun 2019, In: Journal of Medicinal Chemistry. 62, 12, p. 5797-5809

  Research output: Contribution to journal › Journal article › Research › peer-review
  19 Citations (Scopus)

• GAT3 selective substrate l-isoserine upregulates GAT3 expression and increases functional recovery after a focal ischemic stroke in mice

  Lie, M. E., Gowing, E. K., Johansen, N. B., Dalby, N. O., Thiesen, L., Wellendorph, P. & Clarkson, A. N., 1 Jan 2019, In: Journal of Cerebral Blood Flow and Metabolism. 39, 1, p. 74-88 15 p.

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• Lack of evidence for synaptic high-affinity γ-hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na+ -dependent SLC neurotransmitter transporters

  Thiesen, L., Frølund, B. & Wellendorph, P., Apr 2019, In: Journal of Neurochemistry. 149, 2, p. 195-210 16 p.

  Research output: Contribution to journal › Journal article › Research › peer-review
  1 Citation (Scopus)

• Structural and molecular aspects of betaine-GABA transporter 1 (BGT1) and its relation to brain function

  Kickinger, S., Hellsberg, E., Frølund, B., Schousboe, A., Ecker, G. F. & Wellendorph, P., 2019, In: Neuropharmacology. 161, 14 p., 107644.

  Research output: Contribution to journal › Review › Research › peer-review
  24 Citations (Scopus)

• Synthesis and Pharmacological Evaluation of [C-11]4-Methoxy-N-[2-(thiophen-2-yl) imidazo[1,2-a] pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the delta-Subunit-Containing gamma-Aminobutyric Acid Type A Receptors

  L'Estrade, E. T., Hansen, H. D., Falk-Petersen, C., Haugaard, A., Griem-Krey, N., Jung, S., Lueddens, H., Schirmeister, T., Erlandsson, M., Ohlsson, T., Knudsen, G. M., Herth, M. M., Wellendorph, P. & Frolund, B., May 2019, In: ACS Omega. 4, 5, p. 8846-8851

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  7 Citations (Scopus)

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• 2018

  Inhibition of GABA transporters fails to afford significant protection following focal cerebral ischemia

  Lie, M. E., Gowing, E. K., Clausen, R. P., Wellendorph, P. & Clarkson, A. N., 2018, In: Journal of Cerebral Blood Flow and Metabolism. 38, 1, p. 166-173

  Research output: Contribution to journal › Journal article › Research › peer-review

  Open Access
  8 Citations (Scopus)

• Pharmacological Characterization of [³H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter

  Al-Khawaja, A., Haugaard, A. S., Marek, A., Löffler, R., Thiesen, L., Santiveri, M., Damgaard, M., Bundgaard, C., Frølund, B. & Wellendorph, P., 21 Mar 2018, In: A C S Chemical Neuroscience. 9, 3, p. 545–554

  Research output: Contribution to journal › Journal article › Research › peer-review
  9 Citations (Scopus)