P. Wellendorph

S. Pedersen, P. Wellendorph, C. Crocoll, 2019, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

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

G. Knudsen, T. Ohlsson, T. Schirmeister, 2019 .

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

G. Knudsen, T. Ohlsson, T. Schirmeister, 2019, ACS omega.

Low nanomolar GABA effects at extrasynaptic a 4 b 1 / b 3 d GABAA receptor subtypes indicate a different binding mode for GABA at these receptors

J. Hanrahan, P. Wellendorph, G. Johnston, 2012 .

α4βδ GABAA receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)

J. Olsen, G. Knudsen, N. Absalom, 2012, Proceedings of the National Academy of Sciences.

Low nanomolar GABA effects at extrasynaptic α4β1/β3δ GABA(A) receptor subtypes indicate a different binding mode for GABA at these receptors.

J. Hanrahan, N. Absalom, P. Wellendorph, 2012, Biochemical pharmacology.

The l-α-amino acid receptor GPRC6A is expressed in the islets of Langerhans but is not involved in l-arginine-induced insulin release

J. Holst, P. Thams, P. Wellendorph, 2012, Amino Acids.

Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.

U. Kristiansen, B. Rolando, R. Fruttero, 2006, Journal of medicinal chemistry.

Monastrol, a 3,4-dihydropyrimidin-2(1H)-thione, as structural scaffold for the development of modulators for GHB high-affinity binding sites and α1β2δ GABAA receptors.

P. Wellendorph, B. Frølund, M. Damgaard, 2017, European journal of medicinal chemistry.

Positive allosteric modulation of the GHB high-affinity binding site by the GABAA receptor modulator monastrol and the flavonoid catechin.

P. Wellendorph, B. Frølund, K. T. Kongstad, 2014, European journal of pharmacology.

Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H3 receptor

D. Weiner, M. Brann, N. Nash, 2002, Neuropharmacology.

In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1

J. Kehler, C. Bundgaard, P. Wellendorph, 2015, The Journal of Pharmacology and Experimental Therapeutics.

No evidence for a bone phenotype in GPRC6A knockout mice under normal physiological conditions.

E. Casanova, M. Gassmann, B. Bettler, 2008, Journal of molecular endocrinology.

Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).

G. Ecker, A. Schousboe, P. Wellendorph, 2017, Journal of medicinal chemistry.

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.

J. Kehler, D. Gloriam, P. Wellendorph, 2019, Journal of medicinal chemistry.

Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs.

David E. Gloriam, J. Kehler, D. Gloriam, 2017, Journal of medicinal chemistry.

Phenylacetic acids and the structurally related non‐steroidal anti‐inflammatory drug diclofenac bind to specific γ‐hydroxybutyric acid sites in rat brain

Christian Skonberg, P. Wellendorph, H. Bräuner‐Osborne, 2009, Fundamental & clinical pharmacology.

Novel Cyclic γ-Hydroxybutyrate (GHB) Analogs with High Affinity and Stereoselectivity of Binding to GHB Sites in Rat Brain

J. Greenwood, P. Wellendorph, B. Frølund, 2005, Journal of Pharmacology and Experimental Therapeutics.

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

C. Bundgaard, P. Wellendorph, B. Frølund, 2017, ACS chemical neuroscience.

Known regulators of nitric oxide synthase and arginase are agonists at the human G‐protein‐coupled receptor GPRC6A

P. Wellendorph, H. Bräuner‐Osborne, B. Christiansen, 2006, British journal of pharmacology.

Activity of l-α-amino acids at the promiscuous goldfish odorant receptor 5.24

P. Wellendorph, H. Bräuner‐Osborne, B. Christiansen, 2006 .

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

A. Clarkson, P. Wellendorph, B. Frølund, 2022, Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie.

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

P. Wellendorph, B. Frølund, Louise Thiesen, 2019, Journal of neurochemistry.

Delineation of the GPRC6A Receptor Signaling Pathways Using a Mammalian Cell Line Stably Expressing the Receptor

Alex R. B. Thomsen, P. Wellendorph, H. Bräuner‐Osborne, 2013, The Journal of Pharmacology and Experimental Therapeutics.

Activity of L-alpha-amino acids at the promiscuous goldfish odorant receptor 5.24.

P. Wellendorph, H. Bräuner‐Osborne, B. Christiansen, 2006, European journal of pharmacology.

Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites.

C. Bundgaard, G. Knudsen, S. Lehel, 2017, ACS chemical neuroscience.

Structural Determinants for the Mode of Action of the Imidazopyridine DS2 at d-containing g-Aminobutyric Acid Type A (GABAA) Receptors

D. Gloriam, T. Schirmeister, P. Wellendorph, 2020 .

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

G. Ecker, A. Schousboe, H. White, 2020, Neurochemical Research.

Demonstration of the dynamic mass redistribution label-free technology as a useful cell-based pharmacological assay for endogenously expressed GABAA receptors

P. Wellendorph, Anas Al-Khawaja, A. Klein, 2016 .

CaMKIIα as a Promising Drug Target for Ischemic Grey Matter

A. Clarkson, P. Wellendorph, Nane Griem-Krey, 2022, Brain sciences.

Novel Radioiodinated γ-Hydroxybutyric Acid Analogues for Radiolabeling and Photolinking of High-Affinity γ-Hydroxybutyric Acid Binding Sites

G. Knudsen, P. Wellendorph, B. Frølund, 2010, Journal of Pharmacology and Experimental Therapeutics.

Molecular Pharmacology of Promiscuous Seven Transmembrane Receptors Sensing Organic Nutrients

P. Wellendorph, H. Bräuner‐Osborne, L. D. Johansen, 2009, Molecular Pharmacology.

Deorphanization of GPRC6A: A Promiscuous l-α-Amino Acid Receptor with Preference for Basic Amino Acids

J. Greenwood, K. Hansen, P. Wellendorph, 2005, Molecular Pharmacology.

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

G. Ecker, A. Schousboe, P. Wellendorph, 2019, Neuropharmacology.

γ‐Aminobutyric Acid and Glycine Neurotransmitter Transporters

G. Ecker, A. Schousboe, P. Krogsgaard‐Larsen, 2017 .

Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization.

Arne Schousboe, A. Schousboe, P. Krogsgaard‐Larsen, 2013, Journal of medicinal chemistry.

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

D. Gloriam, B. Rolando, D. Boschi, 2019, Journal of medicinal chemistry.

GHB receptor targets in the CNS: focus on high-affinity binding sites.

P. Wellendorph, T. Bay, A. Klein, 2014, Biochemical pharmacology.

Specific γ‐hydroxybutyrate‐binding sites but loss of pharmacological effects of γ‐hydroxybutyrate in GABAB(1)‐deficient mice

J. Cryan, B. Bettler, W. Froestl, 2003 .

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

P. Wellendorph, H. Bräuner‐Osborne, G. V. van Woerden, 2022, Journal of pharmacological and toxicological methods.

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

J. Olsen, J. Kuriyan, D. Kerr, 2021, Proceedings of the National Academy of Sciences.

Development of a Robust Mammalian Cell‐based Assay for Studying Recombinant α4β1/3δ GABAA Receptor Subtypes

K. Madsen, P. Wellendorph, B. Frølund, 2017, Basic & clinical pharmacology & toxicology.

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

S. Shuto, G. Ecker, P. Wellendorph, 2021, Frontiers in Chemistry.

Cyanohydrin glycosides of Passiflora: distribution pattern, a saturated cyclopentane derivative from P. guatemalensis, and formation of pseudocyanogenic alpha-hydroxyamides as isolation artefacts.

B. Budnik, J. Jaroszewski, L. B. Jørgensen, 2002, Phytochemistry.

Molecular basis for amino acid sensing by family C G‐protein‐coupled receptors

P. Wellendorph, H. Bräuner‐Osborne, 2009, British journal of pharmacology.

Tuning Wasp Toxin Structure for Nicotinic Receptor Antagonism: Cyclohexylalanine‐Containing Analogues as Potent and Voltage‐Dependent Blockers

M. Witt, J. Jaroszewski, C. Olsen, 2006, ChemMedChem.

Molecular cloning, expression, and sequence analysis of GPRC6A, a novel family C G-protein-coupled receptor.

P. Wellendorph, H. Bräuner‐Osborne, 2004, Gene.

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

A. Clarkson, P. Wellendorph, R. Clausen, 2018, Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.

The rat GPRC6A: cloning and characterization.

P. Wellendorph, H. Bräuner‐Osborne, H. Schmale, 2007, Gene.

The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABAA Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform

T. Rades, S. Okonogi, A. Müllertz, 2022, Pharmaceutics.

Binding effects of Alpinia galanga oil and its nanoemulsion 1 to GABAA receptors in rat cortical membranes

T. Rades, S. Okonogi, A. Müllertz, 2021 .

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

P. Wellendorph, B. Frølund, M. Shehata, 2022, Journal of medicinal chemistry.

New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.

J. Kehler, C. Bundgaard, P. Wellendorph, 2013, Journal of medicinal chemistry.

Novel high-affinity and selective biaromatic 4-substituted gamma-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies.

Hans Bräuner-Osborne, P. Wellendorph, B. Frølund, 2008, Journal of medicinal chemistry.

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

A. Schousboe, P. Wellendorph, Jens V. Andersen, 2023, Essays in biochemistry.

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

A. Schousboe, L. Pinborg, L. K. Bak, 2020, Glia.

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

N. O. Dalby, A. Clarkson, P. Wellendorph, 2017, Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.

Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3.

G. Ecker, P. Wellendorph, B. Frølund, 2015, ACS chemical neuroscience.

GHB confers neuroprotection by stabilizing the CaMKIIα hub domain

J. Olsen, J. Kuriyan, D. Kerr, 2020, bioRxiv.

The GPCR, class C, group 6, subtype A (GPRC6A) receptor: from cloning to physiological function

P. Wellendorph, C. Clemmensen, H. Bräuner‐Osborne, 2014, British journal of pharmacology.

(1S, 3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a potent γ-aminobutyric acid aminotransferase inactivator for the treatment of cocaine addiction.

J. Brodie, A. Schousboe, C. Craft, 2012, Journal of medicinal chemistry.

Pharmacological characterisation of murine α4β1δ GABAA receptors expressed in Xenopus oocytes

T. Smart, P. Wellendorph, I. S. Villumsen, 2015, BMC Neuroscience.

A sequential high-yielding large-scale solution-method for synthesis of philanthotoxin analogues.

S. Hansen, J. Jaroszewski, H. Franzyk, 2003, European journal of medicinal chemistry.

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

G. Ecker, P. Wellendorph, B. Frølund, 2020, Scientific Reports.

The GHB analogue HOCPCA improves sensorimotor function after MCAO via CaMKIIα

Heung-Chin Cheng, D. Vivien, A. Clarkson, 2022, bioRxiv.

Genetic Variations in the Human G Protein-coupled Receptor Class C, Group 6, Member A (GPRC6A) Control Cell Surface Expression and Function*

T. Hansen, O. Pedersen, N. Grarup, 2016, The Journal of Biological Chemistry.

3-Hydroxy-2'-methoxy-6-methylflavone: a potent anxiolytic with a unique selectivity profile at GABA(A) receptor subtypes.

J. Hanrahan, Navnath S. Gavande, P. Wellendorph, 2011, Biochemical pharmacology.

The l-α-amino acid receptor GPRC6A is expressed in the islets of Langerhans but is not involved in l-arginine-induced insulin release

J. Holst, P. Thams, P. Wellendorph, 2013, Amino Acids.

Specific gamma-hydroxybutyrate-binding sites but loss of pharmacological effects of gamma-hydroxybutyrate in GABA(B)(1)-deficient mice.

J. Cryan, B. Bettler, W. Froestl, 2003, The European journal of neuroscience.

Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H(3) receptor.

D. Weiner, M. Brann, N. Nash, 2002, Neuropharmacology.

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

C. Bundgaard, U. Kristiansen, P. Wellendorph, 2021, Journal of medicinal chemistry.

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

C. Sobey, Heung-Chin Cheng, D. Vivien, 2023, Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.

Potency of GABA at human recombinant GABAA receptors expressed in Xenopus oocytes: a mini review

J. Hanrahan, N. Absalom, P. Wellendorph, 2013, Amino Acids.

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

P. Wellendorph, B. Frølund, A. Marek, 2020 .

Autoradiographic imaging and quantification of the high-affinity GHB binding sites in rodent brain using 3H-HOCPCA

G. Knudsen, P. Wellendorph, B. Frølund, 2016, Neurochemistry International.

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

P. Wellendorph, M. Herth, A. Klein, 2019, Journal of visualized experiments : JoVE.

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

C. Bundgaard, U. Kristiansen, D. Gloriam, 2020, Scientific Reports.

Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)

P. Wellendorph, B. Frølund, R. Clausen, 2014, Neurochemical Research.

Novel cyclic gamma-hydroxybutyrate (GHB) analogs with high affinity and stereoselectivity of binding to GHB sites in rat brain.

J. Greenwood, P. Wellendorph, B. Frølund, 2005, The Journal of pharmacology and experimental therapeutics.

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

N. O. Dalby, P. Scholze, P. Wellendorph, 2020, British journal of pharmacology.

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

P. Wellendorph, B. Kornum, C. Falk-Petersen, 2021, The European journal of neuroscience.

Kinase activity simultaneously determines the constitutive and the orthosteric gating in α4β1/3δ GABAA receptors in hippocampal granule cells

N. O. Dalby, P. Scholze, P. Wellendorph, 2018, bioRxiv.

Molecular Pharmacology of Promiscuous Seven Transmembrane Receptors Sensing Organic Nutrients

P. Wellendorph, H. Bräuner‐Osborne, L. D. Johansen, 2009, Molecular Pharmacology.

(1S, 3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a potent γ-aminobutyric acid aminotransferase inactivator for the treatment of cocaine addiction.

J. Brodie, A. Schousboe, C. Craft, 2012, Journal of medicinal chemistry.

David E. Gloriam, D. Gloriam, P. Krogsgaard‐Larsen, 2013, Journal of medicinal chemistry.

3-Hydroxy-2'-methoxy-6-methylflavone: a potent anxiolytic with a unique selectivity profile at GABA(A) receptor subtypes.

J. Hanrahan, Navnath S. Gavande, P. Wellendorph, 2011, Biochemical pharmacology.

GABA transport cycle: beyond a GAT feeling

P. Wellendorph, A. Shahsavar, 2023, Nature Structural & Molecular Biology.

The emerging role of promiscuous 7TM receptors as chemosensors for food intake.

P. Wellendorph, H. Bräuner‐Osborne, L. D. Johansen, 2010, Vitamins and hormones.

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

C. Bundgaard, P. Wellendorph, B. Frølund, 2017, ACS chemical neuroscience.

Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)

P. Wellendorph, B. Frølund, R. Clausen, 2014, Neurochemical Research.

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

A. Dufour, G. Ciccotosto, R. Medcalf, 2023, Molecular & cellular proteomics : MCP.

N-Terminomic Changes of Neurons During Excitotoxicity Reveals Proteolytic Events Associated with Synaptic Dysfunctions and Potential Targets for Neuroprotection Graphical Abstract Authors

Heung-Chin Cheng, Prasad N. Paradkar, C. Ang, 2022 .

Transmembrane transporter proteins: Capturing transport in motion

U. Gether, C. Loland, P. Wellendorph, 2023, Basic & clinical pharmacology & toxicology.

In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1

J. Kehler, C. Bundgaard, P. Wellendorph, 2015, The Journal of Pharmacology and Experimental Therapeutics.

Ways of modulating GABA transporters to treat neurological disease.

P. Wellendorph, Jonas S. Mortensen, Amalie N L Mikkelsen, 2024, Expert opinion on therapeutic targets.

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

P. Wellendorph, B. Frølund, F. Bavo, 2023, Medicinal Chemistry Research.

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

P. Wellendorph, B. Aldana, Emil W. Westi, 2024, Glia.

The GPCR, class C, group 6, subtype A (GPRC6A) receptor: from cloning to physiological function

P. Wellendorph, C. Clemmensen, H. Bräuner‐Osborne, 2014, British journal of pharmacology.

Rodent ischemic stroke models and their relevance in preclinical research

P. Wellendorph, Andrew N. Clarkson, Maria Thaysen, 2024, Neuroprotection.

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

J. Kastrup, P. Wellendorph, Sara M. Ø. Solbak, 2024, Protein science : a publication of the Protein Society.