List of works - Rasmus P. Clausen

A fluorescence resonance energy transfer-based method for histone methyltransferases.

scientific article published on 19 February 2015

A novel selective gamma-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS.

scientific article

A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain

scientific article

A stereochemical anomaly: the cyclised (R)-AMPA analogue (R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid [(R)-5-HPCA] resembles (S)-AMPA at glutamate receptors

scientific article

A tandem chemoenzymatic methylation by S-adenosyl-L-methionine

scientific article published on 6 May 2013

A tetrazolyl-substituted subtype-selective AMPA receptor agonist

scientific article

Aminolysis of Resin-BoundN-Nosylaziridine-2-carboxylic Acids

scientific article published in July 2006

Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization

scientific article published on 22 May 2014

Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.

scientific article

Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs

scientific article

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

scientific article published on 8 September 2016

Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid

scientific article

Chemoenzymatic synthesis and in situ application of S-adenosyl-L-methionine analogs

scientific article published on November 2013

Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.

scientific article published in May 2005

Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult mice

scientific article

Design, synthesis, and in vitro pharmacology of new radiolabeled gamma-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity gamma-hydroxybutyric acid binding sites

scientific article published on September 2010

Development of 2'-substituted (2S,1'R,2'S)-2-(carboxycyclopropyl)glycine analogues as potent N-methyl-d-aspartic acid receptor agonists

scientific article published on 9 May 2013

Development of Non-GAT1-Selective Inhibitors: Challenges and Achievements

scientific article

Diagnostic evaluation of a nanobody with picomolar affinity toward the protease RgpB from Porphyromonas gingivalis

scientific article

Diastereodivergent Access to Syn and Anti 3,4-Substituted β-Fluoropyrrolidines: Enhancing or Reversing Substrate Preference

scientific article published on 23 February 2016

Differential role of AMPA receptors in mouse tests of antidepressant and anxiolytic action.

scientific article

Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.

scientific article

Dissecting the binding mode of low affinity phage display peptide ligands to protein targets by hydrogen/deuterium exchange coupled to mass spectrometry

scientific article published on 11 November 2014

Does increasing the ratio of AMPA-to-NMDA receptor mediated neurotransmission engender antidepressant action? Studies in the mouse forced swim and tail suspension tests

scientific article published on 2 May 2013

Elucidation of fluorine's impact on pKa and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors

scientific article published on 28 April 2018

Enzyme kinetic studies of histone demethylases KDM4C and KDM6A: Towards understanding selectivity of inhibitors targeting oncogenic histone demethylases

article published in 2011

First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2.

scientific article

Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.

scientific article published on 2 August 2007

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

scientific article

Identification of AICP as a GluN2C-Selective N-Methyl-d-Aspartate Receptor Superagonist at the GluN1 Glycine Site

scientific article published on 6 June 2017

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

scientific article

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

scientific article published on 18 May 2015

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

scientific article published in January 2017

Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC)

scientific article

Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C).

scientific article

Inhibitors of histone demethylases

scientific article published on February 2011

Modified peptides as potent inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction

scientific article published on 24 September 2008

Modulation of burst firing of neurons in nucleus reticularis of the thalamus by GluN2C-containing NMDA receptors

scientific article published on 03 June 2019

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) Analog

scientific article

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

scientific article published on 04 October 2013

Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors

scientific article

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

scientific article

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

scientific article

Novel radioiodinated {gamma}-hydroxybutyric acid analogues for radiolabeling and Photolinking of high-affinity {gamma}-hydroxybutyric acid binding sites

scientific article published on 9 August 2010

Organic chemistry at the interface to biology

scientific article published in May 2006

P2X7 receptor-mediated analgesia in cancer-induced bone pain

scientific article

Partial agonists and subunit selectivity at NMDA receptors

scientific article published on December 2010

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

scientific article published on 04 April 2020

Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

scientific article published on 16 August 2012

Pharmacological identification of a guanidine-containing β-alanine analogue with low micromolar potency and selectivity for the betaine/GABA transporter 1 (BGT1).

scientific article

Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 Receptors

scientific article published on 10 December 2015

Positive allosteric modulation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid glutamate receptors differentially modulates the behavioural effects of citalopram in mouse models of antidepressant and anxiolytic action

scientific article published on 23 June 2016

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

scientific article published on 17 November 2016

Ring opening of pymisyl-protected aziridines with organocuprates

scientific article published on November 2010

Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol.

scientific article

Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid

scientific article

Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol analogues

scientific article published in February 2005

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

scientific article published on 27 February 2013

Stereocontrolled synthesis and pharmacological evaluation of azetidine-2,3-dicarboxylic acids at NMDA receptors

scientific article published on January 2009

Stereoselective synthesis of novel 2'-(S)-CCG-IV analogues as potent NMDA receptor agonists

scientific article published on 18 December 2020

Structural Determinants of Agonist Efficacy at the Glutamate Binding Site of N-Methyl-D-Aspartate Receptors

scientific article

Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites

scientific article

Structure activity relationship of selective GABA uptake inhibitors

scientific article published in May 2015

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

scientific article

Structure-activity relationship and pharmacology of gamma-aminobutyric acid (GABA) transport inhibitors.

scientific article published on January 2006

Structure-activity relationships for negative allosteric mGluR5 modulators

scientific article

Structure-activity relationships of selective GABA uptake inhibitors.

scientific article

Substrate- and cofactor-independent inhibition of histone demethylase KDM4C.

scientific article

Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites.

scientific article published on 17 May 2017

Subunit-specific agonist activity at NR2A-, NR2B-, NR2C-, and NR2D-containing N-methyl-D-aspartate glutamate receptors

scientific article published on 10 July 2007

Synaptic and extrasynaptic GABA transporters as targets for anti-epileptic drugs.

scientific article published in May 2009

Synthesis and Characterisation of Substrate-Based Peptides as Inhibitors of Histone Demethylase KDM4C.

scientific article published on 13 June 2016

Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid

scientific article published in February 2007

Targeting histone lysine demethylases by truncating the histone 3 tail to obtain selective substrate-based inhibitors

scientific article published on 25 August 2011

The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization

scientific article

The labeling of unsaturated γ-hydroxybutyric acid by heavy isotopes of hydrogen: iridium complex-mediated H/D exchange by C─H bond activation vs reduction by boro-deuterides/tritides

scientific article published on 4 September 2016

The respective N-hydroxypyrazole analogues of the classical glutamate receptor ligands ibotenic acid and (RS)-2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.

scientific article published in September 2004

The synthesis of 4,4′(5′)-diformyltetrathiafulvalene

Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues

scientific article

Tweaking agonist efficacy at N-methyl-D-aspartate receptors by site-directed mutagenesis.

scientific article published on 30 August 2005

Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands

scientific article published on 18 April 2019

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

scientific article

List of works by Rasmus P. Clausen

A fluorescence resonance energy transfer-based method for histone methyltransferases.

A novel selective gamma-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS.

A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain

A stereochemical anomaly: the cyclised (R)-AMPA analogue (R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid [(R)-5-HPCA] resembles (S)-AMPA at glutamate receptors

A tandem chemoenzymatic methylation by S-adenosyl-L-methionine

A tetrazolyl-substituted subtype-selective AMPA receptor agonist

Aminolysis of Resin-BoundN-Nosylaziridine-2-carboxylic Acids

Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization

Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.

Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs

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

Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid

Chemoenzymatic synthesis and in situ application of S-adenosyl-L-methionine analogs

Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.

Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult mice

Design, synthesis, and in vitro pharmacology of new radiolabeled gamma-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity gamma-hydroxybutyric acid binding sites

Development of 2'-substituted (2S,1'R,2'S)-2-(carboxycyclopropyl)glycine analogues as potent N-methyl-d-aspartic acid receptor agonists

Development of Non-GAT1-Selective Inhibitors: Challenges and Achievements

Diagnostic evaluation of a nanobody with picomolar affinity toward the protease RgpB from Porphyromonas gingivalis

Diastereodivergent Access to Syn and Anti 3,4-Substituted β-Fluoropyrrolidines: Enhancing or Reversing Substrate Preference

Differential role of AMPA receptors in mouse tests of antidepressant and anxiolytic action.

Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.

Dissecting the binding mode of low affinity phage display peptide ligands to protein targets by hydrogen/deuterium exchange coupled to mass spectrometry

Does increasing the ratio of AMPA-to-NMDA receptor mediated neurotransmission engender antidepressant action? Studies in the mouse forced swim and tail suspension tests

Elucidation of fluorine's impact on pKa and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors

Enzyme kinetic studies of histone demethylases KDM4C and KDM6A: Towards understanding selectivity of inhibitors targeting oncogenic histone demethylases

First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2.

Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.

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

Identification of AICP as a GluN2C-Selective N-Methyl-d-Aspartate Receptor Superagonist at the GluN1 Glycine Site

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

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

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

Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC)

Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C).

Inhibitors of histone demethylases

Modified peptides as potent inhibitors of the postsynaptic density-95/N-methyl-D-aspartate receptor interaction

Modulation of burst firing of neurons in nucleus reticularis of the thalamus by GluN2C-containing NMDA receptors

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) Analog

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

Novel 5-substituted 1-pyrazolol analogues of ibotenic acid: synthesis and pharmacology at glutamate receptors

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

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

Novel radioiodinated {gamma}-hydroxybutyric acid analogues for radiolabeling and Photolinking of high-affinity {gamma}-hydroxybutyric acid binding sites

Organic chemistry at the interface to biology

P2X7 receptor-mediated analgesia in cancer-induced bone pain

Partial agonists and subunit selectivity at NMDA receptors

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

Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

Pharmacological identification of a guanidine-containing β-alanine analogue with low micromolar potency and selectivity for the betaine/GABA transporter 1 (BGT1).

Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 Receptors

Positive allosteric modulation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid glutamate receptors differentially modulates the behavioural effects of citalopram in mouse models of antidepressant and anxiolytic action

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

Ring opening of pymisyl-protected aziridines with organocuprates

Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol.

Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid

Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol analogues

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

Stereocontrolled synthesis and pharmacological evaluation of azetidine-2,3-dicarboxylic acids at NMDA receptors

Stereoselective synthesis of novel 2'-(S)-CCG-IV analogues as potent NMDA receptor agonists

Structural Determinants of Agonist Efficacy at the Glutamate Binding Site of N-Methyl-D-Aspartate Receptors

Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites

Structure activity relationship of selective GABA uptake inhibitors

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

Structure-activity relationship and pharmacology of gamma-aminobutyric acid (GABA) transport inhibitors.

Structure-activity relationships for negative allosteric mGluR5 modulators

Structure-activity relationships of selective GABA uptake inhibitors.

Substrate- and cofactor-independent inhibition of histone demethylase KDM4C.

Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites.

Subunit-specific agonist activity at NR2A-, NR2B-, NR2C-, and NR2D-containing N-methyl-D-aspartate glutamate receptors

Synaptic and extrasynaptic GABA transporters as targets for anti-epileptic drugs.

Synthesis and Characterisation of Substrate-Based Peptides as Inhibitors of Histone Demethylase KDM4C.

Synthesis and pharmacology of glutamate receptor ligands: new isothiazole analogues of ibotenic acid

Targeting histone lysine demethylases by truncating the histone 3 tail to obtain selective substrate-based inhibitors

The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization

The labeling of unsaturated γ-hydroxybutyric acid by heavy isotopes of hydrogen: iridium complex-mediated H/D exchange by C─H bond activation vs reduction by boro-deuterides/tritides

The respective N-hydroxypyrazole analogues of the classical glutamate receptor ligands ibotenic acid and (RS)-2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.

The synthesis of 4,4′(5′)-diformyltetrathiafulvalene

Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues