about
A tetrazolyl-substituted subtype-selective AMPA receptor agonistStructural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sitesThe 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 characterizationBiostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acidStructural Determinants of Agonist Efficacy at the Glutamate Binding Site of N-Methyl-D-Aspartate ReceptorsTweaking 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 Analoguesα4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.Structure-activity relationships of selective GABA uptake inhibitors.Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult miceSubstrate- and cofactor-independent inhibition of histone demethylase KDM4C.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.Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C).Novel cyclic gamma-hydroxybutyrate (GHB) analogs with high affinity and stereoselectivity of binding to GHB sites in rat brain.Identification of the First Highly Subtype-Selective Inhibitor of Human GABA Transporter GAT3.Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.Novel high-affinity and selective biaromatic 4-substituted gamma-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies.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.A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain.A novel selective gamma-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS.Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 ReceptorsStructure-activity relationship and pharmacology of gamma-aminobutyric acid (GABA) transport inhibitors.New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.Inhibitors of histone demethylases.P2X7 receptor-mediated analgesia in cancer-induced bone pain.In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1.Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators.Autoradiographic imaging and quantification of the high-affinity GHB binding sites in rodent brain using (3)H-HOCPCA.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.Development of 2'-substituted (2S,1'R,2'S)-2-(carboxycyclopropyl)glycine analogues as potent N-methyl-d-aspartic acid receptor agonists.Dissecting the binding mode of low affinity phage display peptide ligands to protein targets by hydrogen/deuterium exchange coupled to mass spectrometry.A tandem chemoenzymatic methylation by S-adenosyl-L-methionine.Stereocontrolled synthesis and pharmacological evaluation of azetidine-2,3-dicarboxylic acids at NMDA receptorsChemoenzymatic synthesis and in situ application of S-adenosyl-L-methionine analogs.Partial agonists and subunit selectivity at NMDA receptors.Ring opening of pymisyl-protected aziridines with organocuprates.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.Novel radioiodinated {gamma}-hydroxybutyric acid analogues for radiolabeling and Photolinking of high-affinity {gamma}-hydroxybutyric acid binding sites.Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization.Targeting histone lysine demethylases by truncating the histone 3 tail to obtain selective substrate-based inhibitors.
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P50
description
hulumtues
@sq
researcher
@en
ricercatore
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scheikundige
@nl
հետազոտող
@hy
name
Rasmus P. Clausen
@ast
Rasmus P. Clausen
@en
Rasmus P. Clausen
@es
Rasmus P. Clausen
@nl
Rasmus P. Clausen
@sl
type
label
Rasmus P. Clausen
@ast
Rasmus P. Clausen
@en
Rasmus P. Clausen
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Rasmus P. Clausen
@nl
Rasmus P. Clausen
@sl
altLabel
R P Clausen
@en
Rasmus Prætorius Clausen
@en
prefLabel
Rasmus P. Clausen
@ast
Rasmus P. Clausen
@en
Rasmus P. Clausen
@es
Rasmus P. Clausen
@nl
Rasmus P. Clausen
@sl
P227
P244
P1053
A-6812-2008
P1153
7003423087
P21
P214
3909148876456549740006
P227
1126762555
P244
n2017183769
P31
P3829
P3835
rasmus-clausen
P496
0000-0001-9466-9431
P735
P7859
lccn-n2017183769