Rasmus Prætorius Clausen
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
- 2023
- Published
In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs
Bechthold, E., Grey, L., Diamant, E., Schmidt, J., Steigerwald, R., Zhao, F., Hansen, K. B., Bunch, Lennart, Clausen, Rasmus Prætorius & Wünsch, B., 2023, In: Biological Chemistry. 404, 4, p. 255-265Research output: Contribution to journal › Journal article › Research › peer-review
- 2022
- Published
Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity
Zhao, F., Atxabal, U., Mariottini, S., Yi, F., Lotti, J. S., Rouzbeh, N., Liu, N., Bunch, Lennart, Hansen, K. B. & Clausen, Rasmus Prætorius, 2022, In: Journal of Medicinal Chemistry. 65, 1, p. 734-746Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Discovery of (R)-2-amino-3-triazolpropanoic acid derivatives as NMDA receptor glycine site agonists with GluN2 subunit-specific activity
Zhao, F., Mazis, G., Yi, F., Lotti, J. S., Layeux, M. S., Schultz, E. P., Bunch, Lennart, Hansen, K. B. & Clausen, Rasmus Prætorius, 2022, In: Frontiers in Chemistry. 10, 13 p., 1008233.Research output: Contribution to journal › Journal article › Research › peer-review
- 2021
- Published
Artificial Intelligence and Cheminformatics-Guided Modern Privileged Scaffold Research
Qiu, H., Clausen, Rasmus Prætorius, He, Y. & Zhu, H., 2021, In: Current Topics in Medicinal Chemistry. 21, 28, p. 2593-2608Research output: Contribution to journal › Review › Research › peer-review
- Published
Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery
Clementson, S., Matheu, S. A., Marcher, Emil, Pedersen, H., Jensen, Anders A., Clausen, Rasmus Prætorius, Vital, P., Glibstrup, E., Jessing, M. & Kristensen, Jesper Langgaard, 2021, In: The Journal of Organic Chemistry. 86, 12, p. 8248-8262Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Facilitation of GluN2C-containing NMDA receptors in the external globus pallidus increases firing of fast spiking neurons and improves motor function in a hemiparkinsonian mouse model
Liu, J., Shelkar, G. P., Sarode, L. P., Gawande, D. Y., Zhao, F., Clausen, Rasmus Prætorius, Ugale, R. R. & Dravid, S. M., 2021, In: Neurobiology of Disease. 150, 10 p., 105254.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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, , 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
- Published
Organic osmolytes increase expression of specific tight junction proteins in skin and alter barrier function in keratinocytes
El-Chami, C., Foster, A. R., Johnson, C., Clausen, Rasmus Prætorius, Cornwell, P., Haslam, I. S., Steward, M. C., Watson, R. E. B., Young, H. S. & O'Neill, C. A., 2021, In: British Journal of Dermatology. 184, 3, p. 482-494Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Stereoselective synthesis of novel 2′-(S)-CCG-IV analogues as potent NMDA receptor agonists
Maolanon, A., Papangelis, A., Kawiecki, D., Mou, T. C., Syrenne, J. T., Yi, F., Hansen, K. B. & Clausen, Rasmus Prætorius, 2021, In: European Journal of Medicinal Chemistry. 212, 17 p., 113099.Research output: Contribution to journal › Journal article › Research › peer-review
- 2020
- Published
Improved synthetic route for the GluN2-specific NMDA receptor glycine site agonist AICP
Zhao, F., Rouzbeh, N., Hansen, K. B. & Clausen, Rasmus Prætorius, 31 Mar 2020, In: Tetrahedron Letters. 61, 12, 4 p., 151653.Research output: Contribution to journal › Letter › Research › peer-review
- Published
Compounds for the treatment of acute brain injury
Klein, A. B., Leurs, U., Houlton, J., Clausen, Rasmus Prætorius, Frølund, Bente, Clarkson, A. & Wellendorph, Petrine, 2020, Patent No. CN111989094, 24 Nov 2020, Priority date 1 Feb 2019, Priority No. PCT/DK2019/050041Research output: Patent
- Published
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, Rasmus Prætorius, Schousboe, Arne, White, H. S. & Wellendorph, Petrine, 2020, In: Neurochemical Research. 45, p. 1551–1565Research output: Contribution to journal › Journal article › Research › peer-review
- 2019
- Published
Modulation of burst firing of neurons in nucleus reticularis of the thalamus by GluN2C-containing NMDA receptors
Liu, J., Shelkar, G. P., Zhao, F., Clausen, Rasmus Prætorius & Dravid, S. M., 2019, In: Molecular Pharmacology. 96, p. 193-203Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Use of the 4-Hydroxy-Triazole Moiety as a Bioisosteric Tool for the Development of Ionotropic Glutamate Receptor Ligands
Sainas, S., Temperini, P., Farnsworth, J. C., Yi, F., Møllerud, S., Jensen, Anders A., Nielsen, Birgitte, Kastrup, Jette Sandholm Jensen, Hansen, K. B., Boschi, D., Pickering, Darryl S, Clausen, Rasmus Prætorius & Lolli, M., 2019, In: Journal of Medicinal Chemistry. 62, p. 4467-4482Research output: Contribution to journal › Journal article › Research › peer-review
- 2018
- Published
Elucidation of fluorine's impact on pKa and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors
Fjelbye, K., Marigo, M., Clausen, Rasmus Prætorius, Jørgensen, E. B., Christoffersen, C. T. & Juhl, K., 2018, In: MedChemComm. 9, 5, p. 893-896 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Inhibition of GABA transporters fails to afford significant protection following focal cerebral ischemia
Lie, M. E., Gowing, E. K., Clausen, Rasmus Prætorius, Wellendorph, Petrine & Clarkson, A. N., 2018, In: Journal of Cerebral Blood Flow and Metabolism. 38, 1, p. 166-173Research output: Contribution to journal › Journal article › Research › peer-review
- 2017
- Published
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1)
Jørgensen, L., Al-Khawaja, A., Kickinger, S., Vogensen, S. B., Skovgaard-Petersen, J., Rosenthal, E., Borkar, N., Löffler, R., Madsen, K. K., Bräuner, Hans, Schousboe, Arne, Ecker, G. F., Wellendorph, Petrine & Clausen, Rasmus Prætorius, 9 Oct 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 8834-8846Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites
Maolanon, A. R., Risgaard, R., Wang, S. Y., Snoep, Y., Papangelis, A., Yi, F., Holley, D., Barslund, A. F., Svenstrup, N., Hansen, K. B. & Clausen, Rasmus Prætorius, 16 Aug 2017, In: ACS Chemical Neuroscience. 8, 8, p. 1681-1687 7 p.Research output: Contribution to journal › Letter › Research › peer-review
- Published
Identification of AICP as a GluN2C-Selective N-Methyl-d-Aspartate Receptor Superagonist at the GluN1 Glycine Site
Jessen, M., Frederiksen, K., Yi, F., Clausen, Rasmus Prætorius, Hansen, K. B., Bräuner, Hans, Kilburn, J. P. & Damholt, A., Aug 2017, In: Molecular Pharmacology. 92, 2, p. 151-161 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Radiosynthesis and Evaluation of [(11)C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ-Hydroxybutyric Acid Binding Sites
Jensen, C. H., Hansen, H. D., Bay, T., Vogensen, S. B., Lehel, S., Thiesen, L., Bundgaard, C., Clausen, Rasmus Prætorius, Knudsen, Gitte Moos, Herth, Matthias Manfred, Wellendorph, Petrine & Frølund, Bente, 18 Jan 2017, In: A C S Chemical Neuroscience. 8, 1, p. 22-27 6 p.Research output: Contribution to journal › Letter › Research › peer-review
- Published
Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs
Schousboe, Arne, Wellendorph, Petrine, Frølund, Bente, Clausen, Rasmus Prætorius & Krogsgaard-Larsen, Povl, 2017, Glial Amino Acid Transporters. Springer, Vol. 16. p. 283-296 14 p. (Advances in Neurobiology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Communication
- Published
Development of Non-GAT1-Selective Inhibitors: Challenges and Achievements
Damgaard, M., Haugaard, A. S., Kickinger, S., Al-Khawaja, A., Lie, M. E. K., Ecker, G. F., Clausen, Rasmus Prætorius & Frølund, Bente, 2017, Advances in Neurobiology. Springer, Vol. 16. p. 315-332 18 p. (Advances in Neurobiology).Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
- Published
Enantioselective Fluorination of Spirocyclic β-Prolinals Using Enamine Catalysis
Fjelbye, K., Marigo, M., Clausen, Rasmus Prætorius & Juhl, K., 2017, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 28, 4, p. 425-428 4 p., st-2016-b0535-l.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
Krall, J., Jensen, C. H., Bavo, F., Falk-Petersen, C. B., Haugaard, A. S., Vogensen, S. B., Tian, Y., Nittegaard-Nielsen, M., Sigurdardóttir, S. B., Kehler, J., Kongstad, Kenneth Thermann, Gloriam, David E., Clausen, Rasmus Prætorius, Harpsøe, Kasper, Wellendorph, Petrine & Frølund, Bente, 2017, In: Journal of Medicinal Chemistry. 60, 21, p. 9022-9039 18 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Preparation of Spirocyclic β-Proline Esters: Geometrically Restricted Building Blocks for Medicinal Chemistry
Fjelbye, K., Marigo, M., Clausen, Rasmus Prætorius & Juhl, K., 2017, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 28, 2, p. 231-234 4 p., st-2016-b0534-l.Research output: Contribution to journal › Review › Research › peer-review
- Published
gamma-Aminobutyric Acid and Glycine Neurotransmitter Transporters
Wellendorph, Petrine, Jacobsen, Julie, Skovgaard-Petersen, J., Jurik, A., Vogensen, S. B., Ecker, G., Schousboe, Arne, Krogsgaard-Larsen, Povl & Clausen, Rasmus Prætorius, 2017, Transporters As Drug Targets.Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
- 2016
- Published
Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor
Giacoboni, J., Clausen, Rasmus Prætorius & Marigo, M., Dec 2016, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 27, 20, p. 2803-2806 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Autoradiographic imaging and quantification of the high-affinity GHB binding sites in rodent brain using (3)H-HOCPCA
Klein, A. B., Bay, T., Villumsen, I. S., Falk-Petersen, C. B., Marek, A., Frølund, Bente, Clausen, Rasmus Prætorius, Hansen, H. D., Knudsen, Gitte Moos & Wellendorph, Petrine, Nov 2016, In: Neurochemistry International. 100, p. 138-145 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
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
Marek, A., Pedersen, M. H. F., Vogensen, S. B., Clausen, Rasmus Prætorius, Frølund, Bente & Elbert, T., Oct 2016, In: Journal of Labelled Compounds and Radiopharmaceuticals. 59, 12, p. 476-483 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain
Clausen, Rasmus Prætorius, Mohr, A. Ø., Riise, E., Jensen, Anders A., Gill, A., Madden, D. R., Kastrup, Jette Sandholm Jensen & Skottrup, P. D., 8 Jul 2016, In: International Journal of Biological Macromolecules. 92, p. 779-787 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Positive allosteric modulation of AMPA receptors differentially modulates the behavioural effects of citalopram in mouse models of antidepressant and anxiolytic action
Fitzpatrick, C. M., Larsen, M., Madsen, L., Pickering, Darryl S, Clausen, Rasmus Prætorius & Andreasen T., Jesper, 26 Jun 2016, In: Behavioural Pharmacology. 27, 6, p. 549-555 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C
Nielsen, S. D., Leurs, U., Bergner, M., Barris, S. A., Devkota, K., Meyer, K., Iaria, D., McCaughan, J., Lohse, B., Kristensen, Jesper Langgaard & Clausen, Rasmus Prætorius, 13 Jun 2016, In: Protein and Peptide Letters. 23, 9, p. 772 - 776 5 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 Receptors
Kristensen, Anders Skov, Hansen, K. B., Naur, P., Olsen, L., Kurtkaya, N. L., Dravid, S. M., Kvist, T., Yi, F., Pøhlsgaard, J., Clausen, Rasmus Prætorius, Gajhede, Michael, Kastrup, Jette Sandholm Jensen & Traynelis, S. F., Feb 2016, In: Molecular Pharmacology. 89, 2, p. 253-262 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Diastereodivergent Access to Syn and Anti 3,4-Substituted β-Fluoropyrrolidines: Enhancing or Reversing Substrate Preference
Fjelbye, K., Marigo, M., Clausen, Rasmus Prætorius & Juhl, K., 2016, In: Organic Letters. 18, 5, p. 1170-1173 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Opioid and cannabinoid receptors
Clausen, Rasmus Prætorius & Hansen, Harald S., 2016, Textbook of drug design and discovery. 5. ed. CRC Press, p. 329-346Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
- Published
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
Wang, S., Larsen, Y., Navarrete, C. V., Jensen, Anders A., Nielsen, Birgitte, Al-Musaed, A., Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen, Pickering, Darryl S & Clausen, Rasmus Prætorius, 2016, In: Journal of Medicinal Chemistry. 59, 5, p. 2244-2254 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2015
- Published
Structure activity relationship of selective GABA uptake inhibitors
Vogensen, S. B., Jørgensen, L., Madsen, K. K., Jurik, A., Borkar, N., Rosatelli, E., Nielsen, Birgitte, Ecker, G. F., Schousboe, Arne & Clausen, Rasmus Prætorius, 15 May 2015, In: Bioorganic & Medicinal Chemistry. 23, 10, p. 2480-2488 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Differential role of AMPA receptors in mouse tests of antidepressant and anxiolytic action
Andreasen T., Jesper, Fitzpatrick, C. M., Larsen, M., Skovgaard, L., Nielsen, S. D., Clausen, Rasmus Prætorius, Troelsen, K. & Pickering, Darryl S, 19 Mar 2015, In: Brain Research. 1601, p. 117-26 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
A fluorescence resonance energy transfer-based method for histone methyltransferases
Devkota, K., Lohse, B., Nyby Jakobsen, C., Berthelsen, J. & Clausen, Rasmus Prætorius, 19 Feb 2015, In: Analytical Biochemistry. 476, p. 78-80 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
P2X7 receptor-mediated analgesia in cancer-induced bone pain
Falk, S., D. Schwab, S., Frøsig-Jørgensen, M., Clausen, Rasmus Prætorius, Dickenson, A. & Heegaard, Anne-Marie, 13 Feb 2015, In: Neuroscience. 291, p. 93–105 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Identification of the first highly selective inhibitor of human GABA transporter GAT3
Damgaard, M., Al-Khawaja, A., Vogensen, S. B., Jurik, A., Sijm, M., Lie, M., Bæk, M. I., Rosenthal, E., Jensen, Anders A., Ecker, G. F., Frølund, Bente, Wellendorph, Petrine & Clausen, Rasmus Prætorius, 2015, In: A C S Chemical Neuroscience. 6, p. 1591-1599 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
In vitro and in vivo evidence for active brain uptake of the GHB analogue HOCPCA by the monocarboxylate transporter subtype 1
Thiesen, L., Kehler, J., Clausen, Rasmus Prætorius, Frølund, Bente, Bundgaard, C. & Wellendorph, Petrine, 2015, In: Journal of Pharmacology and Experimental Therapeutics. 354, 2, p. 166-174 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- 2014
- Published
Dissecting the Binding Mode of Low Affinity Phage Display Peptide Ligands to Protein Targets by Hydrogen/Deuterium Exchange Coupled to Mass Spectrometry
Leurs, U., Lohse, B., Ming, S. A., Cole, P. A., Clausen, Rasmus Prætorius, Kristensen, Jesper Langgaard & Rand, Kasper Dyrberg, 17 Oct 2014, In: Analytical Chemistry. 86, 23, p. 11734-11741 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Substrate- and Cofactor-independent Inhibition of Histone Demethylase KDM4C
Leurs, U., Lohse, B., Rand, Kasper Dyrberg, Ming, S., Riise, E. S., Cole, P. A., Kristensen, Jesper Langgaard & Clausen, Rasmus Prætorius, 11 Jul 2014, In: A C S Chemical Biology. 9, 9, p. 2131-2138 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Pharmacological Identification of a Guanidine-Containing β-Alanine Analogue with Low Micromolar Potency and Selectivity for the Betaine/GABA Transporter 1 (BGT1)
Al-Khawaja, A. M. A., Petersen, J. G., Damgaard, M., Jensen, M. H., Vogensen, S. B., Lie, M. E. K., Kragholm, B., Bräuner, Hans, Clausen, Rasmus Prætorius, Frølund, Bente & Wellendorph, Petrine, 23 May 2014, In: Neurochemical Research. 39, 10, p. 1988-1996 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization
Jørgensen, L., Nielsen, Birgitte, Pickering, Darryl S, Kristensen, Anders Skov, Frydenvang, Karla Andrea, Madsen, Ulf & Clausen, Rasmus Prætorius, 2014, In: Neurochemical Research. 39, 10, p. 1895-1905 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2
Devkota, K., Lohse, B., Liu, Q., Wang, M., Stærk, Dan, Berthelsen, J. & Clausen, Rasmus Prætorius, 2014, In: A C S Medicinal Chemistry Letters. 5, 4, p. 293-297Research output: Contribution to journal › Letter › Research › peer-review
- 2013
- Published
Chemoenzymatic synthesis and in situ application of S-adenosyl-L-methionine analogs
Thomsen, M., Vogensen, S. B., Buchardt, J., Burkart, M. D. & Clausen, Rasmus Prætorius, 21 Nov 2013, In: Organic & Biomolecular Chemistry. 11, 43, p. 7606-7610Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Posttranslational Modifications of the Histone 3 Tail and Their Impact on the Activity of Histone Lysine Demethylases In Vitro
Lohse, B., Helgstrand, C., Andersson, J. L., Leurs, U., Cloos, P. A. C., Kristensen, Jesper Langgaard & Clausen, Rasmus Prætorius, 2 Jul 2013, In: P L o S One. 8, 7, p. e67653Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Structural determinants of agonist efficacy at the glutamate binding site of N-methyl-D-aspartate receptors
Hansen, K. B., Tajima, N., Risgaard, R., Perszyk, R. E., Jørgensen, L., Vance, K. M., Ogden, K. K., Clausen, Rasmus Prætorius, Furukawa, H. & Traynelis, S. F., Jul 2013, In: Molecular Pharmacology. 84, 1, p. 114-127Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302218