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

Liu J, Shelkar GP, Zhao F, Clausen RP, Dravid SM.

Mol Pharmacol. 2019 Jun 3. pii: mol.119.116780. doi: 10.1124/mol.119.116780. [Epub ahead of print]


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

Sainas S, Temperini P, Farnsworth JC, Yi F, Møllerud S, Jensen AA, Nielsen B, Passoni A, Kastrup JS, Hansen KB, Boschi D, Pickering DS, Clausen RP, Lolli ML.

J Med Chem. 2019 May 9;62(9):4467-4482. doi: 10.1021/acs.jmedchem.8b01986. Epub 2019 Apr 18.


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

Fjelbye K, Marigo M, Clausen RP, Jørgensen EB, Christoffersen CT, Juhl K.

Medchemcomm. 2018 Apr 28;9(5):893-896. doi: 10.1039/c8md00114f. eCollection 2018 May 1.


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

Lie ME, Gowing EK, Clausen RP, Wellendorph P, Clarkson AN.

J Cereb Blood Flow Metab. 2018 Jan;38(1):166-173. doi: 10.1177/0271678X17743669. Epub 2017 Nov 17.


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 CH, Bavo F, Falk-Petersen CB, Haugaard AS, Vogensen SB, Tian Y, Nittegaard-Nielsen M, Sigurdardóttir SB, Kehler J, Kongstad KT, Gloriam DE, Clausen RP, Harpsøe K, Wellendorph P, Frølund B.

J Med Chem. 2017 Nov 9;60(21):9022-9039. doi: 10.1021/acs.jmedchem.7b01351. Epub 2017 Oct 30.


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 SB, Skovgaard-Petersen J, Rosenthal E, Borkar N, Löffler R, Madsen KK, Bräuner-Osborne H, Schousboe A, Ecker GF, Wellendorph P, Clausen RP.

J Med Chem. 2017 Nov 9;60(21):8834-8846. doi: 10.1021/acs.jmedchem.7b00924. Epub 2017 Oct 19.


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

Damgaard M, Haugaard AS, Kickinger S, Al-Khawaja A, Lie MEK, Ecker GF, Clausen RP, Frølund B.

Adv Neurobiol. 2017;16:315-332. doi: 10.1007/978-3-319-55769-4_16. Review.


Astrocytic GABA Transporters: Pharmacological Properties and Targets for Antiepileptic Drugs.

Schousboe A, Wellendorph P, Frølund B, Clausen RP, Krogsgaard-Larsen P.

Adv Neurobiol. 2017;16:283-296. doi: 10.1007/978-3-319-55769-4_14. Review.


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 RP, Hansen KB, Bräuner-Osborne H, Kilburn P, Damholt A.

Mol Pharmacol. 2017 Aug;92(2):151-161. doi: 10.1124/mol.117.108944. Epub 2017 Jun 6. Erratum in: Mol Pharmacol. 2018 Oct;94(4):1101-1102.


Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites.

Maolanon AR, Risgaard R, Wang SY, Snoep Y, Papangelis A, Yi F, Holley D, Barslund AF, Svenstrup N, Hansen KB, Clausen RP.

ACS Chem Neurosci. 2017 Aug 16;8(8):1681-1687. doi: 10.1021/acschemneuro.7b00117. Epub 2017 May 30.


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

Jensen CH, Hansen HD, Bay T, Vogensen SB, Lehel S, Thiesen L, Bundgaard C, Clausen RP, Knudsen GM, Herth MM, Wellendorph P, Frølund B.

ACS Chem Neurosci. 2017 Jan 18;8(1):22-27. doi: 10.1021/acschemneuro.6b00335. Epub 2016 Nov 17.


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

Klein AB, Bay T, Villumsen IS, Falk-Petersen CB, Marek A, Frølund B, Clausen RP, Hansen HD, Knudsen GM, Wellendorph P.

Neurochem Int. 2016 Nov;100:138-145. doi: 10.1016/j.neuint.2016.09.002. Epub 2016 Sep 8.


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 MH, Vogensen SB, Clausen RP, Frølund B, Elbert T.

J Labelled Comp Radiopharm. 2016 Oct;59(12):476-483. doi: 10.1002/jlcr.3432. Epub 2016 Sep 4.


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

Clausen RP, Mohr AØ, Riise E, Jensen AA, Gill A, Madden DR, Kastrup JS, Skottrup PD.

Int J Biol Macromol. 2016 Nov;92:779-787. doi: 10.1016/j.ijbiomac.2016.07.026. Epub 2016 Jul 8.


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.

Fitzpatrick CM, Larsen M, Madsen LH, Caballero-Puntiverio M, Pickering DS, Clausen RP, Andreasen JT.

Behav Pharmacol. 2016 Sep;27(6):549-55. doi: 10.1097/FBP.0000000000000243.


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

Nielsen SD, Leurs U, Bergner M, Barris SA, Devkota K, Meyer K, Iaria D, McCaughan J, Lohse B, Kristensen JL, Clausen RP.

Protein Pept Lett. 2016;23(9):772-6.


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

Fjelbye K, Marigo M, Clausen RP, Juhl K.

Org Lett. 2016 Mar 4;18(5):1170-3. doi: 10.1021/acs.orglett.6b00293. Epub 2016 Feb 23.


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 SY, Larsen Y, Navarrete CV, Jensen AA, Nielsen B, Al-Musaed A, Frydenvang K, Kastrup JS, Pickering DS, Clausen RP.

J Med Chem. 2016 Mar 10;59(5):2244-54. doi: 10.1021/acs.jmedchem.5b01982. Epub 2016 Feb 22.


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

Kristensen AS, Hansen KB, Naur P, Olsen L, Kurtkaya NL, Dravid SM, Kvist T, Yi F, Pøhlsgaard J, Clausen RP, Gajhede M, Kastrup JS, Traynelis SF.

Mol Pharmacol. 2016 Feb;89(2):253-62. doi: 10.1124/mol.115.100909. Epub 2015 Dec 10.


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

Damgaard M, Al-Khawaja A, Vogensen SB, Jurik A, Sijm M, Lie ME, Bæk MI, Rosenthal E, Jensen AA, Ecker GF, Frølund B, Wellendorph P, Clausen RP.

ACS Chem Neurosci. 2015 Sep 16;6(9):1591-9. doi: 10.1021/acschemneuro.5b00150. Epub 2015 Jul 23.


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

Thiesen L, Kehler J, Clausen RP, Frølund B, Bundgaard C, Wellendorph P.

J Pharmacol Exp Ther. 2015 Aug;354(2):166-74. doi: 10.1124/jpet.115.224543. Epub 2015 May 18.


Structure activity relationship of selective GABA uptake inhibitors.

Vogensen SB, Jørgensen L, Madsen KK, Jurik A, Borkar N, Rosatelli E, Nielsen B, Ecker GF, Schousboe A, Clausen RP.

Bioorg Med Chem. 2015 May 15;23(10):2480-8. doi: 10.1016/j.bmc.2015.03.060. Epub 2015 Mar 30.


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

Devkota K, Lohse B, Jakobsen CN, Berthelsen J, Clausen RP.

Anal Biochem. 2015 May 1;476:78-80. doi: 10.1016/j.ab.2015.02.012. Epub 2015 Feb 19.


P2X7 receptor-mediated analgesia in cancer-induced bone pain.

Falk S, Schwab SD, Frøsig-Jørgensen M, Clausen RP, Dickenson AH, Heegaard AM.

Neuroscience. 2015 Apr 16;291:93-105. doi: 10.1016/j.neuroscience.2015.02.011. Epub 2015 Feb 14.


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

Andreasen JT, Fitzpatrick CM, Larsen M, Skovgaard L, Nielsen SD, Clausen RP, Troelsen K, Pickering DS.

Brain Res. 2015 Mar 19;1601:117-26. doi: 10.1016/j.brainres.2015.01.001. Epub 2015 Jan 8.


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, Cole PA, Clausen RP, Kristensen JL, Rand KD.

Anal Chem. 2014 Dec 2;86(23):11734-41. doi: 10.1021/ac503137u. Epub 2014 Nov 11.


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

Leurs U, Lohse B, Rand KD, Ming S, Riise ES, Cole PA, Kristensen JL, Clausen RP.

ACS Chem Biol. 2014 Sep 19;9(9):2131-8. doi: 10.1021/cb500374f. Epub 2014 Jul 17.


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

Devkota K, Lohse B, Liu Q, Wang MW, Stærk D, Berthelsen J, Clausen RP.

ACS Med Chem Lett. 2014 Jan 31;5(4):293-7. doi: 10.1021/ml4002503. eCollection 2014 Apr 10.


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, Petersen JG, Damgaard M, Jensen MH, Vogensen SB, Lie ME, Kragholm B, Bräuner-Osborne H, Clausen RP, Frølund B, Wellendorph P.

Neurochem Res. 2014 Oct;39(10):1988-96. doi: 10.1007/s11064-014-1336-9. Epub 2014 May 23.


Analogues of 3-hydroxyisoxazole-containing glutamate receptor ligands based on the 3-hydroxypyrazole-moiety: design, synthesis and pharmacological characterization.

Jørgensen L, Nielsen B, Pickering DS, Kristensen AS, Frydenvang K, Madsen U, Clausen RP.

Neurochem Res. 2014 Oct;39(10):1895-905. doi: 10.1007/s11064-014-1332-0. Epub 2014 May 22.


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

Thomsen M, Vogensen SB, Buchardt J, Burkart MD, Clausen RP.

Org Biomol Chem. 2013 Nov 21;11(43):7606-10. doi: 10.1039/c3ob41702f.


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

Vogensen SB, Marek A, Bay T, Wellendorph P, Kehler J, Bundgaard C, Frølund B, Pedersen MH, Clausen RP.

J Med Chem. 2013 Oct 24;56(20):8201-5. doi: 10.1021/jm4011719. Epub 2013 Oct 4.


Posttranslational modifications of the histone 3 tail and their impact on the activity of histone lysine demethylases in vitro.

Lohse B, Helgstrand C, Kristensen JB, Leurs U, Cloos PA, Kristensen JL, Clausen RP.

PLoS One. 2013 Jul 2;8(7):e67653. doi: 10.1371/journal.pone.0067653. Print 2013.


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

Kragholm B, Kvist T, Madsen KK, Jørgensen L, Vogensen SB, Schousboe A, Clausen RP, Jensen AA, Bräuner-Osborne H.

Biochem Pharmacol. 2013 Aug 15;86(4):521-8. doi: 10.1016/j.bcp.2013.06.007. Epub 2013 Jun 19.


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

Lipson JM, Thomsen M, Moore BS, Clausen RP, La Clair JJ, Burkart MD.

Chembiochem. 2013 May 27;14(8):950-3. doi: 10.1002/cbic.201300221. Epub 2013 May 6.


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

Andreasen JT, Gynther M, Rygaard A, Bøgelund T, Nielsen SD, Clausen RP, Mogensen J, Pickering DS.

Neurosci Lett. 2013 Jun 24;546:6-10. doi: 10.1016/j.neulet.2013.04.045. Epub 2013 May 2.


Structural determinants of agonist efficacy at the glutamate binding site of N-methyl-D-aspartate receptors.

Hansen KB, Tajima N, Risgaard R, Perszyk RE, Jørgensen L, Vance KM, Ogden KK, Clausen RP, Furukawa H, Traynelis SF.

Mol Pharmacol. 2013 Jul;84(1):114-27. doi: 10.1124/mol.113.085803. Epub 2013 Apr 26.


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

Risgaard R, Nielsen SD, Hansen KB, Jensen CM, Nielsen B, Traynelis SF, Clausen RP.

J Med Chem. 2013 May 23;56(10):4071-81. doi: 10.1021/jm400346a. Epub 2013 May 9.


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

Vogensen SB, Jørgensen L, Madsen KK, Borkar N, Wellendorph P, Skovgaard-Petersen J, Schousboe A, White HS, Krogsgaard-Larsen P, Clausen RP.

J Med Chem. 2013 Mar 14;56(5):2160-4. doi: 10.1021/jm301872x. Epub 2013 Feb 27.


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

Leurs U, Clausen RP, Kristensen JL, Lohse B.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5811-3. doi: 10.1016/j.bmcl.2012.07.091. Epub 2012 Aug 2.


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

Mølck C, Harpsøe K, Gloriam DE, Clausen RP, Madsen U, Pedersen LØ, Jimenez HN, Nielsen SM, Mathiesen JM, Bräuner-Osborne H.

Mol Pharmacol. 2012 Nov;82(5):929-37. doi: 10.1124/mol.112.078808. Epub 2012 Aug 16.


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

Absalom N, Eghorn LF, Villumsen IS, Karim N, Bay T, Olsen JV, Knudsen GM, Bräuner-Osborne H, Frølund B, Clausen RP, Chebib M, Wellendorph P.

Proc Natl Acad Sci U S A. 2012 Aug 14;109(33):13404-9. doi: 10.1073/pnas.1204376109. Epub 2012 Jul 2.


Structure-activity relationships for negative allosteric mGluR5 modulators.

Kaae BH, Harpsøe K, Kvist T, Mathiesen JM, Mølck C, Gloriam D, Jimenez HN, Uberti MA, Nielsen SM, Nielsen B, Bräuner-Osborne H, Sauerberg P, Clausen RP, Madsen U.

ChemMedChem. 2012 Mar 5;7(3):440-51. doi: 10.1002/cmdc.201100578. Epub 2012 Jan 20.


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

Lohse B, Nielsen AL, Kristensen JB, Helgstrand C, Cloos PA, Olsen L, Gajhede M, Clausen RP, Kristensen JL.

Angew Chem Int Ed Engl. 2011 Sep 19;50(39):9100-3. doi: 10.1002/anie.201101849. Epub 2011 Aug 25. No abstract available.


Inhibitors of histone demethylases.

Lohse B, Kristensen JL, Kristensen LH, Agger K, Helin K, Gajhede M, Clausen RP.

Bioorg Med Chem. 2011 Jun 15;19(12):3625-36. doi: 10.1016/j.bmc.2011.01.046. Epub 2011 Feb 1. Review.


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

Kristensen JB, Nielsen AL, Jørgensen L, Kristensen LH, Helgstrand C, Juknaite L, Kristensen JL, Kastrup JS, Clausen RP, Olsen L, Gajhede M.

FEBS Lett. 2011 Jun 23;585(12):1951-6. doi: 10.1016/j.febslet.2011.05.023. Epub 2011 May 12. Erratum in: FEBS Lett. 2011 Nov 16;585(22):3600.


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

Skottrup PD, Leonard P, Kaczmarek JZ, Veillard F, Enghild JJ, O'Kennedy R, Sroka A, Clausen RP, Potempa J, Riise E.

Anal Biochem. 2011 Aug 15;415(2):158-67. doi: 10.1016/j.ab.2011.04.015. Epub 2011 Apr 20.


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

Lehre AC, Rowley NM, Zhou Y, Holmseth S, Guo C, Holen T, Hua R, Laake P, Olofsson AM, Poblete-Naredo I, Rusakov DA, Madsen KK, Clausen RP, Schousboe A, White HS, Danbolt NC.

Epilepsy Res. 2011 Jun;95(1-2):70-81. doi: 10.1016/j.eplepsyres.2011.02.014. Epub 2011 Apr 3.


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.

Madsen KK, Ebert B, Clausen RP, Krogsgaard-Larsen P, Schousboe A, White HS.

J Pharmacol Exp Ther. 2011 Jul;338(1):214-9. doi: 10.1124/jpet.111.179671. Epub 2011 Mar 30.


Glutamate receptor agonists: stereochemical aspects.

Vogensen SB, Greenwood JR, Bunch L, Clausen RP.

Curr Top Med Chem. 2011;11(7):887-906. Review.


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