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Items: 1 to 50 of 114

1.

N-(7-(1H-Imidazol-1-yl)-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)benzamide, a New Kainate Receptor Selective Antagonist and Analgesic: Synthesis, X-ray Crystallography, Structure-Affinity Relationships, and in Vitro and in Vivo Pharmacology.

Møllerud S, Hansen RB, Pallesen J, Temperini P, Pasini D, Bornholt J, Nielsen B, Mamedova E, Chalupnik P, Paternain AV, Lerma J, Diaz-delCastillo M, Andreasen JT, Frydenvang K, Kastrup JS, Johansen TN, Pickering DS.

ACS Chem Neurosci. 2019 Nov 20;10(11):4685-4695. doi: 10.1021/acschemneuro.9b00479. Epub 2019 Oct 31.

PMID:
31622082
2.

The Presence of Calcitonin Gene-Related Peptide and Its Receptors in Rat, Pig and Human Brain: Species Differences in Calcitonin Gene-Related Peptide Pharmacology.

Warfvinge K, Edvinsson L, Pickering DS, Sheykhzade M.

Pharmacology. 2019;104(5-6):332-341. doi: 10.1159/000502471. Epub 2019 Sep 4.

3.

Investigating the transient and persistent effects of heat on Clostridium difficile spores.

Pickering DS, Vernon JJ, Freeman J, Wilcox MH, Chilton CH.

J Med Microbiol. 2019 Oct;68(10):1445-1454. doi: 10.1099/jmm.0.001048. Epub 2019 Aug 8.

4.

Design and Synthesis of 2,3- trans-Proline Analogues as Ligands for Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters.

Poulie CBM, Alcaide A, Krell-Jørgensen M, Larsen Y, Astier E, Bjørn-Yoshimoto WE, Yi F, Syrenne JT, Storgaard M, Nielsen B, Frydenvang KA, Jensen AA, Hansen KB, Pickering DS, Bunch L.

ACS Chem Neurosci. 2019 Jun 19;10(6):2989-3007. doi: 10.1021/acschemneuro.9b00205. Epub 2019 May 24.

PMID:
31124660
5.

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.

PMID:
30943028
6.

N1-Substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists: X-ray Crystallography, Structure-Affinity Relationships, and in Vitro Pharmacology.

Pallesen J, Møllerud S, Frydenvang K, Pickering DS, Bornholdt J, Nielsen B, Pasini D, Han L, Marconi L, Kastrup JS, Johansen TN.

ACS Chem Neurosci. 2019 Mar 20;10(3):1841-1853. doi: 10.1021/acschemneuro.8b00726. Epub 2019 Jan 23.

PMID:
30620174
7.

Biofilm-derived spores of Clostridioides (Clostridium) difficile exhibit increased thermotolerance compared to planktonic spores.

Pickering DS, Wilcox MH, Chilton CH.

Anaerobe. 2018 Dec;54:169-171. doi: 10.1016/j.anaerobe.2018.10.003. Epub 2018 Oct 5.

8.

Vascular and molecular pharmacology of the metabolically stable CGRP analogue, SAX.

Sheykhzade M, Abdolalizadeh B, Koole C, Pickering DS, Dreisig K, Johansson SE, Abboud BK, Dreier R, Berg JO, Jeppesen JL, Sexton PM, Edvinsson L, Wootten D, Sams A.

Eur J Pharmacol. 2018 Jun 15;829:85-92. doi: 10.1016/j.ejphar.2018.04.007. Epub 2018 Apr 10.

PMID:
29653090
9.

( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.

Brogi S, Brindisi M, Butini S, Kshirsagar GU, Maramai S, Chemi G, Gemma S, Campiani G, Novellino E, Fiorenzani P, Pinassi J, Aloisi AM, Gynther M, Venskutonytė R, Han L, Frydenvang K, Kastrup JS, Pickering DS.

J Med Chem. 2018 Mar 8;61(5):2124-2130. doi: 10.1021/acs.jmedchem.8b00099. Epub 2018 Feb 26.

PMID:
29451794
10.

Investigating the effect of supplementation on Clostridioides (Clostridium) difficile spore recovery in two solid agars.

Pickering DS, Vernon JJ, Freeman J, Wilcox MH, Chilton CH.

Anaerobe. 2018 Apr;50:38-43. doi: 10.1016/j.anaerobe.2018.01.010. Epub 2018 Feb 1.

11.

Microbiologic factors affecting Clostridium difficile recurrence.

Chilton CH, Pickering DS, Freeman J.

Clin Microbiol Infect. 2018 May;24(5):476-482. doi: 10.1016/j.cmi.2017.11.017. Epub 2017 Dec 5. Review.

12.

Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.

Gynther M, Proietti Silvestri I, Hansen JC, Hansen KB, Malm T, Ishchenko Y, Larsen Y, Han L, Kayser S, Auriola S, Petsalo A, Nielsen B, Pickering DS, Bunch L.

J Med Chem. 2017 Dec 14;60(23):9885-9904. doi: 10.1021/acs.jmedchem.7b01624. Epub 2017 Dec 5.

13.

Effects of the dimeric PSD-95 inhibitor UCCB01-144 on functional recovery after fimbria-fornix transection in rats.

Sommer JB, Bach A, Malá H, Strømgaard K, Mogensen J, Pickering DS.

Pharmacol Biochem Behav. 2017 Oct;161:62-67. doi: 10.1016/j.pbb.2017.09.008. Epub 2017 Sep 21.

PMID:
28943199
14.

Revisiting the Quinoxalinedione Scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors.

Demmer CS, Rombach D, Liu N, Nielsen B, Pickering DS, Bunch L.

ACS Chem Neurosci. 2017 Nov 15;8(11):2477-2495. doi: 10.1021/acschemneuro.7b00243. Epub 2017 Sep 5.

PMID:
28872835
15.

Effects of Dimeric PSD-95 Inhibition on Excitotoxic Cell Death and Outcome After Controlled Cortical Impact in Rats.

Sommer JB, Bach A, Malá H, Gynther M, Bjerre AS, Gram MG, Marschner L, Strømgaard K, Mogensen J, Pickering DS.

Neurochem Res. 2017 Dec;42(12):3401-3413. doi: 10.1007/s11064-017-2381-y. Epub 2017 Aug 21.

PMID:
28828633
16.

Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors.

Szymańska E, Nielsen B, Johansen TN, Cuñado Moral AM, Pickering DS, Szczepańska K, Mickowska A, Kieć-Kononowicz K.

Eur J Med Chem. 2017 Sep 29;138:874-883. doi: 10.1016/j.ejmech.2017.07.007. Epub 2017 Jul 8.

PMID:
28738307
17.

Structure and Affinity of Two Bicyclic Glutamate Analogues at AMPA and Kainate Receptors.

Møllerud S, Pinto A, Marconi L, Frydenvang K, Thorsen TS, Laulumaa S, Venskutonytė R, Winther S, Moral AMC, Tamborini L, Conti P, Pickering DS, Kastrup JS.

ACS Chem Neurosci. 2017 Sep 20;8(9):2056-2064. doi: 10.1021/acschemneuro.7b00201. Epub 2017 Jul 21.

PMID:
28691798
18.

Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands.

Szymańska E, Chałupnik P, Johansen TN, Nielsen B, Cuñado Moral AM, Pickering DS, Więckowska A, Kieć-Kononowicz K.

Chem Biol Drug Des. 2017 Dec;90(6):1271-1281. doi: 10.1111/cbdd.13048. Epub 2017 Jul 18.

PMID:
28636281
19.

Binding and functional pharmacological characteristics of gepant-type antagonists in rat brain and mesenteric arteries.

Sheykhzade M, Amandi N, Pla MV, Abdolalizadeh B, Sams A, Warfvinge K, Edvinsson L, Pickering DS.

Vascul Pharmacol. 2017 Mar;90:36-43. doi: 10.1016/j.vph.2017.02.001. Epub 2017 Feb 10.

PMID:
28192258
20.

Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid.

Krogsgaard-Larsen N, Delgar CG, Koch K, Brown PM, Møller C, Han L, Huynh TH, Hansen SW, Nielsen B, Bowie D, Pickering DS, Kastrup JS, Frydenvang K, Bunch L.

J Med Chem. 2017 Jan 12;60(1):441-457. doi: 10.1021/acs.jmedchem.6b01516. Epub 2016 Dec 22.

PMID:
28005385
21.

In vitro and in vivo effects of a novel dimeric inhibitor of PSD-95 on excitotoxicity and functional recovery after experimental traumatic brain injury.

Sommer JB, Bach A, Malá H, Strømgaard K, Mogensen J, Pickering DS.

Eur J Neurosci. 2017 Jan;45(2):238-248. doi: 10.1111/ejn.13483. Epub 2016 Dec 4.

PMID:
27859797
22.

Lessons from crystal structures of kainate receptors.

Møllerud S, Frydenvang K, Pickering DS, Kastrup JS.

Neuropharmacology. 2017 Jan;112(Pt A):16-28. doi: 10.1016/j.neuropharm.2016.05.014. Epub 2016 May 26. Review.

PMID:
27236079
23.

Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands.

Szymańska E, Chałupnik P, Szczepańska K, Cuñado Moral AM, Pickering DS, Nielsen B, Johansen TN, Kieć-Kononowicz K.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5568-5572. doi: 10.1016/j.bmcl.2016.09.075. Epub 2016 Sep 30.

PMID:
27765511
24.

Investigation of antidepressant-like and anxiolytic-like actions and cognitive and motor side effects of four N-methyl-D-aspartate receptor antagonists in mice.

Refsgaard LK, Pickering DS, Andreasen JT.

Behav Pharmacol. 2017 Feb;28(1):37-47. doi: 10.1097/FBP.0000000000000266.

PMID:
27740963
25.

Effects of sertraline, duloxetine, vortioxetine, and idazoxan in the rat affective bias test.

Refsgaard LK, Haubro K, Pickering DS, Stuart SA, Robinson ES, Andreasen JT.

Psychopharmacology (Berl). 2016 Oct;233(21-22):3763-3770. Epub 2016 Aug 30.

PMID:
27572627
26.

The Structure of a High-Affinity Kainate Receptor: GluK4 Ligand-Binding Domain Crystallized with Kainate.

Kristensen O, Kristensen LB, Møllerud S, Frydenvang K, Pickering DS, Kastrup JS.

Structure. 2016 Sep 6;24(9):1582-9. doi: 10.1016/j.str.2016.06.019. Epub 2016 Aug 11.

27.

A pharmacological profile of the high-affinity GluK5 kainate receptor.

Møllerud S, Kastrup JS, Pickering DS.

Eur J Pharmacol. 2016 Oct 5;788:315-320. doi: 10.1016/j.ejphar.2016.06.049. Epub 2016 Jun 29.

PMID:
27373850
28.

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.

PMID:
27341500
29.

Structural rearrangement of the intracellular domains during AMPA receptor activation.

Zachariassen LG, Katchan L, Jensen AG, Pickering DS, Plested AJ, Kristensen AS.

Proc Natl Acad Sci U S A. 2016 Jul 5;113(27):E3950-9. doi: 10.1073/pnas.1601747113. Epub 2016 Jun 16.

30.

Enthalpy-Entropy Compensation in the Binding of Modulators at Ionotropic Glutamate Receptor GluA2.

Krintel C, Francotte P, Pickering DS, Juknaitė L, Pøhlsgaard J, Olsen L, Frydenvang K, Goffin E, Pirotte B, Kastrup JS.

Biophys J. 2016 Jun 7;110(11):2397-2406. doi: 10.1016/j.bpj.2016.04.032.

31.

Systemic and Brain Pharmacokinetics of Perforin Inhibitor Prodrugs.

Gynther M, Pickering DS, Spicer JA, Denny WA, Huttunen KM.

Mol Pharm. 2016 Jul 5;13(7):2484-91. doi: 10.1021/acs.molpharmaceut.6b00217. Epub 2016 Jun 13.

PMID:
27266990
32.

Effects of the dimeric PSD-95 inhibitor UCCB01-144 in mouse models of pain, cognition and motor function.

Andreasen JT, Nasser A, Caballero-Puntiverio M, Sahlholt M, Bach A, Gynther M, Strømgaard K, Pickering DS.

Eur J Pharmacol. 2016 Jun 5;780:166-73. doi: 10.1016/j.ejphar.2016.03.045. Epub 2016 Mar 28.

PMID:
27032314
33.

Neto2 Influences on Kainate Receptor Pharmacology and Function.

Han L, Howe JR, Pickering DS.

Basic Clin Pharmacol Toxicol. 2016 Aug;119(2):141-8. doi: 10.1111/bcpt.12575. Epub 2016 Mar 18. Review.

34.

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.

PMID:
26862980
35.

Modelling affective pain in mice: Effects of inflammatory hypersensitivity on place escape/avoidance behaviour, anxiety and hedonic state.

Refsgaard LK, Hoffmann-Petersen J, Sahlholt M, Pickering DS, Andreasen JT.

J Neurosci Methods. 2016 Mar 15;262:85-92. doi: 10.1016/j.jneumeth.2016.01.019. Epub 2016 Jan 25.

PMID:
26820902
36.

Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors.

Szymanska E, Frydenvang K, Pickering DS, Krintel C, Nielsen B, Kooshki A, Zachariassen LG, Olsen L, Kastrup JS, Johansen TN.

J Med Chem. 2016 Jan 14;59(1):448-61. doi: 10.1021/acs.jmedchem.5b01666. Epub 2015 Dec 22.

PMID:
26653877
37.

Investigation of the presence and antinociceptive function of muscarinic acetylcholine receptors in the African naked mole-rat (Heterocephalus glaber).

Jørgensen KB, Krogh-Jensen K, Pickering DS, Kanui TI, Abelson KS.

J Comp Physiol A Neuroethol Sens Neural Behav Physiol. 2016 Jan;202(1):7-15. doi: 10.1007/s00359-015-1048-x. Epub 2015 Oct 31.

38.

Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.

Krogsgaard-Larsen N, Storgaard M, Møller C, Demmer CS, Hansen J, Han L, Monrad RN, Nielsen B, Tapken D, Pickering DS, Kastrup JS, Frydenvang K, Bunch L.

J Med Chem. 2015 Aug 13;58(15):6131-50. doi: 10.1021/acs.jmedchem.5b00750. Epub 2015 Jul 22.

PMID:
26200741
39.

Binding mode of an α-amino acid-linked quinoxaline-2,3-dione analogue at glutamate receptor subtype GluK1.

Demmer CS, Møller C, Brown PM, Han L, Pickering DS, Nielsen B, Bowie D, Frydenvang K, Kastrup JS, Bunch L.

ACS Chem Neurosci. 2015 Jun 17;6(6):845-54. doi: 10.1021/acschemneuro.5b00038. Epub 2015 Apr 9.

PMID:
25856736
40.

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.

PMID:
25578259
41.

Blood-brain barrier permeability and brain uptake mechanism of kainic acid and dihydrokainic acid.

Gynther M, Petsalo A, Hansen SH, Bunch L, Pickering DS.

Neurochem Res. 2015 Mar;40(3):542-9. doi: 10.1007/s11064-014-1499-4. Epub 2014 Dec 9.

PMID:
25488153
42.

Design, synthesis and in vitro pharmacology of GluK1 and GluK3 antagonists. Studies towards the design of subtype-selective antagonists through 2-carboxyethyl-phenylalanines with substituents interacting with non-conserved residues in the GluK binding sites.

Sköld N, Nielsen B, Olsen J, Han L, Olsen L, Madsen U, Kristensen JL, Pickering DS, Johansen TN.

Bioorg Med Chem. 2014 Oct 1;22(19):5368-77. doi: 10.1016/j.bmc.2014.07.045. Epub 2014 Aug 2.

PMID:
25172149
43.

Molecular recognition of two 2,4-syn-functionalized (S)-glutamate analogues by the kainate receptor GluK3 ligand binding domain.

Venskutonytė R, Larsen AP, Frydenvang K, Gajhede M, Sagot E, Assaf Z, Gefflaut T, Pickering DS, Bunch L, Kastrup JS.

ChemMedChem. 2014 Oct;9(10):2254-9. doi: 10.1002/cmdc.201402204. Epub 2014 Jul 8.

PMID:
25044437
44.

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.

PMID:
24848194
45.

L-Asp is a useful tool in the purification of the ionotropic glutamate receptor A2 ligand-binding domain.

Krintel C, Frydenvang K, Ceravalls de Rabassa A, Kaern AM, Gajhede M, Pickering DS, Kastrup JS.

FEBS J. 2014 May;281(10):2422-30. doi: 10.1111/febs.12795. Epub 2014 Apr 17.

46.

Crystal structure and pharmacological characterization of a novel N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site.

Kvist T, Steffensen TB, Greenwood JR, Mehrzad Tabrizi F, Hansen KB, Gajhede M, Pickering DS, Traynelis SF, Kastrup JS, Bräuner-Osborne H.

J Biol Chem. 2013 Nov 15;288(46):33124-35. doi: 10.1074/jbc.M113.480210. Epub 2013 Sep 26.

47.

Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain.

Krintel C, Harpsøe K, Zachariassen LG, Peters D, Frydenvang K, Pickering DS, Gajhede M, Kastrup JS.

Acta Crystallogr D Biol Crystallogr. 2013 Sep;69(Pt 9):1645-52. doi: 10.1107/S0907444913011839. Epub 2013 Aug 15.

PMID:
23999288
48.

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.

PMID:
23643996
49.

Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization.

Juknaitė L, Sugamata Y, Tokiwa K, Ishikawa Y, Takamizawa S, Eng A, Sakai R, Pickering DS, Frydenvang K, Swanson GT, Kastrup JS, Oikawa M.

J Med Chem. 2013 Mar 28;56(6):2283-93. doi: 10.1021/jm301590z. Epub 2013 Mar 13.

50.

Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.

Assaf Z, Larsen AP, Venskutonytė R, Han L, Abrahamsen B, Nielsen B, Gajhede M, Kastrup JS, Jensen AA, Pickering DS, Frydenvang K, Gefflaut T, Bunch L.

J Med Chem. 2013 Feb 28;56(4):1614-28. doi: 10.1021/jm301433m. Epub 2013 Feb 15. Erratum in: J Med Chem. 2013 Jul 25;56(14):5985.

PMID:
23414088

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