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Items: 1 to 50 of 269

1.

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.

PMID:
28828616
2.

GABAA receptor partial agonists and antagonists: structure, binding mode, and pharmacology.

Krall J, Balle T, Krogsgaard-Larsen N, Sørensen TE, Krogsgaard-Larsen P, Kristiansen U, Frølund B.

Adv Pharmacol. 2015;72:201-27. doi: 10.1016/bs.apha.2014.10.003. Epub 2014 Dec 4. Review.

PMID:
25600372
3.

Probing α4βδ GABAA receptor heterogeneity: differential regional effects of a functionally selective α4β1δ/α4β3δ receptor agonist on tonic and phasic inhibition in rat brain.

Hoestgaard-Jensen K, Dalby NO, Krall J, Hammer H, Krogsgaard-Larsen P, Frølund B, Jensen AA.

J Neurosci. 2014 Dec 3;34(49):16256-72. doi: 10.1523/JNEUROSCI.1495-14.2014.

4.

Probing the orthosteric binding site of GABAA receptors with heterocyclic GABA carboxylic acid bioisosteres.

Petersen JG, Bergmann R, Krogsgaard-Larsen P, Balle T, Frølund B.

Neurochem Res. 2014 Jun;39(6):1005-15. doi: 10.1007/s11064-013-1226-6. Epub 2013 Dec 21. Review.

PMID:
24362592
5.

The orthosteric GABAA receptor ligand Thio-4-PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors.

Hoestgaard-Jensen K, O'Connor RM, Dalby NO, Simonsen C, Finger BC, Golubeva A, Hammer H, Bergmann ML, Kristiansen U, Krogsgaard-Larsen P, Bräuner-Osborne H, Ebert B, Frølund B, Cryan JF, Jensen AA.

Br J Pharmacol. 2013 Oct;170(4):919-32. doi: 10.1111/bph.12340.

6.

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.

PMID:
23398473
7.

Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.

Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, Stensbøl TB, Gloriam DE, Krogsgaard-Larsen P, Frølund B.

J Med Chem. 2013 Feb 14;56(3):1211-27. doi: 10.1021/jm301656h. Epub 2013 Jan 17.

PMID:
23301527
8.

Scientific social responsibility: a call to arms.

Krogsgaard-Larsen P, Thostrup P, Besenbacher F.

Angew Chem Int Ed Engl. 2011 Nov 11;50(46):10738-40. doi: 10.1002/anie.201105641. Epub 2011 Oct 10. No abstract available.

PMID:
21987352
9.

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.

10.

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

Frydenvang K, Pickering DS, Greenwood JR, Krogsgaard-Larsen N, Brehm L, Nielsen B, Vogensen SB, Hald H, Kastrup JS, Krogsgaard-Larsen P, Clausen RP.

J Med Chem. 2010 Dec 9;53(23):8354-61. doi: 10.1021/jm101218a. Epub 2010 Nov 10.

PMID:
21067182
11.

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.

Clausen RP, Naur P, Kristensen AS, Greenwood JR, Strange M, Bräuner-Osborne H, Jensen AA, Nielsen AS, Geneser U, Ringgaard LM, Nielsen B, Pickering DS, Brehm L, Gajhede M, Krogsgaard-Larsen P, Kastrup JS.

J Med Chem. 2009 Aug 13;52(15):4911-22. doi: 10.1021/jm900565c.

PMID:
19588945
12.

Detecting protein-protein interactions in living cells: development of a bioluminescence resonance energy transfer assay to evaluate the PSD-95/NMDA receptor interaction.

Gottschalk M, Bach A, Hansen JL, Krogsgaard-Larsen P, Kristensen AS, Strømgaard K.

Neurochem Res. 2009 Oct;34(10):1729-37. doi: 10.1007/s11064-009-9998-4. Epub 2009 Jun 4.

PMID:
19495967
13.

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

Madsen KK, Clausen RP, Larsson OM, Krogsgaard-Larsen P, Schousboe A, White HS.

J Neurochem. 2009 May;109 Suppl 1:139-44. doi: 10.1111/j.1471-4159.2009.05982.x.

14.

Subtype selective kainic acid receptor agonists: discovery and approaches to rational design.

Bunch L, Krogsgaard-Larsen P.

Med Res Rev. 2009 Jan;29(1):3-28. doi: 10.1002/med.20133. Review.

PMID:
18623169
15.

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

Smith MD, Saunders GW, Clausen RP, Frølund B, Krogsgaard-Larsen P, Larsson OM, Schousboe A, Wilcox KS, White HS.

Epilepsy Res. 2008 Mar;79(1):6-13. doi: 10.1016/j.eplepsyres.2007.12.009. Epub 2008 Feb 8.

16.

5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.

Madsen C, Jensen AA, Liljefors T, Kristiansen U, Nielsen B, Hansen CP, Larsen M, Ebert B, Bang-Andersen B, Krogsgaard-Larsen P, Frølund B.

J Med Chem. 2007 Aug 23;50(17):4147-61. Epub 2007 Jul 26.

PMID:
17655213
17.

A tetrazolyl-substituted subtype-selective AMPA receptor agonist.

Vogensen SB, Frydenvang K, Greenwood JR, Postorino G, Nielsen B, Pickering DS, Ebert B, Bølcho U, Egebjerg J, Gajhede M, Kastrup JS, Johansen TN, Clausen RP, Krogsgaard-Larsen P.

J Med Chem. 2007 May 17;50(10):2408-14. Epub 2007 Apr 25.

PMID:
17455929
18.

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

Jørgensen CG, Bräuner-Osborne H, Nielsen B, Kehler J, Clausen RP, Krogsgaard-Larsen P, Madsen U.

Bioorg Med Chem. 2007 May 15;15(10):3524-38. Epub 2007 Mar 3.

PMID:
17376693
19.

4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.

Frølund B, Jensen LS, Storustovu SI, Stensbøl TB, Ebert B, Kehler J, Krogsgaard-Larsen P, Liljefors T.

J Med Chem. 2007 Apr 19;50(8):1988-92. Epub 2007 Mar 22.

PMID:
17375905
20.

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

Jørgensen CG, Clausen RP, Hansen KB, Bräuner-Osborne H, Nielsen B, Metzler B, Kehler J, Krogsgaard-Larsen P, Madsen U.

Org Biomol Chem. 2007 Feb 7;5(3):463-71. Erratum in: Org Biomol Chem. 2007 Mar 7;5(5):848. Metzler, Birgitte Bjørn [corrected to Metzler, Bjørn].

PMID:
17340770
21.

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

Clausen RP, Madsen K, Larsson OM, Frølund B, Krogsgaard-Larsen P, Schousboe A.

Adv Pharmacol. 2006;54:265-84. Review. No abstract available.

PMID:
17175818
22.

GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.

Krogsgaard-Larsen P, Frølund B, Liljefors T.

Adv Pharmacol. 2006;54:53-71. No abstract available.

PMID:
17175810
23.

Structure-activity relationships of selective GABA uptake inhibitors.

Høg S, Greenwood JR, Madsen KB, Larsson OM, Frølund B, Schousboe A, Krogsgaard-Larsen P, Clausen RP.

Curr Top Med Chem. 2006;6(17):1861-82. Review.

PMID:
17017962
24.

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

Clausen RP, Frølund B, Larsson OM, Schousboe A, Krogsgaard-Larsen P, White HS.

Neurochem Int. 2006 May-Jun;48(6-7):637-42. Epub 2006 Mar 3. Review.

PMID:
16517017
25.

Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.

Krehan D, Storustovu SI, Liljefors T, Ebert B, Nielsen B, Krogsgaard-Larsen P, Frølund B.

J Med Chem. 2006 Feb 23;49(4):1388-96.

PMID:
16480274
26.

Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: synthesis, modelling and molecular pharmacology.

Frølund B, Greenwood JR, Holm MM, Egebjerg J, Madsen U, Nielsen B, Bräuner-Osborne H, Stensbøl TB, Krogsgaard-Larsen P.

Bioorg Med Chem. 2005 Sep 15;13(18):5391-8.

PMID:
16043357
27.

Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.

Jensen AA, Frølund B, Liljefors T, Krogsgaard-Larsen P.

J Med Chem. 2005 Jul 28;48(15):4705-45. Review. No abstract available.

PMID:
16033252
28.

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

Vogensen SB, Clausen RP, Greenwood JR, Johansen TN, Pickering DS, Nielsen B, Ebert B, Krogsgaard-Larsen P.

J Med Chem. 2005 May 5;48(9):3438-42.

PMID:
15857151
29.

EUFEPS report. Contribution of academic research to discovery and development of medicines: current status and future opportunities.

Couvreur P, Barguer D, Crommelin DJ, Duchêne D, Engels JW, Kerr DJ, Krogsgaard-Larsen P, Meijer DK, Paoletti R, Wagner E; EUFEPS.

Eur J Pharm Sci. 2005 Feb;24(2-3):245-52. No abstract available.

PMID:
15776539
30.

Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.

Frølund B, Jensen LS, Guandalini L, Canillo C, Vestergaard HT, Kristiansen U, Nielsen B, Stensbøl TB, Madsen C, Krogsgaard-Larsen P, Liljefors T.

J Med Chem. 2005 Jan 27;48(2):427-39.

PMID:
15658856
31.

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

Clausen RP, Moltzen EK, Perregaard J, Lenz SM, Sanchez C, Falch E, Frølund B, Bolvig T, Sarup A, Larsson OM, Schousboe A, Krogsgaard-Larsen P.

Bioorg Med Chem. 2005 Feb 1;13(3):895-908.

PMID:
15653355
32.

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.

White HS, Watson WP, Hansen SL, Slough S, Perregaard J, Sarup A, Bolvig T, Petersen G, Larsson OM, Clausen RP, Frølund B, Falch E, Krogsgaard-Larsen P, Schousboe A.

J Pharmacol Exp Ther. 2005 Feb;312(2):866-74. Epub 2004 Nov 18.

PMID:
15550575
33.

Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids.

N'goka V, Stenbøl TB, Krogsgaard-Larsen P, Schlewer G.

Eur J Med Chem. 2004 Oct;39(10):889-95.

PMID:
15464623
34.

GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.

Krogsgaard-Larsen P, Frølund B, Liljefors T, Ebert B.

Biochem Pharmacol. 2004 Oct 15;68(8):1573-80.

PMID:
15451401
35.

Carbamoylcholine homologs: synthesis and pharmacology at nicotinic acetylcholine receptors.

Jensen AA, Mikkelsen I, Frølund B, Frydenvang K, Brehm L, Jaroszewski JW, Bräuner-Osborne H, Falch E, Krogsgaard-Larsen P.

Eur J Pharmacol. 2004 Aug 23;497(2):125-37.

PMID:
15306197
36.

Syntheses and GABA uptake properties of 6-ether- and 6-enol ether-substituted nipecotic acids.

N'Goka V, Bissantz C, Bisel P, Stenbøl TB, Krogsgaard-Larsen P, Schlewer G.

Eur J Med Chem. 2004 Jul;39(7):633-8.

PMID:
15236844
37.

Synthesis, theoretical and structural analyses, and enantiopharmacology of 3-carboxy homologs of AMPA.

Brehm L, Greenwood JR, Sløk FA, Holm MM, Nielsen B, Geneser U, Stensbøl TB, Bräuner-Osborne H, Begtrup M, Egebjerg J, Krogsgaard-Larsen P.

Chirality. 2004 Aug;16(7):452-66.

PMID:
15236343
38.

Activation of single heteromeric GABA(A) receptor ion channels by full and partial agonists.

Mortensen M, Kristiansen U, Ebert B, Frølund B, Krogsgaard-Larsen P, Smart TG.

J Physiol. 2004 Jun 1;557(Pt 2):389-413. Epub 2004 Feb 27.

39.

Ibotenic acid and thioibotenic acid: a remarkable difference in activity at group III metabotropic glutamate receptors.

Hermit MB, Greenwood JR, Nielsen B, Bunch L, Jørgensen CG, Vestergaard HT, Stensbøl TB, Sanchez C, Krogsgaard-Larsen P, Madsen U, Bräuner-Osborne H.

Eur J Pharmacol. 2004 Feb 23;486(3):241-50.

PMID:
14985045
40.

Synthesis of aryl- and heteroaryl-substituted 3-benzyloxyisothiazoles via Suzuki and Negishi cross-coupling reactions.

Kaae BH, Krogsgaard-Larsen P, Johansen TN.

J Org Chem. 2004 Feb 20;69(4):1401-4.

PMID:
14961704
41.

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.

Vogensen SB, Greenwood JR, Varming AR, Brehm L, Pickering DS, Nielsen B, Liljefors T, Clausen RP, Johansen TN, Krogsgaard-Larsen P.

Org Biomol Chem. 2004 Jan 21;2(2):206-13. Epub 2003 Nov 24.

PMID:
14737644
42.

Aza-THIP and related analogues of THIP as GABA C antagonists.

Krehan D, Frølund B, Ebert B, Nielsen B, Krogsgaard-Larsen P, Johnston GA, Chebib M.

Bioorg Med Chem. 2003 Nov 17;11(23):4891-6.

PMID:
14604650
43.

Contrasting actions of philanthotoxin-343 and philanthotoxin-(12) on human muscle nicotinic acetylcholine receptors.

Brier TJ, Mellor IR, Tikhonov DB, Neagoe I, Shao Z, Brierley MJ, Strømgaard K, Jaroszewski JW, Krogsgaard-Larsen P, Usherwood PN.

Mol Pharmacol. 2003 Oct;64(4):954-64.

PMID:
14500752
44.

Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.

Jensen AA, Mikkelsen I, Frølund B, Bräuner-Osborne H, Falch E, Krogsgaard-Larsen P.

Mol Pharmacol. 2003 Oct;64(4):865-75.

PMID:
14500743
45.

Synthesis and in vitro pharmacology at AMPA and kainate preferring glutamate receptors of 4-heteroarylmethylidene glutamate analogues.

Valgeirsson J, Christensen JK, Kristensen AS, Pickering DS, Nielsen B, Fischer CH, Bräuner-Osborne H, Nielsen EØ, Krogsgaard-Larsen P, Madsen U.

Bioorg Med Chem. 2003 Oct 1;11(20):4341-9.

PMID:
13129570
46.

Design and synthesis of a new series of 4-alkylated 3-isoxazolol GABA A antagonists.

Frølund B, Tagmose L, Jørgensen AT, Kristiansen U, Stensbøl TB, Liljefors T, Krogsgaard-Larsen P.

Eur J Med Chem. 2003 Apr;38(4):447-9.

PMID:
12750034
47.
48.

(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.

Brehm L, Greenwood JR, Hansen KB, Nielsen B, Egebjerg J, Stensbøl TB, Bräuner-Osborne H, Sløk FA, Kronborg TT, Krogsgaard-Larsen P.

J Med Chem. 2003 Apr 10;46(8):1350-8.

PMID:
12672235
49.

Phosphinic, phosphonic and seleninic acid bioisosteres of isonipecotic acid as novel and selective GABA(C) receptor antagonists.

Krehan D, Frølund B, Krogsgaard-Larsen P, Kehler J, Johnston GA, Chebib M.

Neurochem Int. 2003 Jun;42(7):561-5.

PMID:
12590939
50.

Rational design, synthesis, and pharmacological evaluation of 2-azanorbornane-3-exo,5-endo-dicarboxylic acid: a novel conformationally restricted glutamic acid analogue.

Bunch L, Liljefors T, Greenwood JR, Frydenvang K, Bräuner-Osborne H, Krogsgaard-Larsen P, Madsen U.

J Org Chem. 2003 Feb 21;68(4):1489-95.

PMID:
12585893

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