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Items: 1 to 50 of 115

1.

Developing New 4-PIOL and 4-PHP Analogues for Photoinactivation of γ-Aminobutyric Acid Type A Receptors.

Mortensen M, Krall J, Kongstad KT, Brygger BM, Lenzi O, Francotte P, Sørensen TE, Nielsen B, Jensen AA, Smart TG, Frølund B.

ACS Chem Neurosci. 2019 Nov 20;10(11):4669-4684. doi: 10.1021/acschemneuro.9b00478. Epub 2019 Oct 21.

PMID:
31589403
2.

Synthesis and Pharmacological Evaluation of [11C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors.

L'Estrade ET, Hansen HD, Falk-Petersen C, Haugaard A, Griem-Krey N, Jung S, Lüddens H, Schirmeister T, Erlandsson M, Ohlsson T, Knudsen GM, Herth MM, Wellendorph P, Frølund B.

ACS Omega. 2019 May 22;4(5):8846-8851. doi: 10.1021/acsomega.9b00434. eCollection 2019 May 31.

3.

Designing Poly-agonists for Treatment of Metabolic Diseases: Challenges and Opportunities.

Petersen J, Strømgaard K, Frølund B, Clemmensen C.

Drugs. 2019 Jul;79(11):1187-1197. doi: 10.1007/s40265-019-01153-6. Review.

PMID:
31243696
4.

Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.

Giraudo A, Krall J, Bavo F, Nielsen B, Kongstad KT, Rolando B, De Blasio R, Gloriam DE, Löffler R, Thiesen L, Harpsøe K, Frydenvang K, Boschi D, Wellendorph P, Lolli ML, Jensen AA, Frølund B.

J Med Chem. 2019 Jun 27;62(12):5797-5809. doi: 10.1021/acs.jmedchem.9b00026. Epub 2019 Jun 5.

PMID:
31117514
5.

Structural and molecular aspects of betaine-GABA transporter 1 (BGT1) and its relation to brain function.

Kickinger S, Hellsberg E, Frølund B, Schousboe A, Ecker GF, Wellendorph P.

Neuropharmacology. 2019 May 18:107644. doi: 10.1016/j.neuropharm.2019.05.021. [Epub ahead of print] Review.

PMID:
31108110
6.

Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.

Krall J, Bavo F, Falk-Petersen CB, Jensen CH, Nielsen JO, Tian Y, Anglani V, Kongstad KT, Piilgaard L, Nielsen B, Gloriam DE, Kehler J, Jensen AA, Harpsøe K, Wellendorph P, Frølund B.

J Med Chem. 2019 Mar 14;62(5):2798-2813. doi: 10.1021/acs.jmedchem.9b00131. Epub 2019 Feb 27.

PMID:
30763084
7.

Lack of evidence for synaptic high-affinity γ-hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na+ -dependent SLC neurotransmitter transporters.

Thiesen L, Frølund B, Wellendorph P.

J Neurochem. 2019 Apr;149(2):195-210. doi: 10.1111/jnc.14649. Epub 2019 Jan 31.

PMID:
30570143
8.

4-Hydroxy-1,2,3-triazole moiety as bioisostere of the carboxylic acid function: a novel scaffold to probe the orthosteric γ-aminobutyric acid receptor binding site.

Giraudo A, Krall J, Nielsen B, Sørensen TE, Kongstad KT, Rolando B, Boschi D, Frølund B, Lolli ML.

Eur J Med Chem. 2018 Oct 5;158:311-321. doi: 10.1016/j.ejmech.2018.08.094. Epub 2018 Sep 5.

PMID:
30223119
9.

Structure-Function Evaluation of Imidazopyridine Derivatives Selective for δ-Subunit-Containing γ-Aminobutyric Acid Type A (GABAA) Receptors.

Yakoub K, Jung S, Sattler C, Damerow H, Weber J, Kretzschmann A, Cankaya AS, Piel M, Rösch F, Haugaard AS, Frølund B, Schirmeister T, Lüddens H.

J Med Chem. 2018 Mar 8;61(5):1951-1968. doi: 10.1021/acs.jmedchem.7b01484. Epub 2018 Feb 26.

PMID:
29451785
10.

Pharmacological Characterization of [3H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter.

Al-Khawaja A, Haugaard AS, Marek A, Löffler R, Thiesen L, Santiveri M, Damgaard M, Bundgaard C, Frølund B, Wellendorph P.

ACS Chem Neurosci. 2018 Mar 21;9(3):545-554. doi: 10.1021/acschemneuro.7b00351. Epub 2017 Nov 22.

PMID:
29131576
11.

Functional characterization of GABAA receptor-mediated modulation of cortical neuron network activity in microelectrode array recordings.

Bader BM, Steder A, Klein AB, Frølund B, Schroeder OHU, Jensen AA.

PLoS One. 2017 Oct 13;12(10):e0186147. doi: 10.1371/journal.pone.0186147. eCollection 2017.

12.

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.

PMID:
29028338
13.

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.

PMID:
28828618
14.

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
15.

Monastrol, a 3,4-dihydropyrimidin-2(1H)-thione, as structural scaffold for the development of modulators for GHB high-affinity binding sites and α1β2δ GABAA receptors.

Damgaard M, Al-Khawaja A, Nittegaard-Nielsen M, Petersen RF, Wellendorph P, Frølund B.

Eur J Med Chem. 2017 Sep 29;138:300-312. doi: 10.1016/j.ejmech.2017.06.024. Epub 2017 Jun 15.

PMID:
28683403
16.

Discovery and Evaluation of Anti-Fibrinolytic Plasmin Inhibitors Derived from 5-(4-Piperidyl)isoxazol-3-ol (4-PIOL).

Schmidt TC, Eriksson PO, Gustafsson D, Cosgrove D, Frølund B, Boström J.

J Chem Inf Model. 2017 Jul 24;57(7):1703-1714. doi: 10.1021/acs.jcim.7b00255. Epub 2017 Jul 12.

PMID:
28653850
17.

Development of a Robust Mammalian Cell-based Assay for Studying Recombinant α4 β1/3 δ GABAA Receptor Subtypes.

Falk-Petersen CB, Søgaard R, Madsen KL, Klein AB, Frølund B, Wellendorph P.

Basic Clin Pharmacol Toxicol. 2017 Aug;121(2):119-129. doi: 10.1111/bcpt.12778. Epub 2017 May 25.

18.

Imidazole-4-acetic acid, a new lead structure for interaction with the taurine transporter in outer blood-retinal barrier cells.

Valembois S, Krall J, Frølund B, Steffansen B.

Eur J Pharm Sci. 2017 May 30;103:77-84. doi: 10.1016/j.ejps.2017.02.041. Epub 2017 Mar 1.

PMID:
28259832
19.

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.

PMID:
28095676
20.

Discovery of α-Substituted Imidazole-4-acetic Acid Analogues as a Novel Class of ρ1 γ-Aminobutyric Acid Type A Receptor Antagonists with Effect on Retinal Vascular Tone.

Krall J, Brygger BM, Sigurðardóttir SB, Ng CK, Bundgaard C, Kehler J, Nielsen B, Bek T, Jensen AA, Frølund B.

ChemMedChem. 2016 Oct 19;11(20):2299-2310. doi: 10.1002/cmdc.201600356. Epub 2016 Sep 13.

PMID:
27620323
21.

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.

PMID:
27615059
22.

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.

PMID:
27593893
23.

Delineation of the functional properties and the mechanism of action of TMPPAA, an allosteric agonist and positive allosteric modulator of 5-HT3 receptors.

Gasiorek A, Trattnig SM, Ahring PK, Kristiansen U, Frølund B, Frederiksen K, Jensen AA.

Biochem Pharmacol. 2016 Jun 15;110-111:92-108. doi: 10.1016/j.bcp.2016.04.004. Epub 2016 Apr 13.

PMID:
27086281
24.

Context-Dependent Modulation of GABAAR-Mediated Tonic Currents.

Patel B, Bright DP, Mortensen M, Frølund B, Smart TG.

J Neurosci. 2016 Jan 13;36(2):607-21. doi: 10.1523/JNEUROSCI.2047-15.2016.

25.

Differential interactions of 5-(4-piperidyl)-3-isoxazolol analogues with insect γ-aminobutyric acid receptors leading to functional selectivity.

Liu G, Frølund B, Ozoe F, Ozoe Y.

Insect Biochem Mol Biol. 2015 Nov;66:64-71. doi: 10.1016/j.ibmb.2015.10.002. Epub 2015 Oct 8.

PMID:
26453818
26.

Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.

Bach TB, Jensen AA, Petersen JG, Sørensen TE, Della Volpe S, Liu J, Blaazer AR, van Muijlwijk-Koezen JE, Balle T, Frølund B.

Eur J Med Chem. 2015 Sep 18;102:425-44. doi: 10.1016/j.ejmech.2015.07.024. Epub 2015 Jul 17.

PMID:
26301559
27.

Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.

de la Fuente Revenga M, Balle T, Jensen AA, Frølund B.

Eur J Med Chem. 2015 Sep 18;102:352-62. doi: 10.1016/j.ejmech.2015.07.029. Epub 2015 Jul 17.

PMID:
26298493
28.

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.

PMID:
26154082
29.

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.

PMID:
25986445
30.

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
31.

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.

32.

5-(Piperidin-4-yl)-3-hydroxypyrazole: A novel scaffold for probing the orthosteric γ-aminobutyric acid type A receptor binding site.

Krall J, Kongstad KT, Nielsen B, Sørensen TE, Balle T, Jensen AA, Frølund B.

ChemMedChem. 2014 Nov;9(11):2475-85. doi: 10.1002/cmdc.201402248. Epub 2014 Aug 26.

PMID:
25156407
33.

The GABAA antagonist DPP-4-PIOL selectively antagonises tonic over phasic GABAergic currents in dentate gyrus granule cells.

Boddum K, Frølund B, Kristiansen U.

Neurochem Res. 2014 Nov;39(11):2078-84. doi: 10.1007/s11064-014-1397-9. Epub 2014 Aug 8.

PMID:
25103229
34.

Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.

Petersen JG, Sørensen T, Damgaard M, Nielsen B, Jensen AA, Balle T, Bergmann R, Frølund B.

Eur J Med Chem. 2014 Sep 12;84:404-16. doi: 10.1016/j.ejmech.2014.07.039. Epub 2014 Jul 11.

PMID:
25038482
35.

Positive allosteric modulation of the GHB high-affinity binding site by the GABAA receptor modulator monastrol and the flavonoid catechin.

Eghorn LF, Hoestgaard-Jensen K, Kongstad KT, Bay T, Higgins D, Frølund B, Wellendorph P.

Eur J Pharmacol. 2014 Oct 5;740:570-7. doi: 10.1016/j.ejphar.2014.06.028. Epub 2014 Jun 25.

PMID:
24973695
36.

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.

PMID:
24852577
37.

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
38.

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.

39.

GABAergic control of arteriolar diameter in the rat retina.

Hinds K, Monaghan KP, Frølund B, McGeown JG, Curtis TM.

Invest Ophthalmol Vis Sci. 2013 Oct 21;54(10):6798-805. doi: 10.1167/iovs.13-12362.

PMID:
24045989
40.

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.

41.

Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation.

Krall J, Jensen CH, Sørensen TE, Nielsen B, Jensen AA, Sander T, Balle T, Frølund B.

J Med Chem. 2013 Aug 22;56(16):6536-40. doi: 10.1021/jm4006466. Epub 2013 Aug 8.

PMID:
23855889
42.

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
43.

Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.

Petersen JG, Bergmann R, Møller HA, Jørgensen CG, Nielsen B, Kehler J, Frydenvang K, Kristensen J, Balle T, Jensen AA, Kristiansen U, Frølund B.

J Med Chem. 2013 Feb 14;56(3):993-1006. doi: 10.1021/jm301473k. Epub 2013 Jan 23.

PMID:
23294161
44.

Synthesis, pharmacology, and biostructural characterization of novel α4β2 nicotinic acetylcholine receptor agonists.

Ussing CA, Hansen CP, Petersen JG, Jensen AA, Rohde LA, Ahring PK, Nielsen EØ, Kastrup JS, Gajhede M, Frølund B, Balle T.

J Med Chem. 2013 Feb 14;56(3):940-51. doi: 10.1021/jm301409f. Epub 2013 Jan 22.

PMID:
23256554
45.

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.

46.

New insights into the GABA(A) receptor structure and orthosteric ligand binding: receptor modeling guided by experimental data.

Sander T, Frølund B, Bruun AT, Ivanov I, McCammon JA, Balle T.

Proteins. 2011 May;79(5):1458-77. doi: 10.1002/prot.22975. Epub 2011 Mar 1.

47.

Discovery of benzamide analogues as a novel class of 5-HT₃ receptor agonists.

Jørgensen CG, Frølund B, Kehler J, Jensen AA.

ChemMedChem. 2011 Apr 4;6(4):725-36. doi: 10.1002/cmdc.201000444. Epub 2011 Jan 18.

PMID:
21246737
48.

Potentiating action of propofol at GABAA receptors of retinal bipolar cells.

Yue L, Xie A, Bruzik KS, Frølund B, Qian H, Pepperberg DR.

Invest Ophthalmol Vis Sci. 2011 Apr 16;52(5):2497-509. doi: 10.1167/iovs.10-5991. Print 2011 Apr.

49.

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.

Sabbatini P, Wellendorph P, Høg S, Pedersen MH, Bräuner-Osborne H, Martiny L, Frølund B, Clausen RP.

J Med Chem. 2010 Sep 9;53(17):6506-10. doi: 10.1021/jm1006325.

PMID:
20715819
50.

Novel radioiodinated {gamma}-hydroxybutyric acid analogues for radiolabeling and Photolinking of high-affinity {gamma}-hydroxybutyric acid binding sites.

Wellendorph P, Høg S, Sabbatini P, Pedersen MH, Martiny L, Knudsen GM, Frølund B, Clausen RP, Bräuner-Osborne H.

J Pharmacol Exp Ther. 2010 Nov;335(2):458-64. doi: 10.1124/jpet.110.170670. Epub 2010 Aug 9.

PMID:
20696866

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