Research Topics
Species | Bjarke EbertSummaryAffiliation: H. Lundbeck A/S Country: Denmark Publications
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Detail Information
Publications
Treating insomnia: Current and investigational pharmacological approachesBjarke Ebert
Department of Electrophysiology, H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Copenhagen, Denmark
Pharmacol Ther 112:612-29. 2006....
Characterization of GABA(A) receptor ligands in the rat cortical wedge preparation: evidence for action at extrasynaptic receptors?B Ebert
Department of Molecular Pharmacology, H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Denmark
Br J Pharmacol 137:1-8. 2002..Results therefore indicate a significant contribution of extrasynaptic receptors to pharmacological activity of exogenous applied GABA(A) agonists in this system...- Discontinued drugs 2007: central and peripheral nervous system drugsBjarke Ebert
Department of Electrophysiology, H Lundbeck A S, Ottiliavej 9, Valby, 2500, Denmark
Expert Opin Investig Drugs 18:109-23. 2009..This year's list of discontinued compounds spans the range from truly innovative drugs to 'me-too' compounds and as such is highly useful in illustrating the current dilemmas for the pharmaceutical industry... 
Gaboxadol -- a different hypnotic profile with no tolerance to sleep EEG and sedative effects after repeated daily dosingBjarke Ebert
H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Denmark
Pharmacol Biochem Behav 90:113-22. 2008..Withdrawal from gaboxadol, zolpidem and indiplon did not affect the seizure threshold to bicuculline. Gaboxadol's apparent rapid development of tolerance in the rotarod assay appears to be kinetically determined...- Lack of generalisation between the GABAA receptor agonist, gaboxadol, and allosteric modulators of the benzodiazepine binding site in the rat drug discrimination procedureSigne Michelsen
Department of Neuropharmacology, H Lundbeck A S, Ottiliavej 9, 2500, Copenhagen, Valby, Denmark
Psychopharmacology (Berl) 193:151-7. 2007.... - Rotarod studies in the rat of the GABAA receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-toleranceJeppe Voss
Department of Neuropharmacology, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark
Eur J Pharmacol 482:215-22. 2003..No cross-tolerance was observed, indicating that the motor coordination effects observed with gaboxadol and zolpidem may arise from interaction with different receptor populations... - Pharmacological characterization of agonists at delta-containing GABAA receptors: Functional selectivity for extrasynaptic receptors is dependent on the absence of gamma2Signe I Storustovu
Department of Electrophysiology, H Lundbeck A S, 9 Ottiliavej, DK 2500 Valby, Denmark
J Pharmacol Exp Ther 316:1351-9. 2006.... - Gaboxadol: in vitro interaction studies with benzodiazepines and ethanol suggest functional selectivitySigne I Storustovu
Department of Molecular Pharmacology, H Lundbeck A S, 9 Ottiliavej, DK 2500 Valby, Denmark
Eur J Pharmacol 467:49-56. 2003..These findings suggest that gaboxadol in functionally intact tissue may interact with a receptor population, which is insensitive to the modulation by benzodiazepines... - R-citalopram functionally antagonises escitalopram in vivo and in vitro: evidence for kinetic interaction at the serotonin transporterSigne I Storustovu
Department of Electrophysiology, H Lundbeck A S, 9 Ottiliavej, Valby DK 2500, Denmark
Br J Pharmacol 142:172-80. 2004..6. We propose that the kinetic interaction of R- and S-citalopram with SERT is a critical factor contributing to the antagonistic effects of R-citalopram on S-citalopram in vitro and in vivo... - Upregulation of glutamate receptor subtypes during alcohol withdrawal in ratsSteven Rosenzweig Haugbøl
Department of Psychiatry, University Hospital Rigshospitalet, Copenhagen, Denmark
Alcohol Alcohol 40:89-95. 2005..To investigate glutamate receptor subtypes during alcohol withdrawal... - Escitalopram versus citalopram: the surprising role of the R-enantiomerConnie Sanchez
Research and Development, H Lundbeck A S, Ottiliavej 9, 2500 Valby Copenhagen, Denmark
Psychopharmacology (Berl) 174:163-76. 2004..e. containing the same amount of the S-enantiomer, showed better effect for escitalopram. These results suggested that the R-citalopram in citalopram inhibits the effect of the S-enantiomer... - 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 gaboxadolKarsten K Madsen
Department of Pharmacology and Pharmacotherapy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark
J Pharmacol Exp Ther 338:214-9. 2011..Taken together, these results highlight the mechanistic differences between tiagabine and EF1502 and support a functional role for BGT1 and extrasynaptic GABA(A) receptors... - GABA(A) receptor ligands and their therapeutic potentialsBente Frølund
Departments of Medicinal Chemistry, The Royal Danish School of Pharmacy, Copenhagen, DK 2100, Denmark
Curr Top Med Chem 2:817-32. 2002.... - Molecular cloning and pharmacological characterization of serotonin 5-HT(3A) receptor subtype in dogThomas N Jensen
Department of Electrophysiology, H Lundbeck A S, 9 Ottiliavej, DK 2500 Valby, Denmark
Eur J Pharmacol 538:23-31. 2006..We therefore conclude that position 195 is strongly involved in the receptor-ligand interaction, but additional residues must contribute to the overall pharmacological profile... - Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake timeKeith A Wafford
Eli Lilly UK, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK
Nat Rev Drug Discov 7:530-40. 2008.... - Plasma and CNS concentrations of Gaboxadol in rats following subcutaneous administrationThomas Cremers
Brains on Line, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands
Eur J Pharmacol 562:47-52. 2007..It is concluded that concentrations of Gaboxadol in the CNS are in a range, which are likely to activate only extrasynaptic (nongamma subunit containing) GABA(A) receptors... - Gaboxadol--a new awakening in sleepKeith A Wafford
Merck, Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
Curr Opin Pharmacol 6:30-6. 2006..This unique mechanism has contributed to our increased understanding of sleep mechanisms, and targeting of this system offers potential advantages over existing insomnia treatments... - Pharmacology of GABA(A) receptors exhibiting different levels of spontaneous activityMartin Mortensen
Department of Pharmacology, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK-2100 Copenhagen, Denmark
Eur J Pharmacol 476:17-24. 2003..These novel findings indicate that the potency and efficacy of ligands acting on GABA(A) receptors are highly dependent on the level of spontaneous activity of the receptor... - 4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationshipsBente Frølund
Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, DK 2100 Copenhagen, Denmark
J Med Chem 50:1988-92. 2007..These potencies are significantly higher than those of previously reported 4-PIOL antagonists and considerably higher than that of the standard GABAA antagonist SR 95531... - Extrasynaptic GABA(A) channels activated by THIP are modulated by diazepam in CA1 pyramidal neurons in the rat brain hippocampal sliceCatarina E L Lindquist
Molecular and Cellular Physiology, Department of Physiological Sciences, Lund University, Tornavagen 10 BMC F11, 22184 Lund, Sweden
Mol Cell Neurosci 24:250-7. 2003..5-5 microM ) of GABA. The increase in the inhibitory conductance with membrane depolarization permits gradation of the shunt pathway relative to the level of the excitatory input... - GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnoticPovl Krogsgaard-Larsen
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK 2100 Copenhagen, Denmark
Biochem Pharmacol 68:1573-80. 2004..In this connection, a series of GABA(A) ligands has been developed showing pharmacological profiles ranging from low-efficacy partial GABA(A) agonist activity to selective antagonist effect... - 5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonistsChristian Madsen
Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, DK 2100 Copenhagen, Denmark
J Med Chem 50:4147-61. 2007..However, in contrast to GABA and 4, which exhibited increased agonist potencies at a alpha1(Thr129Ser)beta2gamma2 mutant compared to WT GABAA receptor, the data obtained for 8a at the WT and mutant receptors were nonconclusive... - A tetrazolyl-substituted subtype-selective AMPA receptor agonistStine B Vogensen
Department of Medicinal Chemistry, The Faculty of Pharmaceutical Sciences, University of Copenhagen, 2 Universitetsparken, DK 2100 Copenhagen, Denmark
J Med Chem 50:2408-14. 2007.... - GABA(A) receptor inhibition - site matters!Bjarke Ebert
Acta Physiol (Oxf) 188:151. 2006 - Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacologyDorte Krehan
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, DK-2100 Copenhagen, Denmark
J Med Chem 49:1388-96. 2006..This antagonist profile of 7e and 7h was particularly pronounced at alpha4beta3delta-containing GABA(A) receptors, which showed three- and 10-fold selectivity for 7h and 6h, respectively... - The delta subunit of gamma-aminobutyric acid type A receptors does not confer sensitivity to low concentrations of ethanolCecilia M Borghese
The University of Texas at Austin, Waggoner Center for Alcohol and Addiction Research, 1 University Station A4800, Austin, TX 78712-0159, USA
J Pharmacol Exp Ther 316:1360-8. 2006..This suggests that as yet unidentified factors may play a critical role in the ethanol effects on delta-containing GABA(A)Rs... - Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analoguesStine B Vogensen
Department of Medicinal Chemistry and Department of Pharmacology, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK-2100 Copenhagen, Denmark
J Med Chem 48:3438-42. 2005..The 2-substituted isomers were selective agonists, and their activity correlated inversely with the size of the substituent. Structural explanations of the structure-activity relationship are provided... - Analogues of homoibotenic acid show potent and selective activity following sensitisation by quisqualic acidHenrik T Vestergaard
Department of Pharmacology, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK 2100 Copenhagen Ø, Denmark
Eur J Pharmacol 488:101-9. 2004..This demonstrates the involvement of a transport system in the mechanism underlying the quisqualate-effect... - Activation of single heteromeric GABA(A) receptor ion channels by full and partial agonistsMartin Mortensen
Department of Pharmacology, University College London, Gower Street, London WC1E 6BT, UK
J Physiol 557:389-413. 2004.... - Aza-THIP and related analogues of THIP as GABA C antagonistsDorte Krehan
Centre for Drug Design and Transport, Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, DK 2100 Copenhagen, Denmark
Bioorg Med Chem 11:4891-6. 2003.... - Activity of novel 4-PIOL analogues at human alpha 1 beta 2 gamma 2S GABA(A) receptors--correlation with hydrophobicityMartin Mortensen
Department of Pharmacology, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK-2100 Copenhagen, Denmark
Eur J Pharmacol 451:125-32. 2002.... - Correlation of the expression of kainate receptor subtypes to responses evoked in cultured cortical and spinal cord neuronesWei-Min Dai
Department of Physiology, University of Aarhus, , DK-8000 Aarhus C, Denmark
Brain Res 926:94-107. 2002..The most likely expression patterns of functional KA receptors is GluR6/KA2 for cortical neurones and GluR5/KA2 for spinal cord neurones...