Bjarke Ebert

Summary

Affiliation: H. Lundbeck A/S
Country: Denmark

Publications

  1. ncbi request reprint Treating insomnia: Current and investigational pharmacological approaches
    Bjarke Ebert
    Department of Electrophysiology, H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Copenhagen, Denmark
    Pharmacol Ther 112:612-29. 2006
  2. pmc 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
  3. ncbi request reprint Discontinued drugs 2007: central and peripheral nervous system drugs
    Bjarke Ebert
    Department of Electrophysiology, H Lundbeck A S, Ottiliavej 9, Valby, 2500, Denmark
    Expert Opin Investig Drugs 18:109-23. 2009
  4. ncbi request reprint Gaboxadol -- a different hypnotic profile with no tolerance to sleep EEG and sedative effects after repeated daily dosing
    Bjarke Ebert
    H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Denmark
    Pharmacol Biochem Behav 90:113-22. 2008
  5. ncbi request reprint Lack of generalisation between the GABAA receptor agonist, gaboxadol, and allosteric modulators of the benzodiazepine binding site in the rat drug discrimination procedure
    Signe Michelsen
    Department of Neuropharmacology, H Lundbeck A S, Ottiliavej 9, 2500, Copenhagen, Valby, Denmark
    Psychopharmacology (Berl) 193:151-7. 2007
  6. ncbi request reprint Rotarod studies in the rat of the GABAA receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-tolerance
    Jeppe Voss
    Department of Neuropharmacology, H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Denmark
    Eur J Pharmacol 482:215-22. 2003
  7. ncbi request reprint Pharmacological characterization of agonists at delta-containing GABAA receptors: Functional selectivity for extrasynaptic receptors is dependent on the absence of gamma2
    Signe I Storustovu
    Department of Electrophysiology, H Lundbeck A S, 9 Ottiliavej, DK 2500 Valby, Denmark
    J Pharmacol Exp Ther 316:1351-9. 2006
  8. ncbi request reprint Gaboxadol: in vitro interaction studies with benzodiazepines and ethanol suggest functional selectivity
    Signe I Storustovu
    Department of Molecular Pharmacology, H Lundbeck A S, 9 Ottiliavej, DK 2500 Valby, Denmark
    Eur J Pharmacol 467:49-56. 2003
  9. ncbi request reprint Upregulation of glutamate receptor subtypes during alcohol withdrawal in rats
    Steven Rosenzweig Haugbøl
    Department of Psychiatry, University Hospital Rigshospitalet, Copenhagen, Denmark
    Alcohol Alcohol 40:89-95. 2005
  10. ncbi request reprint Escitalopram versus citalopram: the surprising role of the R-enantiomer
    Connie Sanchez
    Research and Development, H Lundbeck A S, Ottiliavej 9, 2500 Valby Copenhagen, Denmark
    Psychopharmacology (Berl) 174:163-76. 2004

Collaborators

Detail Information

Publications32

  1. ncbi request reprint Treating insomnia: Current and investigational pharmacological approaches
    Bjarke Ebert
    Department of Electrophysiology, H Lundbeck A S, Ottiliavej 9, DK 2500 Valby, Copenhagen, Denmark
    Pharmacol Ther 112:612-29. 2006
    ....
  2. pmc 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...
  3. ncbi request reprint Discontinued drugs 2007: central and peripheral nervous system drugs
    Bjarke 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...
  4. ncbi request reprint Gaboxadol -- a different hypnotic profile with no tolerance to sleep EEG and sedative effects after repeated daily dosing
    Bjarke 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...
  5. ncbi request reprint Lack of generalisation between the GABAA receptor agonist, gaboxadol, and allosteric modulators of the benzodiazepine binding site in the rat drug discrimination procedure
    Signe Michelsen
    Department of Neuropharmacology, H Lundbeck A S, Ottiliavej 9, 2500, Copenhagen, Valby, Denmark
    Psychopharmacology (Berl) 193:151-7. 2007
    ....
  6. ncbi request reprint Rotarod studies in the rat of the GABAA receptor agonist gaboxadol: lack of ethanol potentiation and benzodiazepine cross-tolerance
    Jeppe 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...
  7. ncbi request reprint Pharmacological characterization of agonists at delta-containing GABAA receptors: Functional selectivity for extrasynaptic receptors is dependent on the absence of gamma2
    Signe I Storustovu
    Department of Electrophysiology, H Lundbeck A S, 9 Ottiliavej, DK 2500 Valby, Denmark
    J Pharmacol Exp Ther 316:1351-9. 2006
    ....
  8. ncbi request reprint Gaboxadol: in vitro interaction studies with benzodiazepines and ethanol suggest functional selectivity
    Signe 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...
  9. ncbi request reprint Upregulation of glutamate receptor subtypes during alcohol withdrawal in rats
    Steven Rosenzweig Haugbøl
    Department of Psychiatry, University Hospital Rigshospitalet, Copenhagen, Denmark
    Alcohol Alcohol 40:89-95. 2005
    ..To investigate glutamate receptor subtypes during alcohol withdrawal...
  10. ncbi request reprint Escitalopram versus citalopram: the surprising role of the R-enantiomer
    Connie 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...
  11. pmc 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
    Karsten 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...
  12. ncbi request reprint GABA(A) receptor ligands and their therapeutic potentials
    Bente Frølund
    Departments of Medicinal Chemistry, The Royal Danish School of Pharmacy, Copenhagen, DK 2100, Denmark
    Curr Top Med Chem 2:817-32. 2002
    ....
  13. pmc R-citalopram functionally antagonises escitalopram in vivo and in vitro: evidence for kinetic interaction at the serotonin transporter
    Signe 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...
  14. ncbi request reprint Molecular cloning and pharmacological characterization of serotonin 5-HT(3A) receptor subtype in dog
    Thomas 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...
  15. ncbi request reprint Plasma and CNS concentrations of Gaboxadol in rats following subcutaneous administration
    Thomas 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...
  16. ncbi request reprint Gaboxadol--a new awakening in sleep
    Keith 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...
  17. ncbi request reprint Pharmacology of GABA(A) receptors exhibiting different levels of spontaneous activity
    Martin 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...
  18. ncbi request reprint 4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships
    Bente 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...
  19. ncbi request reprint Extrasynaptic GABA(A) channels activated by THIP are modulated by diazepam in CA1 pyramidal neurons in the rat brain hippocampal slice
    Catarina 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...
  20. ncbi request reprint GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic
    Povl 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...
  21. ncbi request reprint Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake time
    Keith A Wafford
    Eli Lilly UK, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK
    Nat Rev Drug Discov 7:530-40. 2008
    ....
  22. ncbi request reprint 5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists
    Christian 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...
  23. ncbi request reprint A tetrazolyl-substituted subtype-selective AMPA receptor agonist
    Stine 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
    ....
  24. ncbi request reprint GABA(A) receptor inhibition - site matters!
    Bjarke Ebert
    Acta Physiol (Oxf) 188:151. 2006
  25. ncbi request reprint Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology
    Dorte 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...
  26. ncbi request reprint The delta subunit of gamma-aminobutyric acid type A receptors does not confer sensitivity to low concentrations of ethanol
    Cecilia 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...
  27. ncbi request reprint Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues
    Stine 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...
  28. ncbi request reprint Analogues of homoibotenic acid show potent and selective activity following sensitisation by quisqualic acid
    Henrik 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...
  29. pmc Activation of single heteromeric GABA(A) receptor ion channels by full and partial agonists
    Martin Mortensen
    Department of Pharmacology, University College London, Gower Street, London WC1E 6BT, UK
    J Physiol 557:389-413. 2004
    ....
  30. ncbi request reprint Aza-THIP and related analogues of THIP as GABA C antagonists
    Dorte 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
    ....
  31. ncbi request reprint Activity of novel 4-PIOL analogues at human alpha 1 beta 2 gamma 2S GABA(A) receptors--correlation with hydrophobicity
    Martin Mortensen
    Department of Pharmacology, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen Ø, Denmark
    Eur J Pharmacol 451:125-32. 2002
    ....
  32. ncbi request reprint Correlation of the expression of kainate receptor subtypes to responses evoked in cultured cortical and spinal cord neurones
    Wei Min Dai
    Department of Physiology, University of Aarhus, Ole Worms Alle 160, 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...