Finn Olav Levy

Summary

Affiliation: University of Oslo
Country: Norway

Publications

  1. doi request reprint Cardiac PDEs and crosstalk between cAMP and cGMP signalling pathways in the regulation of contractility
    Finn Olav Levy
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Sognsvannsveien 20, P O Box 1057 Blindern, 0316, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 386:665-70. 2013
  2. doi request reprint Effects of serotonin in failing cardiac ventricle: signalling mechanisms and potential therapeutic implications
    Finn Olav Levy
    Department of Pharmacology, Faculty of Medicine, University of Oslo, P O Box 1057 Blindern, N 0316 Oslo, Norway
    Neuropharmacology 55:1066-71. 2008
  3. ncbi request reprint Serotonin responsiveness through 5-HT2A and 5-HT4 receptors is differentially regulated in hypertrophic and failing rat cardiac ventricle
    Trond Brattelid
    Department of Pharmacology, University of Oslo, Sognsvannsvn 20, Oslo, Norway
    J Mol Cell Cardiol 43:767-79. 2007
  4. ncbi request reprint Appearance of a ventricular 5-HT4 receptor-mediated inotropic response to serotonin in heart failure
    Eirik Qvigstad
    Department of Pharmacology, University of Oslo, 0316 Oslo, Norway
    Cardiovasc Res 65:869-78. 2005
  5. doi request reprint Prostanoid F receptors elicit an inotropic effect in rat left ventricle by enhancing myosin light chain phosphorylation
    Jon Riise
    Department of Pharmacology, University of Oslo, Sognsvannsvn 20, Building A2 A3, PO Box 1057 Blindern, N 0316 Oslo, Norway
    Cardiovasc Res 80:407-15. 2008
  6. ncbi request reprint Heterologous desensitization is evoked by both agonist and antagonist stimulation of the human 5-HT(7) serotonin receptor
    Kurt A Krobert
    Department of Pharmacology and Center for Heart Failure Research, University of Oslo, Blindern, N 0316 Oslo, Norway
    Eur J Pharmacol 532:1-10. 2006
  7. ncbi request reprint Dual serotonergic regulation of ventricular contractile force through 5-HT2A and 5-HT4 receptors induced in the acute failing heart
    Eirik Qvigstad
    Department of Pharmacology, University of Oslo, PO Box 1057 Blindern, 0316 Oslo, Norway
    Circ Res 97:268-76. 2005
  8. pmc The cardiac ventricular 5-HT4 receptor is functional in late foetal development and is reactivated in heart failure
    Trond Brattelid
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway
    PLoS ONE 7:e45489. 2012
  9. pmc Agents increasing cyclic GMP amplify 5-HT4-elicited positive inotropic response in failing rat cardiac ventricle
    Faraz Afzal
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, P O Box 1057 Blindern, 0316, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 384:543-53. 2011
  10. doi request reprint Prostanoid-mediated inotropic responses are attenuated in failing human and rat ventricular myocardium
    Jon Riise
    Department of Pharmacology, Institute of Clinical Medicine, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway
    Eur J Pharmacol 686:66-73. 2012

Collaborators

Detail Information

Publications50

  1. doi request reprint Cardiac PDEs and crosstalk between cAMP and cGMP signalling pathways in the regulation of contractility
    Finn Olav Levy
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Sognsvannsveien 20, P O Box 1057 Blindern, 0316, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 386:665-70. 2013
    ..If present in human hearts, this effect of CNP may have clinical implications. ..
  2. doi request reprint Effects of serotonin in failing cardiac ventricle: signalling mechanisms and potential therapeutic implications
    Finn Olav Levy
    Department of Pharmacology, Faculty of Medicine, University of Oslo, P O Box 1057 Blindern, N 0316 Oslo, Norway
    Neuropharmacology 55:1066-71. 2008
    ..Further studies are needed to clarify if such treatment will be useful for patients with heart failure...
  3. ncbi request reprint Serotonin responsiveness through 5-HT2A and 5-HT4 receptors is differentially regulated in hypertrophic and failing rat cardiac ventricle
    Trond Brattelid
    Department of Pharmacology, University of Oslo, Sognsvannsvn 20, Oslo, Norway
    J Mol Cell Cardiol 43:767-79. 2007
    ..While the 5-HT(2A)-mediated PIR is linearly correlated with the degree of hypertrophy, the 5-HT(4)-mediated PIR seems to increase with LV dilatation, as also seen in postinfarction CHF...
  4. ncbi request reprint Appearance of a ventricular 5-HT4 receptor-mediated inotropic response to serotonin in heart failure
    Eirik Qvigstad
    Department of Pharmacology, University of Oslo, 0316 Oslo, Norway
    Cardiovasc Res 65:869-78. 2005
    ..Serotonin [5-hydroxytryptamine (5-HT)] enhances contractility and causes arrhythmias through 5-HT(4) receptors in human atrium and ventricle but not through rat ventricular 5-HT(4) receptors...
  5. doi request reprint Prostanoid F receptors elicit an inotropic effect in rat left ventricle by enhancing myosin light chain phosphorylation
    Jon Riise
    Department of Pharmacology, University of Oslo, Sognsvannsvn 20, Building A2 A3, PO Box 1057 Blindern, N 0316 Oslo, Norway
    Cardiovasc Res 80:407-15. 2008
    ....
  6. ncbi request reprint Heterologous desensitization is evoked by both agonist and antagonist stimulation of the human 5-HT(7) serotonin receptor
    Kurt A Krobert
    Department of Pharmacology and Center for Heart Failure Research, University of Oslo, Blindern, N 0316 Oslo, Norway
    Eur J Pharmacol 532:1-10. 2006
    ..It is concluded that the human 5-HT(7) receptor mediates heterologous desensitization of endogenous G(s)-coupled receptors through an unknown and potentially novel mechanism...
  7. ncbi request reprint Dual serotonergic regulation of ventricular contractile force through 5-HT2A and 5-HT4 receptors induced in the acute failing heart
    Eirik Qvigstad
    Department of Pharmacology, University of Oslo, PO Box 1057 Blindern, 0316 Oslo, Norway
    Circ Res 97:268-76. 2005
    ..Ca2+ transients were slightly decreased by 5-HT2A stimulation. The acute failing rat ventricle is, thus, dually regulated by serotonin through Gq-coupled 5-HT2A receptors and Gs-coupled 5-HT4 receptors...
  8. pmc The cardiac ventricular 5-HT4 receptor is functional in late foetal development and is reactivated in heart failure
    Trond Brattelid
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway
    PLoS ONE 7:e45489. 2012
    ..We suggest that the 5-HT(4) receptor is a representative of a foetal cardiac gene program, functional in late foetal development and reactivated in heart failure...
  9. pmc Agents increasing cyclic GMP amplify 5-HT4-elicited positive inotropic response in failing rat cardiac ventricle
    Faraz Afzal
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, P O Box 1057 Blindern, 0316, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 384:543-53. 2011
    ..Thus, cGMP from different sources is functionally compartmented, giving differential regulation of different G(s)-coupled receptors...
  10. doi request reprint Prostanoid-mediated inotropic responses are attenuated in failing human and rat ventricular myocardium
    Jon Riise
    Department of Pharmacology, Institute of Clinical Medicine, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway
    Eur J Pharmacol 686:66-73. 2012
    ..The pathophysiological significance of changes in prostanoid-mediated inotropic support in the failing heart remains to be determined...
  11. doi request reprint Prostaglandin E1 facilitates inotropic effects of 5-HT4 serotonin receptors and β-adrenoceptors in failing human heart
    Jon Riise
    Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Sognsvannsvn 20, Blindern, Oslo, Norway
    Basic Res Cardiol 107:295. 2012
    ..This effect of PGE(1) possibly contributes to the increase of cardiac output, independent of decreased afterload, observed after prostaglandin administration in humans...
  12. doi request reprint Natriuretic peptides increase beta1-adrenoceptor signalling in failing hearts through phosphodiesterase 3 inhibition
    Eirik Qvigstad
    Department of Pharmacology, University of Oslo, PO Box 1057 Blindern, Oslo 0316, Norway
    Cardiovasc Res 85:763-72. 2010
    ....
  13. doi request reprint Diastolic dysfunction in alveolar hypoxia: a role for interleukin-18-mediated increase in protein phosphatase 2A
    Karl Otto Larsen
    Department of Pulmonary Medicine, Ulleval University Hospital, University of Oslo, Oslo, Norway
    Cardiovasc Res 80:47-54. 2008
    ..Here, we study the mechanisms leading to the hypoxia-induced reduction in phosphorylation of phospholamban at Ser16...
  14. ncbi request reprint Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants
    Kurt A Krobert
    Department of Pharmacology, University of Oslo, P O Box 1057, Blindern, 0316 Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 371:473-9. 2005
    ..Since prucalopride acts similarly through 5-HT4(a), 5-HT4(b), 5-HT4(g), and 5-HT4(i) receptors, any of these variants could be involved in the mediation of cardiostimulation...
  15. ncbi request reprint Expression of mRNA encoding G protein-coupled receptors involved in congestive heart failure--a quantitative RT-PCR study and the question of normalisation
    Trond Brattelid
    Dept of Pharmacology, University of Oslo, 1057, Blindern, 0316 Oslo, Norway
    Basic Res Cardiol 102:198-208. 2007
    ..Q-RT-PCR is a sensitive and powerful method to monitor changes in GPCR mRNA expression in CHF. However, the normalisation standard used is important for the interpretation of mRNA regulation...
  16. doi request reprint Connective tissue growth factor/CCN2 attenuates β-adrenergic receptor responsiveness and cardiotoxicity by induction of G protein-coupled receptor kinase-5 in cardiomyocytes
    Jørgen Gravning
    Institute for Surgical Research, Oslo University Hospital and University of Oslo, Oslo, Norway
    Mol Pharmacol 84:372-83. 2013
    ..In conclusion, this study uncovers a novel mechanism controlling β-AR responsiveness in cardiomyocytes involving CTGF-mediated regulation of GRK5...
  17. ncbi request reprint Cloning, pharmacological characterisation and tissue distribution of a novel 5-HT4 receptor splice variant, 5-HT4(i)
    Trond Brattelid
    Department of Pharmacology, University of Oslo, PO Box 1057, 0316, Blindern, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 369:616-28. 2004
    ..We conclude that the novel 5-HT4(i) receptor splice variant is pharmacologically indistinguishable from other 5-HT4 splice variants and that the 5-HT4(i) C-terminal tail does not influence coupling to AC...
  18. pmc Differential regulation of β2 -adrenoceptor-mediated inotropic and lusitropic response by PDE3 and PDE4 in failing and non-failing rat cardiac ventricle
    Faraz Afzal
    Department of Pharmacology, Faculty of Medicine, University of Oslo, Norway
    Br J Pharmacol 162:54-71. 2011
    ..We explored the involvement of PDEs in limiting the β(2) adrenoceptor-mediated positive inotropic (PIR) and lusitropic (LR) responses in sham-operated (Sham) and failing rat hearts...
  19. ncbi request reprint Endogenous expression and protein kinase A-dependent phosphorylation of the guanine nucleotide exchange factor Ras-GRF1 in human embryonic kidney 293 cells
    Jens Henrik Norum
    Department of Pharmacology, University of Oslo, Norway
    FEBS J 272:2304-16. 2005
    ..Therefore, both cAMP and Ca2+ may contribute to the Ras-dependent ERK1/2 activation after 5-HT7 receptor stimulation, through activation of a guanine nucleotide exchange factor with activity towards Ras...
  20. ncbi request reprint Epac- and Rap- independent ERK1/2 phosphorylation induced by Gs-coupled receptor stimulation in HEK293 cells
    Jens Henrik Norum
    Department of Pharmacology, University of Oslo, N 0316 Oslo, Norway
    FEBS Lett 581:15-20. 2007
    ..Different signalling pathways seem to be utilised by G(s)-coupled receptors in various isolates of HEK293 cells...
  21. ncbi request reprint Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure
    Trond Brattelid
    Department of Pharmacology, University of Oslo, P O Box 1057 Blindern, 0316 Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 370:157-66. 2004
    ..We conclude that phosphodiesterase inhibition uncovers functional ventricular 5-HT(4) receptors, coupled to a PKA pathway, through which 5-HT enhances contractility, hastens relaxation and can potentially cause arrhythmias...
  22. doi request reprint Calculating reaction rate constants and estimating the efficacy of selective enzyme inhibitors
    Hilde Eikemo
    Department of Pharmacology and Center for Heart Failure Research, University of Oslo, N 0316 Oslo, Norway
    Anal Biochem 383:323-5. 2008
    ..Here we present and discuss a method for calculating the reaction rate constants and, thus, for evaluating the efficacy of one or more inhibitors when introduced to a forward-backward pair of enzymatic reactions...
  23. ncbi request reprint Substrate specificities of g protein-coupled receptor kinase-2 and -3 at cardiac myocyte receptors provide basis for distinct roles in regulation of myocardial function
    Leif Erik Vinge
    Institute for Surgical Research, Rikshospitalet Radiumhospitalet Medical Center, University of Oslo, Oslo, Norway
    Mol Pharmacol 72:582-91. 2007
    ....
  24. doi request reprint CaMKII in addition to MLCK contributes to phosphorylation of regulatory light chain in cardiomyocytes
    Hilde Eikemo
    Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway K G Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway Electronic address
    Biochem Biophys Res Commun 471:219-25. 2016
    ..RLC phosphorylation was insensitive to protein kinase C inhibition. In conclusion, in addition to MLCK, CaMKII phosphorylates RLC in cardiomyocytes. Involvement of other kinases cannot be excluded. ..
  25. pmc The inotropic effect of the active metabolite of levosimendan, OR-1896, is mediated through inhibition of PDE3 in rat ventricular myocardium
    Øivind Ørstavik
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway K G Jebsen Cardiac Research Centre, Faculty of Medicine, University of Oslo, Oslo, Norway Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway
    PLoS ONE 10:e0115547. 2015
    ....
  26. doi request reprint Non-classical regulation of β1- and β 2-adrenoceptor-mediated inotropic responses in rat heart ventricle by the G protein Gi
    Caroline Bull Melsom
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 387:1177-86. 2014
    ..Gi together with PDE3&4 tonically restrict the β2AR-IR. Gi inhibition did not restore the βAR-IR in HF despite increasing cAMP levels, suggesting that the mechanism of impairment resides downstream to cAMP signalling...
  27. doi request reprint Different compartmentation of responses to brain natriuretic peptide and C-type natriuretic peptide in failing rat ventricle
    Lise Román Moltzau
    Department of Pharmacology L R M, S M, Ø Ø, T S, J B O, F O L, E Q and Institute for Experimental Medical Research J M A, J S, G B L, I S, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital K G Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway L R M, S M, J S, Ø Ø, I S, T S, J B O, F O L, E Q and Bjørknes College, Oslo, Norway J M A, G B L
    J Pharmacol Exp Ther 350:681-90. 2014
    ..In conclusion, different responses to cGMP generated by BNP and CNP suggest different compartmentation of the cGMP signal and different roles of the two NPs in the failing heart. ..
  28. doi request reprint Differential regulation of C-type natriuretic peptide-induced cGMP and functional responses by PDE2 and PDE3 in failing myocardium
    Lise Román Moltzau
    Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Sognsvannsveien 20, P O Box 1057 Blindern, N 0316, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 387:407-17. 2014
    ....
  29. ncbi request reprint Activation of adenylyl cyclase by endogenous G(s)-coupled receptors in human embryonic kidney 293 cells is attenuated by 5-HT(7) receptor expression
    Kjetil Wessel Andressen
    Department of Pharmacology, University of Oslo, P O Box 1057 Blindern, N 0316 Oslo, Norway
    Mol Pharmacol 69:207-15. 2006
    ..Although the 5-HT(7) receptor may preassociate with G protein and/or AC, the mechanism of this heterologous desensitization remains elusive...
  30. doi request reprint Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists
    Bjarne Brudeli
    Drug Discovery Laboratory AS, Oslo Research Park, Oslo, Norway
    Bioorg Med Chem 18:8600-13. 2010
    ..These new molecules may be useful to target peripheral 5-HT(4) receptors...
  31. doi request reprint Effect of piboserod, a 5-HT4 serotonin receptor antagonist, on left ventricular function in patients with symptomatic heart failure
    John K Kjekshus
    Department of Cardiology, Oslo University Hospital, Rikshospitalet, Sognsvannsveien 20, Oslo, Norway
    Eur J Heart Fail 11:771-8. 2009
    ..Blockade of 5-HT(4) receptors reduced left ventricular (LV) remodelling in HF rats. We evaluated the effect of piboserod, a potent, selective, 5-HT(4) serotonin receptor antagonist, on LV function in patients with HF...
  32. doi request reprint CaMKII and at least two unidentified kinases phosphorylate regulatory light chain in non-contracting cardiomyocytes
    Hilde Eikemo
    Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway Center for Heart Failure Research, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway Electronic address
    Biochem Biophys Res Commun 477:14-9. 2016
    ..Thus the RLC phosphorylation seems to be ensured by redundant kinase activities. ..
  33. doi request reprint Discovery and pharmacological profile of new hydrophilic 5-HT(4) receptor antagonists
    Bjarne Brudeli
    Drug Discovery Laboratory AS, Oslo Innovation Center, N 0349 Oslo, Norway Department of Medicinal Chemistry, School of Pharmacy, University of Oslo, PO Box 1068 Blindern, N 0316 Oslo, Norway
    Bioorg Med Chem Lett 24:4598-602. 2014
    ..Propanediol derivative 25 was identified as a potent antagonist with low affinity for the hERG potassium channel and promising pharmacokinetics. ..
  34. doi request reprint EBV infection renders B cells resistant to growth inhibition via adenylyl cyclase
    Martine Müller Kloster
    Department of Biochemistry, Institute of Basic Medical Sciences, University of Oslo, N 0317 Oslo, Norway
    Cell Signal 20:1169-78. 2008
    ..We conclude that EBV infection of B cells abrogates the activation of AC and thereby cAMP formation, and that this dysfunction renders the cells resistant to growth inhibition via the cAMP/PKA pathway...
  35. doi request reprint Acidic biphenyl derivatives: synthesis and biological activity of a new series of potent 5-HT(4) receptor antagonists
    Bjarne Brudeli
    Drug Discovery Laboratory AS, Oslo Innovation Center, N 0349 Oslo, Norway Department of Medicinal Chemistry, School of Pharmacy, University of Oslo, PO Box 1068 Blindern, N 0316 Oslo, Norway
    Bioorg Med Chem 21:7134-45. 2013
    ..Methyl ester 20 has promising oral bioavailability and pharmacokinetics and may target 5-HT4 receptors in both CNS and peripheral organs. ..
  36. doi request reprint Identification of small molecule NPR-B antagonists by high throughput screening--potential use in heart failure
    Trond Bach
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Sognsvannsveien 20, P O Box 1057, Blindern, 0316, Oslo, Norway
    Naunyn Schmiedebergs Arch Pharmacol 387:5-14. 2014
    ....
  37. doi request reprint Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist
    Bjarne Brudeli
    Drug Discovery Laboratory AS, Oslo Innovation Center, N 0349 Oslo, Norway
    Eur J Med Chem 64:629-37. 2013
    ..The medoxomil ester prodrug 10 showed complete conversion and sufficient bioavailability of 9 to advance into further preclinical testing for treatment of heart failure...
  38. ncbi request reprint RAMP2 and RAMP3 mRNA levels are increased in failing rat cardiomyocytes and associated with increased responsiveness to adrenomedullin
    Erik Øie
    MSD Cardiovascular Research Center, Rikshospitalet University Hospital, University of Oslo, N 0027 Oslo, Norway
    J Mol Cell Cardiol 38:145-51. 2005
    ..Furthermore, our data suggest that induction of RAMP2 and RAMP3 contributes to the increased responsiveness to AM in failing cardiomyocytes...
  39. pmc Gi proteins regulate adenylyl cyclase activity independent of receptor activation
    Caroline Bull Melsom
    Department of Pharmacology, Faculty of Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway K G Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway
    PLoS ONE 9:e106608. 2014
    ..Therefore, we wanted to determine if Gi exerts tonic receptor-independent inhibition upon basal adenylyl cyclase (AC) activity in cardiomyocytes...
  40. pmc Reference gene alternatives to Gapdh in rodent and human heart failure gene expression studies
    Trond Brattelid
    Institute for Experimental Medical Research, Oslo University Hospital Ulleval, Oslo, Norway
    BMC Mol Biol 11:22. 2010
    ..Our aim was to evaluate and identify suitable reference genes in human failing myocardium, in rat and mouse post-myocardial infarction (post-MI) heart failure and across developmental stages in fetal and neonatal rat myocardium...
  41. ncbi request reprint Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a)
    Jens Henrik Norum
    Merck Sharp and Dohme Cardiovascular Research Center, Institute for Surgical Research and Department of Pharmacology, Rikshospitalet University Hospital, University of Oslo, N 0316 Oslo, Norway
    J Biol Chem 278:3098-104. 2003
    ..These findings suggest that activation of ERK1/2 through the human G(s)-coupled serotonin receptors 5-HT(4(b)) and 5-HT(7(a)) in HEK293 cells is dependent on Ras, but independent of Rap1...
  42. ncbi request reprint Unaltered agonist potency upon inducible 5-HT7(a) but not 5-HT4(b) receptor expression indicates agonist-independent association of 5-HT7(a) receptor and Gs
    Skjalg Bruheim
    MSD Cardiovascular Research Center, Institute for Surgical Research, Department of Pharmacology, University of Oslo, Rikshospitalet University Hospital, Oslo, Norway
    Receptors Channels 9:107-16. 2003
    ..In such a system, spare receptors do not lead to increased potency of an agonist with increased receptor density...
  43. doi request reprint Downregulation of 5-HT7 Serotonin Receptors by the Atypical Antipsychotics Clozapine and Olanzapine. Role of Motifs in the C-Terminal Domain and Interaction with GASP-1
    Ornella Manfra
    Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, P O Box 1057 Blindern, 0316 Oslo, Norway
    ACS Chem Neurosci 6:1206-18. 2015
    ..Taken together, our data demonstrate that binding of clozapine or olanzapine to the 5-HT7 receptor leads to antagonist-mediated lysosomal degradation by exposing key residues in the C-terminal tail that interact with GASP-1. ..
  44. ncbi request reprint Alpha1-AR-mediated activation of NKCC in rat cardiomyocytes involves ERK-dependent phosphorylation of the cotransporter
    Geir Øystein Andersen
    Department of Pharmacology, University of Oslo, Oslo, Norway
    Am J Physiol Heart Circ Physiol 286:H1354-60. 2004
    ..We conclude that the NKCC is present in rat cardiomyocytes and that ion transport by the cotransporter is regulated by alpha(1)-AR stimulation through phosphorylation of this protein involving the ERK pathway...
  45. doi request reprint The heterotrimeric G-protein alpha-subunit Galphaq regulates TCR-mediated immune responses through an Lck-dependent pathway
    Jacob Ngai
    The Biotechnology Centre of Oslo, Nordic EMBL Partnership, University of Oslo, Oslo, Norway
    Eur J Immunol 38:3208-18. 2008
    ..Together these data argue for a role of Galphaq in the fine-tuning of proximal TCR signals at the level of Lck and a negative regulatory role of Galphaq in transcriptional activation of cytokine responses...
  46. pmc Low β₂-adrenergic receptor level may promote development of castration resistant prostate cancer and altered steroid metabolism
    Peder Rustøen Braadland
    Department of Tumor Biology, Institute for Cancer Research, Oslo University Hospital, Oslo, Norway
    Oncotarget 7:1878-94. 2016
    ..Similar to ADRB2, we show that low levels of UGT2B15 are associated with a more rapid CRPC progression. We propose a novel mechanism by which ADRB2 may affect the development of CRPC through downregulation of UGT2B15 and UGT2B17...
  47. doi request reprint NSC23766, a widely used inhibitor of Rac1 activation, additionally acts as a competitive antagonist at muscarinic acetylcholine receptors
    Magdolna Lévay
    Institute of Experimental Pharmacology and Toxicology, Medical Faculty Mannheim, Heidelberg University, Mannheim, Germany M L, K W, T W DZHK German Center for Cardiovascular Research, Partner Site, Heidelberg Mannheim, Mannheim, Germany M L, D D, T W Department of Pharmacology, Institute of Clinical Medicine, Faculty of Medicine and K G Jebsen Cardiac Research Center and Center for Heart Failure Research, University of Oslo, Oslo, Norway K A K, F O V Institute of Pharmacology, Faculty of Medicine, University Duisburg Essen, Essen, Germany, and Division of Experimental Cardiology, Medical Faculty Mannheim, Heidelberg University, Mannheim, Germany N V, D D and Computer Aided Drug Design, Institute of Pharmacy, Free University of Berlin, Berlin, Germany M B, G W
    J Pharmacol Exp Ther 347:69-79. 2013
    ..Molecular docking analysis at M2 and M3 mAChR crystal structures confirmed this interpretation. ..
  48. pmc Retinoic acid signalling is activated in the postischemic heart and may influence remodelling
    Dusan Bilbija
    Department of Physiology, University of Oslo, Oslo, Norway
    PLoS ONE 7:e44740. 2012
    ..We hypothesized that the retinoic acid (RA) signalling pathway is activated in myocardial ischemia and postischemic remodelling...
  49. pmc The human 5-HT7 serotonin receptor splice variants: constitutive activity and inverse agonist effects
    Kurt A Krobert
    MSD Cardiovascular Research Center, University of Oslo, Rikshospitalet University Hospital, Blindern, N 0316 Oslo, Norway
    Br J Pharmacol 135:1563-71. 2002
    ..6. It is concluded that the h5-HT(7) splice variants display similar constitutive activity and inverse agonist properties...
  50. doi request reprint Hormonal regulation of beta2-adrenergic receptor level in prostate cancer
    Håkon Ramberg
    Faculty Division Aker University Hospital, University of Oslo, Oslo Urological University Clinic, Aker University Hospital, Oslo, Norway
    Prostate 68:1133-42. 2008
    ..The beta(2)-adrenergic receptor (beta(2)-AR) is a well-known activator of the androgen receptor...