Christopher J Fowler

Summary

Country: Sweden

Publications

  1. ncbi Acidic nonsteroidal anti-inflammatory drugs inhibit rat brain fatty acid amide hydrolase in a pH-dependent manner
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    J Enzyme Inhib Med Chem 18:55-8. 2003
  2. pmc Association between cannabinoid CB₁ receptor expression and Akt signalling in prostate cancer
    Mariateresa Cipriano
    Pharmacology, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 8:e65798. 2013
  3. pmc Fatty acid amide hydrolase in prostate cancer: association with disease severity and outcome, CB1 receptor expression and regulation by IL-4
    Lina Thors
    Pharmacology Unit, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 5:e12275. 2010
  4. pmc Tumour Cannabinoid CB(1) receptor and phosphorylated epidermal growth factor receptor expression are additive prognostic markers for prostate cancer
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umea University, Umea, Sweden
    PLoS ONE 5:e15205. 2010
  5. pmc High tumour cannabinoid CB1 receptor immunoreactivity negatively impacts disease-specific survival in stage II microsatellite stable colorectal cancer
    Sofia B Gustafsson
    Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umea University, Umea, Sweden
    PLoS ONE 6:e23003. 2011
  6. pmc Phospho-Akt immunoreactivity in prostate cancer: relationship to disease severity and outcome, Ki67 and phosphorylated EGFR expression
    Peter Hammarsten
    Department of Medical Biosciences, Pathology, Umea University, Umea, Sweden
    PLoS ONE 7:e47994. 2012
  7. doi Ketoconazole inhibits the cellular uptake of anandamide via inhibition of FAAH at pharmacologically relevant concentrations
    Emmelie Björklund
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 9:e87542. 2014
  8. doi Tumour epithelial expression levels of endocannabinoid markers modulate the value of endoglin-positive vascular density as a prognostic marker in prostate cancer
    Christopher J Fowler
    Pharmacology Unit, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden Electronic address
    Biochim Biophys Acta 1831:1579-87. 2013
  9. doi Transport of endocannabinoids across the plasma membrane and within the cell
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    FEBS J 280:1895-904. 2013
  10. pmc Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamide
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    J Enzyme Inhib Med Chem 28:172-82. 2013

Collaborators

Detail Information

Publications80

  1. ncbi Acidic nonsteroidal anti-inflammatory drugs inhibit rat brain fatty acid amide hydrolase in a pH-dependent manner
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    J Enzyme Inhib Med Chem 18:55-8. 2003
    ..The data are consistent with the conclusion that the non-ionised forms of the acidic NSAIDs are responsible for the inhibition of fatty acid amide hydrolase...
  2. pmc Association between cannabinoid CB₁ receptor expression and Akt signalling in prostate cancer
    Mariateresa Cipriano
    Pharmacology, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 8:e65798. 2013
    ..In the present study, we have investigated the association between CB₁ receptor expression and the Akt pathway in a well-characterised prostate cancer tissue microarray...
  3. pmc Fatty acid amide hydrolase in prostate cancer: association with disease severity and outcome, CB1 receptor expression and regulation by IL-4
    Lina Thors
    Pharmacology Unit, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 5:e12275. 2010
    ....
  4. pmc Tumour Cannabinoid CB(1) receptor and phosphorylated epidermal growth factor receptor expression are additive prognostic markers for prostate cancer
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umea University, Umea, Sweden
    PLoS ONE 5:e15205. 2010
    ....
  5. pmc High tumour cannabinoid CB1 receptor immunoreactivity negatively impacts disease-specific survival in stage II microsatellite stable colorectal cancer
    Sofia B Gustafsson
    Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umea University, Umea, Sweden
    PLoS ONE 6:e23003. 2011
    ..In the present study, we have investigated whether CB(1) receptor immunoreactive intensity (CB(1)IR intensity) is associated with disease severity and outcome...
  6. pmc Phospho-Akt immunoreactivity in prostate cancer: relationship to disease severity and outcome, Ki67 and phosphorylated EGFR expression
    Peter Hammarsten
    Department of Medical Biosciences, Pathology, Umea University, Umea, Sweden
    PLoS ONE 7:e47994. 2012
    ....
  7. doi Ketoconazole inhibits the cellular uptake of anandamide via inhibition of FAAH at pharmacologically relevant concentrations
    Emmelie Björklund
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 9:e87542. 2014
    ..In the present study, we have investigated whether ketoconazole affects the cellular uptake and hydrolysis of the endogenous cannabinoid receptor ligand anandamide (AEA)...
  8. doi Tumour epithelial expression levels of endocannabinoid markers modulate the value of endoglin-positive vascular density as a prognostic marker in prostate cancer
    Christopher J Fowler
    Pharmacology Unit, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden Electronic address
    Biochim Biophys Acta 1831:1579-87. 2013
    ..This article is part of a Special Issue entitled Lipid Metabolism in Cancer. ..
  9. doi Transport of endocannabinoids across the plasma membrane and within the cell
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    FEBS J 280:1895-904. 2013
    ....
  10. pmc Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamide
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    J Enzyme Inhib Med Chem 28:172-82. 2013
    ..Compound 2 was confirmed to be active in vivo in a murine model of visceral nociception, but the effects of the compound were not blocked by CB receptor antagonists...
  11. pmc Monoacylglycerol lipase - a target for drug development?
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Br J Pharmacol 166:1568-85. 2012
    ..In this review, the pharmacology of monoacylglycerol lipase will be discussed, together with an analysis of the therapeutic potential of monoacylglycerol lipase inhibitors as analgesics and anticancer agents...
  12. doi Anandamide uptake explained?
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Trends Pharmacol Sci 33:181-5. 2012
    ..In this article I review the current state of the art of endocannabinoid uptake...
  13. ncbi The cannabinoid system and its pharmacological manipulation--a review, with emphasis upon the uptake and hydrolysis of anandamide
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
    Fundam Clin Pharmacol 20:549-62. 2006
    ....
  14. ncbi The endocannabinoid signaling system: pharmacological and therapeutic aspects
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
    Pharmacol Biochem Behav 81:248-62. 2005
    ..Modulation of the endocannabionid system may also produce neuroprotective effects, although present data would suggest that the observed effects are highly dependent upon the nature of the neurotoxic insult...
  15. ncbi Cyclooxygenation of the arachidonoyl side chain of 1-arachidonoylglycerol and related compounds block their ability to prevent anandamide and 2-oleoylglycerol metabolism by rat brain in vitro
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 90187 Umea, Sweden
    Biochem Pharmacol 69:1241-5. 2005
    ..Thus, cyclooxygenation of the arachidonoyl side chain greatly reduces the ability of 1-arachidonoylglycerol and related compounds to inhibit the hydrolysis of [3H]2-oleoylglycerol and [3H]anandamide...
  16. ncbi Selective inhibition of anandamide cellular uptake versus enzymatic hydrolysis--a difficult issue to handle
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Eur J Pharmacol 492:1-11. 2004
    ..It is concluded that the cause/effect relationship between AEA uptake and hydrolysis cannot be investigated uniquely by using supposedly selective inhibitors of each process...
  17. ncbi Possible involvement of the endocannabinoid system in the actions of three clinically used drugs
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Trends Pharmacol Sci 25:59-61. 2004
    ..In this article, the findings of these studies are summarized and possible spectra of actions of these drugs is discussed...
  18. pmc Oleamide: a member of the endocannabinoid family?
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Br J Pharmacol 141:195-6. 2004
    ..In the present issue of this journal, Leggett et al present data indicating that oleamide functionally activates CB(1) cannabinoid receptors in vitro. The significance of their finding is discussed in this commentary...
  19. pmc The contribution of cyclooxygenase-2 to endocannabinoid metabolism and action
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    Br J Pharmacol 152:594-601. 2007
    ....
  20. ncbi The pharmacology of the cannabinoid system--a question of efficacy and selectivity
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 90187, Umea, Sweden
    Mol Neurobiol 36:15-25. 2007
    ....
  21. doi Does the hydrolysis of 2-arachidonoylglycerol regulate its cellular uptake?
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
    Pharmacol Res 58:72-6. 2008
    ..It is concluded that unlike the situation for anandamide, hydrolysis of 2-AG does not regulate its cellular uptake in RBL2H3, AT-1 and PC3 cells, but may gate the uptake in Neuro-2a cells...
  22. ncbi "The tools of the trade"--an overview of the pharmacology of the endocannabinoid system
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Curr Pharm Des 14:2254-65. 2008
    ....
  23. pmc The case for the development of novel analgesic agents targeting both fatty acid amide hydrolase and either cyclooxygenase or TRPV1
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Br J Pharmacol 156:412-9. 2009
    ..Although finding the right balance of actions upon the two targets is a key to success, it is hoped that dual-action compounds of the types illustrated in this review will prove to be useful analgesic drugs...
  24. ncbi Modulation of the endocannabinoid system: neuroprotection or neurotoxicity?
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Exp Neurol 224:37-47. 2010
    ....
  25. ncbi Targeting the endocannabinoid system for the treatment of cancer--a practical view
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    Curr Top Med Chem 10:814-27. 2010
    ....
  26. ncbi Fatty acid amide hydrolase: biochemistry, pharmacology, and therapeutic possibilities for an enzyme hydrolyzing anandamide, 2-arachidonoylglycerol, palmitoylethanolamide, and oleamide
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Biochem Pharmacol 62:517-26. 2001
    ....
  27. ncbi Effects of water-soluble cigarette smoke extracts upon the release of beta-hexosaminidase from RBL-2H3 basophilic leukaemia cells in response to substance P, compound 48/80, concanavalin A and antigen stimulation
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, 901 87 Umea, Sweden
    Inflamm Res 52:461-9. 2003
    ..To determine whether water-soluble constituents of cigarette smoke affect mast cell function using an in vitro model, RBL-2H3 basophilic leukaemia cells...
  28. ncbi Cellular transport of anandamide, 2-arachidonoylglycerol and palmitoylethanolamide--targets for drug development?
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Prostaglandins Leukot Essent Fatty Acids 66:193-200. 2002
    ..In addition, the possibility that these transport mechanisms can be targets for therapeutic strategies aimed at prolonging the effects of the endocannabinoids is discussed...
  29. ncbi The sulphydryl oxidizing reagent diamide affects phosphoinositide-mediated signal transduction: implications for the pathogenesis of Alzheimer's disease
    C J Fowler
    Department of Pharmacology, Umea University, Sweden
    Cell Signal 10:399-406. 1998
    ..It is suggested that oxidative stress may contribute to the disturbances in the phosphoinositide transduction pathway that are found in Alzheimer's disease...
  30. ncbi Comparison of the effects of hydrogen peroxide, 4-hydroxy-2-nonenal and beta-amyloid (25-35) upon calcium signalling
    C J Fowler
    Department of Pharmacology, Umea University, Sweden
    Neurochem Int 33:161-72. 1998
    ..The qualitative differences in the calcium responses of these two agents can be explained (a) by an additional effect of Abeta(25-35) upon calcium entry and (b) by differences in their effects upon the Ins(1,4,5)P3 receptor...
  31. ncbi Serotonin-stimulated calcium responses in human platelets: assay buffer dependency
    C J Fowler
    Department of Pharmacology, Umea University, Sweden
    Cell Signal 10:561-8. 1998
    ..For the response to thrombin, the response intensity is affected by the pH of the buffer used but is not sensitive to the buffer composition...
  32. ncbi Inhibition of anandamide hydrolysis by the enantiomers of ibuprofen, ketorolac, and flurbiprofen
    C J Fowler
    Department of Pharmacology, Umea University, Sweden
    Arch Biochem Biophys 362:191-6. 1999
    ..The enantiomers of flurbiprofen and R-ketorolac are the most potent NSAID inhibitors of fatty acid amide hydrolase yet reported...
  33. ncbi Evidence for cooperative binding of (-)Isoproterenol to rat brain beta1-adrenergic receptors
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, SE 901 87, Sweden
    Biochem Biophys Res Commun 257:629-34. 1999
    ..These results suggest that cooperative interactions reported for cardiac muscarinic receptors may also occur for beta1-adrenergic receptors in the rat brain...
  34. ncbi Serotonin stimulation of calcium mobilisation in human platelets: choice of units of measurement, effects of age and tobacco use, and correlation with serotonin2A receptor density
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Clin Chim Acta 287:1-18. 1999
    ..The measurement of Ca2+ responses to serotonin provides a useful such functional correlate...
  35. pmc Differences in the pharmacological properties of rat and chicken brain fatty acid amidohydrolase
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Br J Pharmacol 131:498-504. 2000
    ..Chicken FAAH was less sensitive to indomethacin than its rodent counterpart, but the inhibition was also competitive (K(i)). It is concluded that chicken FAAH activity has different pharmacological properties to its rodent counterpart...
  36. ncbi Pharmacological properties of cannabinoid receptors in the avian brain: similarity of rat and chicken cannabinoid1 receptor recognition sites and expression of cannabinoid2 receptor-like immunoreactivity in the embryonic chick brain
    C J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Pharmacol Toxicol 88:213-22. 2001
    ..However, a "classical" cannabinoid2-receptor component of [3H]WIN 55212-2 binding (i.e. a fraction inhibited by low concentrations of the cannabinoid2-receptor-selective antagonist SR 144528) was not found...
  37. ncbi Plant-derived, synthetic and endogenous cannabinoids as neuroprotective agents. Non-psychoactive cannabinoids, 'entourage' compounds and inhibitors of N-acyl ethanolamine breakdown as therapeutic strategies to avoid pyschotropic effects
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87, Umea, Sweden
    Brain Res Brain Res Rev 41:26-43. 2003
    ....
  38. ncbi The role of the phosphoinositide signalling system in the pathogenesis of sporadic Alzheimer's disease: a hypothesis
    C J Fowler
    Department of Pharmacology, University of Umea, Sweden
    Brain Res Brain Res Rev 25:373-80. 1997
    ....
  39. ncbi Calibration of Fura-2 signals introduces errors into measurement of thrombin-stimulated calcium mobilisation in human platelets
    C J Fowler
    Department of Pharmacology, Umea University, Sweden
    Clin Chim Acta 265:247-61. 1997
    ..Consistent with this, addition of bovine serum albumin to the assay medium has no significant effect on the fluorescence ratio response to thrombin, but greatly increases the observed calibrated calcium signal...
  40. ncbi Inhibition of C6 glioma cell proliferation by anandamide, 1-arachidonoylglycerol, and by a water soluble phosphate ester of anandamide: variability in response and involvement of arachidonic acid
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 90187 Umea, Sweden
    Biochem Pharmacol 66:757-67. 2003
    ....
  41. ncbi Inhibition of fatty acid amidohydrolase, the enzyme responsible for the metabolism of the endocannabinoid anandamide, by analogues of arachidonoyl-serotonin
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    J Enzyme Inhib Med Chem 18:225-31. 2003
    ..The linolenamide derivative was also found to be a mixed-type inhibitor. It is concluded that the 5-hydroxy group of arachidonoyl-serotonin contributes to, but is not essential for, inhibitory potency at fatty acid amidohydrolase...
  42. ncbi Inhibition of fatty acid amide hydrolase, a key endocannabinoid metabolizing enzyme, by analogues of ibuprofen and indomethacin
    Sandra Holt
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Eur J Pharmacol 565:26-36. 2007
    ....
  43. ncbi The cannabinoid agonist WIN 55,212-2 inhibits TNF-alpha-induced neutrophil transmigration across ECV304 cells
    Olov Nilsson
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87, Sweden
    Eur J Pharmacol 547:165-73. 2006
    ....
  44. ncbi AM404 and VDM 11 non-specifically inhibit C6 glioma cell proliferation at concentrations used to block the cellular accumulation of the endocannabinoid anandamide
    Kent Olov Jonsson
    Department of Pharmacology and Clinical Neuroscience, Umea University, 901 87, Umea, Sweden
    Arch Toxicol 77:201-7. 2003
    ....
  45. ncbi Acyl-based anandamide uptake inhibitors cause rapid toxicity to C6 glioma cells at pharmacologically relevant concentrations
    Eva de Lago
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    J Neurochem 99:677-88. 2006
    ..Such effects should be kept in mind when acyl-derived compounds are used to probe the function of the endocannabinoid system in the CNS, particularly in chronic administration protocols...
  46. doi A high cannabinoid CB(1) receptor immunoreactivity is associated with disease severity and outcome in prostate cancer
    Sui Chu Chung
    Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umea University, Umea, Sweden
    Eur J Cancer 45:174-82. 2009
    ..It is concluded that a high tumour CB(1)IR score is associated with prostate cancer severity and outcome...
  47. pmc Inhibitors of fatty acid amide hydrolase reduce carrageenan-induced hind paw inflammation in pentobarbital-treated mice: comparison with indomethacin and possible involvement of cannabinoid receptors
    Sandra Holt
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Br J Pharmacol 146:467-76. 2005
    ..In conclusion, the results show that in mice, treatment with indomethacin and URB597 produce SR144528-sensitive anti-inflammatory effects in the carrageenan model of acute inflammation...
  48. ncbi Influence of the degree of unsaturation of the acyl side chain upon the interaction of analogues of 1-arachidonoylglycerol with monoacylglycerol lipase and fatty acid amide hydrolase
    Severine Vandevoorde
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Biochem Biophys Res Commun 337:104-9. 2005
    ..It is concluded that increasing the number of unsaturated bonds on the acyl side chain of 1-AG from 1 to 5 has little effect on the affinity of acylglycerols for cytosolic MAGL...
  49. ncbi Anandamide metabolism by fatty acid amide hydrolase in intact C6 glioma cells. Increased sensitivity to inhibition by ibuprofen and flurbiprofen upon reduction of extra- but not intracellular pH
    Sandra Holt
    Department of Pharmacology and Clinical Neuroscience, Umea University, 901 87 Umea, Sweden
    Naunyn Schmiedebergs Arch Pharmacol 367:237-44. 2003
    ..It is concluded that a reduction of extracellular pH produces an enhanced accumulation of the acidic NSAIDs ibuprofen and flurbiprofen into C6 glioma cells and thereby an inhibition of anandamide metabolism...
  50. doi Effect of nitric oxide donors on membrane tritium accumulation of endocannabinoids and related endogenous lipids
    Lina Thors
    Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    Eur J Pharmacol 621:10-8. 2009
    ..These data raise the possibility that the cellular processing of endocannabinoids following its uptake can be regulated by nitric oxide...
  51. ncbi Cannabinoid CB1 receptor activation does not prevent the toxicity of glutamate towards embryonic chick telencephalon primary cultures
    Olov Nilsson
    Department of Pharmacology and Clinical Neuroscience, Umea University, Building 6B, Umea SE 901 87, Sweden
    Comp Biochem Physiol C Toxicol Pharmacol 136:245-51. 2003
    ..It is concluded that embryonic chick neurons in primary serum-free culture are not a useful model for the study of neuroprotective effects mediated by CB1 receptors in vitro...
  52. ncbi The cannabinoid CB2 receptor selective agonist JWH133 reduces mast cell oedema in response to compound 48/80 in vivo but not the release of beta-hexosaminidase from skin slices in vitro
    Kent Olov Jonsson
    Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
    Life Sci 78:598-606. 2006
    ..It is concluded that the ability of JWH133 to affect mast cell dependent inflammation in vivo may be mediated by an indirect action upon the mast cells...
  53. ncbi The potency of the fatty acid amide hydrolase inhibitor URB597 is dependent upon the assay pH
    Ben Paylor
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Pharmacol Res 54:481-5. 2006
    ..07 and 6.45+/-0.07 at extracellular pH values of 6 and 8, respectively. Since tissue pH is affected by inflammation, these data would suggest that the pH selectivity of the inhibition can contribute to the potency of the compound in vivo...
  54. pmc Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerol
    Nazdar Ghafouri
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Br J Pharmacol 143:774-84. 2004
    ..v. It is concluded that compounds like alpha-Methyl-1-AG, O-2203 and O-2204 may be useful as leads for the discovery of selective MAGL inhibitors that lack direct effects upon cannabinoid receptors...
  55. pmc Inhibition of fatty acid amide hydrolase and monoacylglycerol lipase by the anandamide uptake inhibitor VDM11: evidence that VDM11 acts as an FAAH substrate
    Severine Vandevoorde
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Br J Pharmacol 145:885-93. 2005
    ..It is concluded that VDM11 is an inhibitor of FAAH under the assay conditions used here, and that the inhibition may at least in part be a consequence of the compound acting as an alternative substrate...
  56. ncbi Lipopolysaccharide-induced pulmonary inflammation is not accompanied by a release of anandamide into the lavage fluid or a down-regulation of the activity of fatty acid amide hydrolase
    Sandra Holt
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
    Life Sci 76:461-72. 2004
    ..p. of this compound, which produced a complete inhibition of brain anandamide metabolism, only partially inhibited the lung metabolic activity...
  57. ncbi Measurement of saturable and non-saturable components of anandamide uptake into P19 embryonic carcinoma cells in the presence of fatty acid-free bovine serum albumin
    Anna Sandberg
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Chem Phys Lipids 134:131-9. 2005
    ....
  58. ncbi A novel assay for monoacylglycerol hydrolysis suitable for high-throughput screening
    Johan Brengdahl
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Anal Biochem 359:40-4. 2006
    ..The assay could also be adapted to a 96-well plate format, using C6 cells as the source of hydrolytic activity. Thus the assay is simple and appropriate for high-throughput screening of inhibitors of monoacylglycerol hydrolysis...
  59. doi Residual effects of focal brain ischaemia upon cannabinoid CB(1) receptor density and functionality in female rats
    Maria Luisa Rojo
    Department of Pharmacology and Clinical Neuroscience, Medicine, Umea University, SE 901 87 Umea, Sweden
    Brain Res 1373:195-201. 2011
    ..Our results reveal that although there are modest long-term decreases in ipsilateral CB(1) receptor densities following MCAO in female rats, these decreases do not result in a functional CB(1) receptor deficit...
  60. ncbi The endocannabinoid system: current pharmacological research and therapeutic possibilities
    Kent Olov Jonsson
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Basic Clin Pharmacol Toxicol 98:124-34. 2006
    ....
  61. doi Inhibition of fatty acid amide hydrolase and cyclooxygenase by the N-(3-methylpyridin-2-yl)amide derivatives of flurbiprofen and naproxen
    Mariateresa Cipriano
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Eur J Pharmacol 720:383-90. 2013
    ....
  62. ncbi Reversible, temperature-dependent, and AM404-inhibitable adsorption of anandamide to cell culture wells as a confounding factor in release experiments
    Marie Karlsson
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
    Eur J Pharm Sci 22:181-9. 2004
    ..It is concluded that the reversible adsorption of AEA by cell culture wells can be a confounding factor in release experiments...
  63. ncbi A simple stopped assay for fatty acid amide hydrolase avoiding the use of a chloroform extraction phase
    Linda Boldrup
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
    J Biochem Biophys Methods 60:171-7. 2004
    ..It is concluded that the acidic charcoal extraction method provides a robust and simple stopped assay for FAAH without the need to use potentially hazardous solvents like chloroform...
  64. doi Lysophosphatidylinositol stimulates [³⁵S]GTPγS binding in the rat prefrontal cortex and hippocampus
    Maria Luisa Rojo
    Department of Pharmacology and Clinical Neuroscience, Umea University, 901 87 Umea, Sweden
    Neurochem Res 37:1037-42. 2012
    ....
  65. doi NSAIDs: eNdocannabinoid stimulating anti-inflammatory drugs?
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Trends Pharmacol Sci 33:468-73. 2012
    ..In this Opinion article, our current understanding of the involvement of the endocannabinoid system in the actions of NSAIDs is described, and the ways in which this can lead to novel drug development is discussed...
  66. pmc Increased expression of cannabinoid CB₁ receptors in Achilles tendinosis
    Emmelie Björklund
    Pharmacology Unit, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
    PLoS ONE 6:e24731. 2011
    ..Here we investigate the expression of the cannabinoid receptor 1 (CB₁) in human Achilles tendons from healthy volunteers and from patients with Achilles tendinosis...
  67. ncbi Pharmacological properties and therapeutic possibilities for drugs acting upon endocannabinoid receptors
    Christopher J Fowler
    Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
    Curr Drug Targets CNS Neurol Disord 4:685-96. 2005
    ..An important aspect of these compounds is their efficacy and selectivity, and this is discussed in detail in the present review...
  68. pmc 'Entourage' effects of N-acyl ethanolamines at human vanilloid receptors. Comparison of effects upon anandamide-induced vanilloid receptor activation and upon anandamide metabolism
    Darren Smart
    Neuroscience Research, Glaxo SmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Br J Pharmacol 136:452-8. 2002
    ..It is possible that they may play an important role under conditions where their synthesis is increased, such as in severe inflammation...
  69. ncbi Design, synthesis and biological evaluation of new endocannabinoid transporter inhibitors
    María L Lopez-Rodriguez
    Departamento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense, 28040, Madrid, Spain
    Eur J Med Chem 38:403-12. 2003
    ..In vivo it enhances the analgesia and hypokinetic effects induced by a subeffective dose of anandamide...
  70. ncbi Esters, retroesters, and a retroamide of palmitic acid: pool for the first selective inhibitors of N-palmitoylethanolamine-selective acid amidase
    Severine Vandevoorde
    Unite de Chimie pharmaceutique et de Radiopharmacie, Universite Catholique de Louvain, Avenue Mounier, 73, UCL CMFA 73 40, B 1200 Brussels, Belgium
    J Med Chem 46:4373-6. 2003
    ..0, 70.5, and 76.7% inhibition at 100 microM, respectively) with much lower inhibitory effect on either fatty acid amide hydrolase or the uptake of anandamide...
  71. ncbi The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications
    Didier M Lambert
    Unite de Chimie pharmaceutique et de Radiopharmacie, Universite Catholique de Louvain, 73 Avenue Mounier, UCL CMFA 73 40, B 1200 Brussels, Belgium
    J Med Chem 48:5059-87. 2005
  72. ncbi Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase
    María L Lopez-Rodriguez
    Departamento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense, E 28040 Madrid, Spain
    J Med Chem 46:1512-22. 2003
    ..8 and 30 microM, respectively), will provide useful tools for the elucidation of the role of the anandamide transporter system in vivo...
  73. ncbi Modifications of the ethanolamine head in N-palmitoylethanolamine: synthesis and evaluation of new agents interfering with the metabolism of anandamide
    Severine Vandevoorde
    Unite de Chimie pharmaceutique et de Radiopharmacie, Universite Catholique de Louvain, Avenue Mounier, 73, UCL CMFA 73 40, B 1200 Brussels, Belgium
    J Med Chem 46:1440-8. 2003
    ....
  74. ncbi Inflammation and inflammatory agents activate protein kinase C epsilon translocation and excite guinea-pig submucosal neurons
    Daniel P Poole
    Department of Anatomy and Cell Biology, Centre for Neuroscience, University of Melbourne, Parkville, Victoria, Australia
    Gastroenterology 133:1229-39. 2007
    ....
  75. ncbi The palmitoylethanolamide family: a new class of anti-inflammatory agents?
    Didier M Lambert
    Unite de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Facult de M decine, Universit catholique de Louvain, UCL CMFA 73 40, 73, Avenue Emmanuel Mounier, Brussels, B 1200, Belgium
    Curr Med Chem 9:663-74. 2002
    ..However, its precise mechanism of action remains debated. In the present review, the biochemical and pharmacological properties of PEA are discussed, in particular with respect to its analgesic and anti-inflammatory properties...
  76. ncbi N-Morpholino- and N-diethyl-analogues of palmitoylethanolamide increase the sensitivity of transfected human vanilloid receptors to activation by anandamide without affecting fatty acid amidohydrolase activity
    Severine Vandevoorde
    Unite de Chimie pharmaceutique et de Radiopharmacie, Universite Catholique de Louvain, Avenue Mounier, 73, UCL CMFA 73 40, B 1200 Brussels, Belgium
    Bioorg Med Chem 11:817-25. 2003
    ..It is concluded that 19 and 20 selectively enhance AEA effects upon VR1 receptors without potentially confounding effects upon CB receptors or fatty acid amidohydrolase activity...
  77. ncbi Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase
    Jose Antonio Cisneros
    Departamento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense, E 28040 Madrid, Spain
    J Med Chem 50:5012-23. 2007
    ..These compounds will be useful in delineating the importance of the cytosolic hydrolytic activity in the regulation of 2-AG levels and, hence, its potential as a target for drug development...
  78. ncbi Regulation of the slow afterhyperpolarization in enteric neurons by protein kinase A
    Craig B Neylon
    Department of Anatomy and Cell Biology, University of Melbourne, Parkville 3010, Australia
    Auton Neurosci 126:258-63. 2006
    ..The regulation of the channel through kinases and phophatases results in exquisite control of neuronal firing and subsequent modulation of enteric reflexes...
  79. ncbi Effects of compounds that influence IK (KCNN4) channels on afterhyperpolarizing potentials, and determination of IK channel sequence, in guinea pig enteric neurons
    Trung V Nguyen
    Department of Anatomy and Cell Biology, University of Melbourne, Parkville, VIC 3010, Australia
    J Neurophysiol 97:2024-31. 2007
    ..It is concluded that the channels that carry the current of the late afterhyperpolarizing potential in guinea pig enteric neurons are I(K) channels...
  80. ncbi Metal complexes of porphycene, corrphycene, and hemiporphycene: stability and coordination chemistry
    Christopher J Fowler
    Department of Chemistry and Biochemistry The University of Texas at Austin, Austin, TX 78712 USA
    Chemistry 8:3485-96. 2002
    ..These solid-state structures confirm four-coordinate species for the Ni(II) complexes, four- and five-coordinate species for the Mg(II) and Zn(II) complexes, and a six-coordinate species for the lone Co(II) complex...