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| Christopher J FowlerSummaryCountry: Sweden Publications
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Acidic nonsteroidal anti-inflammatory drugs inhibit rat brain fatty acid amide hydrolase in a pH-dependent mannerChristopher 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...
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...
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...
Calibration of Fura-2 signals introduces errors into measurement of thrombin-stimulated calcium mobilisation in human plateletsC 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...
"The tools of the trade"--an overview of the pharmacology of the endocannabinoid systemChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
Curr Pharm Des 14:2254-65. 2008....
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...
The pharmacology of the cannabinoid system--a question of efficacy and selectivityChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, SE 90187, Umea, Sweden
Mol Neurobiol 36:15-25. 2007....
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 acidChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, SE 90187 Umea, Sweden
Biochem Pharmacol 66:757-67. 2003....
Inhibition of fatty acid amidohydrolase, the enzyme responsible for the metabolism of the endocannabinoid anandamide, by analogues of arachidonoyl-serotoninChristopher 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...
The contribution of cyclooxygenase-2 to endocannabinoid metabolism and actionC J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
Br J Pharmacol 152:594-601. 2007....
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 stimulationC 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...
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...
Possible involvement of the endocannabinoid system in the actions of three clinically used drugsChristopher 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...
Selective inhibition of anandamide cellular uptake versus enzymatic hydrolysis--a difficult issue to handleChristopher 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...
The cannabinoid system and its pharmacological manipulation--a review, with emphasis upon the uptake and hydrolysis of anandamideChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, SE901 87 Umea, Sweden
Fundam Clin Pharmacol 20:549-62. 2006....
The endocannabinoid signaling system: pharmacological and therapeutic aspectsChristopher 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...
The case for the development of novel analgesic agents targeting both fatty acid amide hydrolase and either cyclooxygenase or TRPV1C 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...
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....
The role of the phosphoinositide signalling system in the pathogenesis of sporadic Alzheimer's disease: a hypothesisC J Fowler
Department of Pharmacology, University of Umea, Sweden
Brain Res Brain Res Rev 25:373-80. 1997....
The sulphydryl oxidizing reagent diamide affects phosphoinositide-mediated signal transduction: implications for the pathogenesis of Alzheimer's diseaseC 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...
Comparison of the effects of hydrogen peroxide, 4-hydroxy-2-nonenal and beta-amyloid (25-35) upon calcium signallingC 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...
Serotonin-stimulated calcium responses in human platelets: assay buffer dependencyC 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...
Inhibition of anandamide hydrolysis by the enantiomers of ibuprofen, ketorolac, and flurbiprofenC 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...
Evidence for cooperative binding of (-)Isoproterenol to rat brain beta1-adrenergic receptorsC 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...
Serotonin stimulation of calcium mobilisation in human platelets: choice of units of measurement, effects of age and tobacco use, and correlation with serotonin2A receptor densityC 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...
Differences in the pharmacological properties of rat and chicken brain fatty acid amidohydrolaseC 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...
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 effectsChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87, Umea, Sweden
Brain Res Brain Res Rev 41:26-43. 2003....
Targeting the endocannabinoid system for the treatment of cancer--a practical viewChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
Curr Top Med Chem 10:814-27. 2010....
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 vitroChristopher 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...
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...
Fatty acid amide hydrolase: biochemistry, pharmacology, and therapeutic possibilities for an enzyme hydrolyzing anandamide, 2-arachidonoylglycerol, palmitoylethanolamide, and oleamideC J Fowler
Department of Pharmacology and Clinical Neuroscience, Umea University, Sweden
Biochem Pharmacol 62:517-26. 2001....
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 brainC 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...
Inhibition of fatty acid amide hydrolase, a key endocannabinoid metabolizing enzyme, by analogues of ibuprofen and indomethacinSandra Holt
Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87 Umea, Sweden
Eur J Pharmacol 565:26-36. 2007....
AM404 and VDM 11 non-specifically inhibit C6 glioma cell proliferation at concentrations used to block the cellular accumulation of the endocannabinoid anandamideKent Olov Jonsson
Department of Pharmacology and Clinical Neuroscience, Umea University, 901 87, Umea, Sweden
Arch Toxicol 77:201-7. 2003....
The cannabinoid agonist WIN 55,212-2 inhibits TNF-alpha-induced neutrophil transmigration across ECV304 cellsOlov Nilsson
Department of Pharmacology and Clinical Neuroscience, Umea University, SE 901 87, Sweden
Eur J Pharmacol 547:165-73. 2006....
Acyl-based anandamide uptake inhibitors cause rapid toxicity to C6 glioma cells at pharmacologically relevant concentrationsEva de Lago
Department of Pharmacology and Clinical Neuroscience, , Ume, 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...
Inhibitors of fatty acid amide hydrolase reduce carrageenan-induced hind paw inflammation in pentobarbital-treated mice: comparison with indomethacin and possible involvement of cannabinoid receptorsSandra 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...
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 pHSandra 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...
Fatty acid amide hydrolase in prostate cancer: association with disease severity and outcome, CB1 receptor expression and regulation by IL-4Lina Thors
Pharmacology Unit, Department of Pharmacology and Clinical Neuroscience, Umea University, Umea, Sweden
PLoS ONE 5:e12275. 2010....
Cannabinoid CB1 receptor activation does not prevent the toxicity of glutamate towards embryonic chick telencephalon primary culturesOlov 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...
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 vitroKent 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...
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 hydrolaseSeverine 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...
Effect of nitric oxide donors on membrane tritium accumulation of endocannabinoids and related endogenous lipidsLina 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...
The potency of the fatty acid amide hydrolase inhibitor URB597 is dependent upon the assay pHBen Paylor
Department of Pharmacology and Clinical Neuroscience, , SE-901 87 Ume, 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...
Phospho-Akt immunoreactivity in prostate cancer: relationship to disease severity and outcome, Ki67 and phosphorylated EGFR expressionPeter Hammarsten
Department of Medical Biosciences, Pathology, Umea University, Umea, Sweden
PLoS ONE 7:e47994. 2012....
Inhibition of fatty acid amide hydrolase and monoacylglycerol lipase by the anandamide uptake inhibitor VDM11: evidence that VDM11 acts as an FAAH substrateSeverine 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...
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 hydrolaseSandra 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...
Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerolNazdar Ghafouri
Department of Pharmacology and Clinical Neuroscience, , SE-901 87 Ume, 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...
Residual effects of focal brain ischaemia upon cannabinoid CB(1) receptor density and functionality in female ratsMaria 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...
A novel assay for monoacylglycerol hydrolysis suitable for high-throughput screeningJohan Brengdahl
Department of Pharmacology and Clinical Neuroscience, , SE-901 87 Ume, 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...
Tumour Cannabinoid CB(1) receptor and phosphorylated epidermal growth factor receptor expression are additive prognostic markers for prostate cancerChristopher J Fowler
Department of Pharmacology and Clinical Neuroscience, Pharmacology, Umea University, Umea, Sweden
PLoS ONE 5:e15205. 2010....
The endocannabinoid system: current pharmacological research and therapeutic possibilitiesKent-Olov Jonsson
Department of Pharmacology and Clinical Neuroscience, , SE-901 87 Ume, Sweden
Basic Clin Pharmacol Toxicol 98:124-34. 2006....
High tumour cannabinoid CB1 receptor immunoreactivity negatively impacts disease-specific survival in stage II microsatellite stable colorectal cancerSofia 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...
Lysophosphatidylinositol stimulates [³⁵S]GTPγS binding in the rat prefrontal cortex and hippocampusMaria Luisa Rojo
Department of Pharmacology and Clinical Neuroscience, Umea University, 901 87 Umea, Sweden
Neurochem Res 37:1037-42. 2012....
A high cannabinoid CB(1) receptor immunoreactivity is associated with disease severity and outcome in prostate cancerSui 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...
Measurement of saturable and non-saturable components of anandamide uptake into P19 embryonic carcinoma cells in the presence of fatty acid-free bovine serum albuminAnna Sandberg
Department of Pharmacology and Clinical Neuroscience, , SE-901 87 Ume, Sweden
Chem Phys Lipids 134:131-9. 2005....
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...
A simple stopped assay for fatty acid amide hydrolase avoiding the use of a chloroform extraction phaseLinda Boldrup
Department of Pharmacology and Clinical Neuroscience, , SE901 87 Ume, 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...
Reversible, temperature-dependent, and AM404-inhibitable adsorption of anandamide to cell culture wells as a confounding factor in release experimentsMarie Karlsson
Department of Pharmacology and Clinical Neuroscience, , 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...
Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamideChristopher 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...
Pharmacological properties and therapeutic possibilities for drugs acting upon endocannabinoid receptorsChristopher 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...
Increased expression of cannabinoid CB₁ receptors in Achilles tendinosisEmmelie 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...
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...
'Entourage' effects of N-acyl ethanolamines at human vanilloid receptors. Comparison of effects upon anandamide-induced vanilloid receptor activation and upon anandamide metabolismDarren 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...
The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applicationsDidier M Lambert
, , 73 Avenue Mounier, UCL-CMFA 73.40, B-1200 Brussels, Belgium
J Med Chem 48:5059-87. 2005
Design, synthesis and biological evaluation of new endocannabinoid transporter inhibitorsMaría 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...
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 activitySeverine 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...
Esters, retroesters, and a retroamide of palmitic acid: pool for the first selective inhibitors of N-palmitoylethanolamine-selective acid amidaseSeverine 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...
Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolaseJose 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...
Modifications of the ethanolamine head in N-palmitoylethanolamine: synthesis and evaluation of new agents interfering with the metabolism of anandamideSeverine 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....
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolaseMaría 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...
Inflammation and inflammatory agents activate protein kinase C epsilon translocation and excite guinea-pig submucosal neuronsDaniel P Poole
Department of Anatomy and Cell Biology, Centre for Neuroscience, University of Melbourne, Parkville, Victoria, Australia
Gastroenterology 133:1229-39. 2007....
Regulation of the slow afterhyperpolarization in enteric neurons by protein kinase ACraig 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...
Metal complexes of porphycene, corrphycene, and hemiporphycene: stability and coordination chemistryChristopher 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...
Effects of compounds that influence IK (KCNN4) channels on afterhyperpolarizing potentials, and determination of IK channel sequence, in guinea pig enteric neuronsTrung 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...
