Research Topics
| Susanna M SaarioSummaryAffiliation: University of Kuopio Country: Finland Publications
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Detail Information
Publications
URB754 has no effect on the hydrolysis or signaling capacity of 2-AG in the rat brainSusanna M Saario
Department of Pharmaceutical Chemistry, Department of Physiology, University of Kuopio, P O Box 1627, FIN 70211 Kuopio, Finland
Chem Biol 13:811-4. 2006..Thus, in our hands URB754 was not able to block the endocannabinoid-hydrolyzing enzymes and cannot serve as a lead structure for future development of MGL-specific inhibitors...- Therapeutic potential of endocannabinoid-hydrolysing enzyme inhibitorsSusanna M Saario
Department of Pharmaceutical Chemistry, University of Kuopio, Kuopio, Finland
Basic Clin Pharmacol Toxicol 101:287-93. 2007..g. for the treatment of pain and movement disorders). This MiniReview summarizes the literature concerning the potential therapeutic potential of FAAH and MGL inhibitors... - Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranesSusanna M Saario
Department of Pharmaceutical Chemistry, University of Kuopio, P O Box 1627, FIN 70211 Kuopio, Finland
Biochem Pharmacol 67:1381-7. 2004..This enzyme assay provides a useful method for future inhibition studies of 2-AG degrading enzyme(s) in brain membrane preparation having considerably higher MGL-like activity when compared to FAAH activity... - Characterization of the sulfhydryl-sensitive site in the enzyme responsible for hydrolysis of 2-arachidonoyl-glycerol in rat cerebellar membranesSusanna M Saario
Department of Pharmaceutical Chemistry, P O Box 1627, FIN 70211 Kuopio, Finland
Chem Biol 12:649-56. 2005.... - Monoglyceride lipase as an enzyme hydrolyzing 2-arachidonoylglycerolSusanna M Saario
Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 1627, FI-70211 Kuopio
Chem Biodivers 4:1903-13. 2007 - Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid systemSusanna M Saario
Department of Pharmaceutical Chemistry, University of Kuopio, P O Box 1627, FIN 70211 Kuopio, Finland
J Med Chem 49:4650-6. 2006..2005, 48, 7166) were also tested in our FAAH assay, and four active compounds (7-10) were found with IC50 values between 0.52 and 22 microM. Additionally, compound 7 inhibited MGL-like enzymatic activity with an IC50 value of 31 microM... - Synthesis, cannabinoid receptor activity, and enzymatic stability of reversed amide derivatives of arachidonoyl ethanolamideTeija Parkkari
Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FIN 70211 Kuopio, Finland
Bioorg Med Chem 14:5252-8. 2006..Therefore, the reversed amide analogues of AEA may serve as enzymatically stable structural basis for the drug design based on the endogenous cannabinoids... - 3-Heterocycle-phenyl N-alkylcarbamates as FAAH inhibitors: design, synthesis and 3D-QSAR studiesHeikki Käsnänen
Department of Pharmaceutical Chemistry, University of Kuopio, P O Box 1627, 70211 Kuopio, Finland
ChemMedChem 5:213-31. 2010..732 and 0.760, respectively. These models could be of high value in further FAAH inhibitor design... - Alpha-methylated derivatives of 2-arachidonoyl glycerol: synthesis, CB1 receptor activity, and enzymatic stabilityTeija Parkkari
Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FIN 70211 Kuopio, Finland
Bioorg Med Chem Lett 16:2437-40. 2006..In addition, the results showed that the replacement of the hydroxyl group(s) of 2-AG by fluorine does not improve the CB1 activity of 2-AG... - The synthesis and biological evaluation of para-substituted phenolic N-alkyl carbamates as endocannabinoid hydrolyzing enzyme inhibitorsAnna Minkkilä
University of Kuopio, Department of Pharmaceutical Chemistry, Kuopio, Finland
Eur J Med Chem 44:2994-3008. 2009..0 microM), respectively. Compound 26 also inhibited both FAAH-dependent AEA uptake and AEA hydrolysis (IC(50); 0.082 microM) by intact RBL2H3 cells, and could also reduce 2-AG hydrolysis by these cells at concentrations >or=0.030 microM... - Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolaseAnna Minkkilä
Department of Pharmaceutical Chemistry, University of Kuopio, P O Box 1627, FI 70211 Kuopio, Finland
J Med Chem 51:7057-60. 2008..Eight of these compounds inhibited MGL with IC50 in the micromolar range. The most potent compound, phenylboronic acid with para-nonyl substituent (13), inhibited FAAH and MGL with IC50 of 0.0091 and 7.9 microM, respectively... - An optimized approach to study endocannabinoid signaling: evidence against constitutive activity of rat brain adenosine A1 and cannabinoid CB1 receptorsJuha R Savinainen
Department of Physiology, University of Kuopio, PO Box 1627, Kuopio FIN-70211, Finland
Br J Pharmacol 140:1451-9. 2003.... - 4-Phenylbutanoyl-2(S)-acylpyrrolidines and 4-phenylbutanoyl-L-prolyl-2(S)-acylpyrrolidines as prolyl oligopeptidase inhibitorsErik A A Wallen
Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FIN 70211 Kuopio, Finland
Bioorg Med Chem 10:2199-206. 2002..The acyl group in the two series of new compounds seems to bind to different sites of the enzyme, since the second series of new compounds did not show the same cyclopentanecarbonyl or benzoyl specificity as the first series... - Design, synthesis, and in vitro evaluation of carbamate derivatives of 2-benzoxazolyl- and 2-benzothiazolyl-(3-hydroxyphenyl)-methanones as novel fatty acid amide hydrolase inhibitorsMikko J Myllymäki
Laboratory of Organic Chemistry, Department of Chemical Technology, Helsinki University of Technology, Post Office Box 6100, Kemistintie 1, FIN 02015 TKK, Finland
J Med Chem 50:4236-42. 2007..All the active compounds belong to the structural family of carbamates. Compounds 14 and 18 were found to be the most potent FAAH inhibitors, which may serve as lead structures for novel FAAH inhibitors...