J. Savinainen

发表

Regulating membrane lipid levels at the synapse by small-molecule inhibitors of monoacylglycerol lipase: new developments in therapeutic and PET imaging applications.

N. Grimsey, B. Attili, J. Savinainen, 2020, Drug discovery today.

Brain regional cannabinoid CB(1) receptor signalling and alternative enzymatic pathways for 2-arachidonoylglycerol generation in brain sections of diacylglycerol lipase deficient mice.

J. Laitinen, M. Lehtonen, J. Savinainen, 2014, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL).

Guy Bormans, Sofie Celen, Alfons Verbruggen, 2017, European journal of medicinal chemistry.

Despite substantial degradation, 2‐arachidonoylglycerol is a potent full efficacy agonist mediating CB1 receptor‐dependent G‐protein activation in rat cerebellar membranes

J. Laitinen, T. Järvinen, J. Savinainen, 2001, British journal of pharmacology.

Mutation of Cys242 of Human Monoacylglycerol Lipase Disrupts Balanced Hydrolysis of 1-and 2-monoacylglycerols and Selectively Impairs Inhibitor Potency Running Title Page Running Title: Structural Determinants of Magl for Substrate Preference Introduction

A. Poso, T. Laitinen, J. Laitinen, 2022 .

Discovery of Triterpenoids as Reversible Inhibitors of α/β-hydrolase Domain Containing 12 (ABHD12)

T. Laitinen, J. Laitinen, S. Alakurtti, 2014, PloS one.

Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists.

A. Poso, J. Laitinen, T. Nevalainen, 2006, Journal of medicinal chemistry.

Visualization of 2‐arachidonoylglycerol accumulation and cannabinoid CB1 receptor activity in rat brain cryosections by functional autoradiography

J. Laitinen, M. Lehtonen, J. Savinainen, 2007, Journal of neurochemistry.

Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranes.

J. Laitinen, T. Järvinen, S. Saario, 2004, Biochemical pharmacology.

Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors.

J. Leppänen, A. Poso, T. Laitinen, 2013, Journal of medicinal chemistry.

Distinct Activity of Endocannabinoid-Hydrolyzing Enzymes MAGL and FAAH in Key Regions of Peripheral and Central Nervous System Implicated in Migraine

R. Giniatullin, J. Savinainen, Adriana Della Pietra, 2021, International journal of molecular sciences.

Synthesis, cannabinoid receptor activity, and enzymatic stability of reversed amide derivatives of arachidonoyl ethanolamide.

J. Laitinen, T. Nevalainen, T. Järvinen, 2006, Bioorganic & medicinal chemistry.

Metabolomics of Synovial Fluid and Infrapatellar Fat Pad in Patients with Osteoarthritis or Rheumatoid Arthritis

P. Nieminen, A. Mustonen, H. Kröger, 2022, Inflammation.

An optimized approach to study endocannabinoid signaling: evidence against constitutive activity of rat brain adenosine A1 and cannabinoid CB1 receptors

J. Laitinen, T. Järvinen, S. Saario, 2003, British journal of pharmacology.

New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.

S. Fogli, A. Malfitano, V. Di Marzo, 2015, European journal of medicinal chemistry.

Biochemical and Pharmacological Characterization of the Human Lymphocyte Antigen B-Associated Transcript 5 (BAT5/ABHD16A)

T. Laitinen, J. Laitinen, T. Nevalainen, 2014, PloS one.

Evaluation of FASN inhibitors by a versatile toolkit reveals differences in pharmacology between human and rodent FASN preparations and in antiproliferative efficacy in vitro vs. in situ in human cancer cells.

A. Poso, T. Laitinen, J. Laitinen, 2020, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections – Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils

M. Varjosalo, T. Wirth, J. Laitinen, 2020, Biological Procedures Online.

Tissue-ABPP enables high-resolution confocal fluorescence imaging of serine hydrolase activity in cryosections – Application to glioma brain unveils activity hotspots originating from tumor-associated neutrophils

M. Varjosalo, T. Wirth, J. Laitinen, 2019, bioRxiv.

Effects of Topical Anandamide-Transport Inhibitors, AM404 and Olvanil, on Intraocular Pressure in Normotensive Rabbits

K. Järvinen, J. Laitinen, T. Järvinen, 2001, Pharmaceutical Research.

Robust Hydrolysis of Prostaglandin Glycerol Esters by Human Monoacylglycerol Lipase (MAGL)

A. Poso, T. Laitinen, J. Laitinen, 2014, Molecular Pharmacology.

Synthesis and In Vitro Evaluation of Novel 2‐oxo‐1,2‐dihydroquinoline CB2 Receptor Inverse Agonists

T. Nevalainen, T. Järvinen, J. Vepsäläinen, 2006, Chemical biology & drug design.

The serine hydrolases MAGL, ABHD6 and ABHD12 as guardians of 2-arachidonoylglycerol signalling through cannabinoid receptors

J. Laitinen, S. Saario, J. Savinainen, 2012, Acta physiologica.

A Sensitive and Versatile Fluorescent Activity Assay for ABHD6.

J. Laitinen, J. Savinainen, Dina Navia-Paldanius, 2016, Methods in molecular biology.

A Sensitive and Versatile Fluorescent Activity Assay for ABHD12.

J. Laitinen, J. Savinainen, Dina Navia-Paldanius, 2016, Methods in molecular biology.

Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors.

T. Laitinen, J. Laitinen, T. Nevalainen, 2015, Bioorganic & medicinal chemistry.

Optimization of 1,2,5‐Thiadiazole Carbamates as Potent and Selective ABHD6 Inhibitors

F. Maxfield, T. Laitinen, R. Runyon, 2015, ChemMedChem.

Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescence-based technique.

J. Laitinen, T. Nevalainen, J. Savinainen, 2010, Analytical biochemistry.

Detection of Cannabinoid CB1, Adenosine A1, Muscarinic Acetylcholine, and GABAB Receptor-Dependent G Protein Activity in Transducin-Deactivated Membranes and Autoradiography Sections of Rat Retina

J. Laitinen, J. Savinainen, 2004, Cellular and Molecular Neurobiology.

Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid α/β-Hydrolase Domain 6 (ABHD6).

W. Vanduffel, G. Bormans, G. Cowin, 2022, Journal of medicinal chemistry.

Design, synthesis, and biological evaluation of 2,4‐dihydropyrano[2,3‐c]pyrazole derivatives as autotaxin inhibitors

J. Leppänen, A. Poso, T. Laitinen, 2017, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Screening of Various Hormone‐Sensitive Lipase Inhibitors as Endocannabinoid‐Hydrolyzing Enzyme Inhibitors

Henri Xhaard, Antti Poso, Jukka Leppänen, 2009, ChemMedChem.

Inhibiting Endocannabinoid Hydrolysis as Emerging Analgesic Strategy Targeting a Spectrum of Ion Channels Implicated in Migraine Pain

R. Giniatullin, J. Savinainen, Adriana Della Pietra, 2022, International journal of molecular sciences.

S-Nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific manner

T. Kokkola, J. Laitinen, Juha R Savinainen, 2005, BMC Cell Biology.

Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives.

J. Laitinen, T. Nevalainen, J. Gynther, 2004, Bioorganic & medicinal chemistry letters.

Chemoproteomic, biochemical and pharmacological approaches in the discovery of inhibitors targeting human α/β-hydrolase domain containing 11 (ABHD11).

T. Laitinen, J. Laitinen, T. Nevalainen, 2016, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands.

Ettore Novellino, Luciana Marinelli, Marco Macchia, 2015, European journal of medicinal chemistry.

Biochemical and pharmacological characterization of human α/β-hydrolase domain containing 6 (ABHD6) and 12 (ABHD12)[S]

J. Laitinen, J. Savinainen, Dina Navia-Paldanius, 2012, Journal of Lipid Research.

Increased tonic cannabinoid CB1R activity and brain region-specific desensitization of CB1R Gi/o signaling axis in mice with global genetic knockout of monoacylglycerol lipase.

U. Taschler, R. Zimmermann, J. Laitinen, 2015, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists.

A. Irving, A. Poso, T. Laitinen, 2016, European journal of medicinal chemistry.

In Vivo Characterization of the Ultrapotent Monoacylglycerol Lipase Inhibitor {4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl}(1H-1,2,4-triazol-1-yl)methanone (JJKK-048)

J. Laitinen, T. Nevalainen, M. Lehtonen, 2016, The Journal of Pharmacology and Experimental Therapeutics.

Loratadine analogues as MAGL inhibitors.

Tuomo Laitinen, T. Laitinen, J. Laitinen, 2015, Bioorganic & medicinal chemistry letters.

Alpha-methylated derivatives of 2-arachidonoyl glycerol: synthesis, CB1 receptor activity, and enzymatic stability.

J. Laitinen, T. Nevalainen, S. Saario, 2006, Bioorganic & medicinal chemistry letters.

Synthesis and CB1 receptor activities of dimethylheptyl derivatives of 2-arachidonoyl glycerol (2-AG) and 2-arachidonyl glyceryl ether (2-AGE).

A. Poso, J. Laitinen, T. Nevalainen, 2006, Bioorganic & medicinal chemistry.

Identification of WIN55212‐3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor

Antti Poso, Tomi Järvinen, A. Poso, 2005, British journal of pharmacology.

Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase.

A. Poso, T. Laitinen, J. Laitinen, 2013, Chemistry & biology.

α‐Methylated Derivatives of 2‐Arachidonoyl Glycerol: Synthesis, CB1 Receptor Activity, and Enzymatic Stability.

J. Laitinen, T. Nevalainen, S. Saario, 2006 .

Mutation of Cys 242 of Human Monoacylglycerol Lipase Disrupts Balanced Hydrolysis of 1-and 2-Monoacylglycerols and Selectively Impairs Inhibitor Potency s

A. Poso, T. Laitinen, J. Laitinen, 2014 .

A prolyl oligopeptidase inhibitor reduces tau pathology in cellular models and in mice with tauopathy

S. Haggarty, H. Huttunen, M. C. Silva, 2023, Science Translational Medicine.

1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor.

A. Malfitano, V. Di Marzo, A. Ligresti, 2014, European journal of medicinal chemistry.

High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections – Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils

M. Varjosalo, T. Wirth, J. Laitinen, 2020, Biological Procedures Online.

Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).

T. Laitinen, J. Laitinen, T. Nevalainen, 2014, Bioorganic & medicinal chemistry.

Discovery of 12-Thiazole Abietanes as Selective Inhibitors of the Human Metabolic Serine Hydrolase hABHD16A.

E. Kalso, J. Laitinen, J. Yli-Kauhaluoma, 2018, ACS Medicinal Chemistry Letters.

Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor.

Antti Poso, Tomi Järvinen, Maija Lahtela-Kakkonen, 2005, Journal of medicinal chemistry.