scholarly journals Cover Picture: Structure-Property Relationships of a Class of Carbamate-Based Fatty Acid Amide Hydrolase (FAAH) Inhibitors: Chemical and Biological Stability / A Second Generation of Carbamate-Based Fatty Acid Amide Hydrolase Inhibitors with Improved Activity in vivo (ChemMedChem 9/2009)

ChemMedChem ◽  
2009 ◽  
Vol 4 (9) ◽  
pp. 1385-1385
Author(s):  
Federica Vacondio ◽  
Claudia Silva ◽  
Alessio Lodola ◽  
Alessandro Fioni ◽  
Silvia Rivara ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Biological Stability ◽  
Structure Property ◽  
Structure Property Relationships ◽  
Amide Hydrolase ◽  
Faah Inhibitors ◽  
Fatty Acid Amide

scholarly journals A Second Generation of Carbamate-Based Fatty Acid Amide Hydrolase Inhibitors with Improved Activity in vivo

ChemMedChem ◽  
2009 ◽  
Vol 4 (9) ◽  
pp. 1505-1513 ◽  
Author(s):  
Jason R. Clapper ◽  
Federica Vacondio ◽  
Alvin R. King ◽  
Andrea Duranti ◽  
Andrea Tontini ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Second Generation ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Chemistry around imidazopyrazine and ibuprofen: Discovery of novel fatty acid amide hydrolase (FAAH) inhibitors

2010 ◽  
Vol 45 (9) ◽  
pp. 3564-3574 ◽  
Author(s):  
Frédéric De Wael ◽  
Giulio G. Muccioli ◽  
Didier M. Lambert ◽  
Thérèse Sergent ◽  
Yves-Jacques Schneider ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Faah Inhibitors ◽  
Fatty Acid Amide

Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors

2013 ◽  
Vol 21 (1) ◽  
pp. 28-41 ◽  
Author(s):  
Mitsunori Kono ◽  
Takahiro Matsumoto ◽  
Toru Kawamura ◽  
Atsushi Nishimura ◽  
Yoshihiro Kiyota ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Biological Evaluation ◽  
Amide Hydrolase ◽  
Faah Inhibitors ◽  
Sar Study ◽  
Fatty Acid Amide

scholarly journals O-(Triazolyl)methyl Carbamates as a Novel and Potent Class of Fatty Acid Amide Hydrolase (FAAH) Inhibitors

ChemMedChem ◽  
2014 ◽  
Vol 10 (2) ◽  
pp. 380-395 ◽  
Author(s):  
Giampiero Colombano ◽  
Clara Albani ◽  
Giuliana Ottonello ◽  
Alison Ribeiro ◽  
Rita Scarpelli ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Amide Hydrolase ◽  
Faah Inhibitors ◽  
Fatty Acid Amide

scholarly journals Blocking of Fatty Acid Amide Hydrolase Activity with PF-04457845 in Human Brain: A Positron Emission Tomography Study with the Novel Radioligand [11C]CURB

2015 ◽  
Vol 35 (11) ◽  
pp. 1827-1835 ◽  
Author(s):  
Isabelle Boileau ◽  
Pablo M Rusjan ◽  
Belinda Williams ◽  
Esmaeil Mansouri ◽  
Romina Mizrahi ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Fatty Acid ◽  
Human Brain ◽  
Fatty Acid Amide Hydrolase ◽  
Acid Amide ◽  
Emission Tomography ◽  
Positron Emission ◽  
Amide Hydrolase ◽  
Fatty Acid Amide

Positron emission tomography with [11C]CURB was recently developed to quantify fatty acid amide hydrolase (FAAH), the enzyme responsible for hydrolyzing the endocannabinoid anandamide. This study investigated the test–retest reliability of [11C]CURB as well as its in vivo specificity and the validity of the kinetic model by using the highly specific FAAH inhibitor, PF-04457845. Five healthy volunteers completed test–retest [11C]CURB scans 1 to 2 months apart and six subjects completed baseline and blocking scans on the same day after PF-04457845 (p.o.) administration (1, 4, or 20 mg; n = 2 each). The composite parameter γ k3 (an index of FAAH activity, γ = K1/ k2) was estimated using an irreversible two-tissue compartment model with plasma input function. There were no clinically observable responses to oral PF-04457845 or [11C]CURB injection. Oral administration of PF-04457845 reduced [11C]CURB binding to a homogeneous level at all three doses, with γ k3 values decreased by ≥91%. Excellent reproducibility and good reliability (test–retest variability = 9%; intraclass correlation coefficient = 0.79) were observed across all regions of interest investigated. Our findings suggest that γ k3/[11C]CURB is a reliable, highly sensitive, and selective tool to measure FAAH activity in human brain in vivo. Moreover, PF-04457845 is a highly potent FAAH inhibitor (>95% inhibition at 1 mg) in living human brain.

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