fatty acid amide hydrolase

Carprofen (Ridamyl) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic activities.

Biochanin A (4-Methylgenistein) is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor.

Dual FAAH sEH-IN-1 is a dual inhibitor of sEH (soluble epoxide hydrolase) (IC50: 9.6 nM) and FAAH (fatty acid amide hydrolase) (IC50: 7 nM) with high affinity and anti-inflammatory activity.

MK-4409 is a novel and selective inhibitor of oxazole fatty acid amide hydrolase FAAH.MK-4409 can be used to study inflammatory and neuropathic pain.

MM-433593 is a selective fatty acid amide hydrolase (FAAH-1) inhibitor for the treatment of pain, inflammation, and other disorders.

URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) inhibites three SHs (ABHD6, ABHD11, and FAAH)

FAAH inhibitor 1 (Benzothiazole analog 3) is a potent FAAH inhibitor with an IC50 of 18 nM.

JZP-430 is an effective, highly selective, irreversible inhibitor of α β-hydrolase domain 6 (ABHD6) (IC50: 44 nM). It also shows ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

JNJ-1661010 (Takeda-25) is an effective and specific FAAH inhibitor (IC50: 10 12 nM for rat human), shows >100-fold selectivity for FAAH-1 than FAAH-2.

BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.

4-Nonylphenylboronic acid is a inhibitor of FAAH.

WWL 154 is an serine hydrolase (SH) and fatty acid amide hydrolase FAAH-4 inhibitor.

LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). LY2183240 is a novel and highly effective blocker of anandamide uptake (IC50 = 270 pM).

CB2R FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

N-(3-Methoxybenzyl)Palmitamide is a promising FAAH inhibitor for the treatment of pain, inflammation, and CNS degenerative disorders.

Oleoyl proline is an N-acyl amine that can be detected in bovine brain extracts and D. melanogaster larvae using mass spectrometry. In a preclinical model of pain, mice lacking fatty acid amide hydrolase (FAAH KO) had decreased N-oleoyl proline levels in

N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide binds to the cannabinoid 1 (CB1) receptor with a Ki value of 365 nM in a radioligand binding assay using rat brain homogenate. It has an EC50 value of 698 nM for the peroxisome proliferator-activated receptor α (PPARα) in a luciferase reporter assay and, in rats, it decreases food intake. It does not inhibit fatty acid amide hydrolase (FAAH).

Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.

Methyl ganoderate A, an inhibitor of Farnesyl protein transferase (FPT) with an IC50 of 38 µM, exhibits potential anticancer effects. Additionally, it inhibits fatty acid amide hydrolase (FAAH), further underscoring its therapeutic potential.

FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor with IC50 values of 145 nM for rat FAAH and 650 nM for human FAAH.

MAGL-IN-5 is a non-selective lipase inhibitor.

JNJ-40413269 is a competitive inhibitor of fatty acid amide hydrolase (FAAH), which demonstrates robust central target engagement, and shows efficacious in a rat model of neuropathic pain.

Decanoyl Chloride is used in the synthesis of an effective metalloproteinase inhibitor. Also acts as a reagent in the synthesis of reversible α-ketoheterocycle inhibitors of fatty acid amide hydrolase as potnetial analgesics.