| DC10404 |
BIA 10-2474
|
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions. |
| DC73733 |
UCM1341
|
UCM1341 (UCM 1341) is a bivalent ligand with melatonin receptor agonist (hMT1/hMT2, pKi=9.11/8.77) and fatty acid amide hydrolase (FAAH) inhibitory activity (rFAAH IC5=0.85 nM). |
| DC73732 |
ARN15381
|
ARN15381 is a potent, multitarget FAAH inhibitor/D3 partial agonist with low nanomolar range activity, decreases nicotine self-administration in male rats. |
| DC71543 |
Carpro-AM1
|
Carpro-AM1 is a dual-acting FAAH/substrate-selective COX inhibitor with an IC50 value of 94 nM for FAAH. |
| DC70700 |
PKM-833
|
PKM-833 (PKM833) is a potent, selective, and orally active FAAH inhibitor with IC50 of 8.8 and 10 nM against human and rat FAAH, respectively.PKM‐833 showed human and rat K inact/K i values with 34 300 ± 10 800 and 128 000 ± 39 800 mol-1 L−1 s-1, respectively.PKM-833 does not inhibit human MAGL and a panel of 137 molecular targets, exhibits weak inhibitory effects (>50%) in five receptor binding assays [PFA, 5‐HT2B, sigma, Na+ channel and Cl‐ channel (GABA gated) at 20 uM.PKM-833 showed excellent brain penetration and good oral bioavailability, and elevated anandamide (AEA) concentrations in the rat brain.PKM-833 significantly attenuated formalin-induced pain responses (3 mg/kg) and improved mechanical allodynia in CFA-induced inflammatory pain (0.3-3 mg/kg) in rat models, without significant side effects on catalepsy and motor coordination up to 30 mg/kg. |
