2020
DOI: 10.3390/molecules26010048
|View full text |Cite
|
Sign up to set email alerts
|

In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors

Abstract: Accumulated evidence suggests that enhancing the endocannabinoid (eCB) tone, in particular of anandamide (N-arachidonoylethanolamine, AEA), has therapeutic potential in many human diseases. Fatty acid amide hydrolase (FAAH) is a membrane-bound enzyme principally responsible for the degradation of AEA, and thus it represents a relevant target to increase signaling thereof. In recent years, different synthetic and natural compounds have been developed and tested on rat FAAH, but little is known of their effect o… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
1
1
1
1

Citation Types

0
5
0

Year Published

2021
2021
2024
2024

Publication Types

Select...
4
2
1

Relationship

0
7

Authors

Journals

citations
Cited by 9 publications
(5 citation statements)
references
References 75 publications
0
5
0
Order By: Relevance
“…The positions were rescored by GBVI/WSA dG scoring function. The cognate redocking was performed to validate the docking protocol and RMSD value of co‐crystallized ligand was calculated 24 . Ultimately, docking scores, best poses, and two‐ and three‐dimensional structures were recorded.…”
Section: Methodsmentioning
confidence: 99%
“…The positions were rescored by GBVI/WSA dG scoring function. The cognate redocking was performed to validate the docking protocol and RMSD value of co‐crystallized ligand was calculated 24 . Ultimately, docking scores, best poses, and two‐ and three‐dimensional structures were recorded.…”
Section: Methodsmentioning
confidence: 99%
“…Interestingly, the reduction of psychotic symptoms was significantly associated with an increase in the serum concentrations of N-arachidonoylethanolamine (anandamide, AEA, Figure 2), which is the most important endogenous ligand of CBR, and this outcome was found only in patients treated with CBD. The results indicated that, at least in part, the antipsychotic activity of CBD was due to the inhibition of the enzymes physiologically devoted to the degradation of AEA [22], thus acting as an indirect agonist. This finding agrees with the observation that both increased availability of CB 1 R and upregulation of AEA seem beneficial, although the underlying mechanisms are mostly elusive.…”
Section: Endocannabinoid Systemmentioning
confidence: 98%
“…CB1 [(PDB: 7V3Z]/, CB2 [(PDB: 5ZTY)]. The proteins were prepared using a protein preparation workflow tool on Schrӧdinger Protein Preparation Wizard [3,4]. The external water molecules and ions were removed.…”
Section: Proteins and Ligands Preparationmentioning
confidence: 99%
“…This peak does not appear at the 1 H-NMR spectrum of HHC. 13 C NMR: For Me-HHC (3), in the region between 50-60 ppm appears a peak corresponding with the methyl carbon in the methoxy group, which does not appear in the HHC (11). Table 2 provides NMR spectroscopic data for the Me-HHC (4) and D9-THC-ME (5).…”
Section: Synthesis and Characterization Of Hhc-me And D 8 Thc-mementioning
confidence: 99%
See 1 more Smart Citation