Endocannabinoid transporter
The endocannabinoid transporters (eCBTs) are
fatty acid amide hydrolase (FAAH) in cell culture.[6] One of these inhibitors (SB-FI-26), isolated from a virtual library of a million compounds, belongs to a class of compounds (named the "truxilloids') that act as an anti-nociceptive agent with mild anti-inflammatory activity in mice.[10] These truxillic acids and their derivatives have been known to have anti-inflammatory and anti-nociceptive effects in mice[11] and are active components of a Chinese herbal medicine ((−)-Incarvillateine Incarvillea sinensis) used to treat rheumatism
and pain in human. The blockade of anandamide transport may, at least in part, be the mechanism through which these compounds exert their anti-nociceptive effects.
Studies have found the involvement of
Michaelis–Menten constant) of the AEA membrane transporter (AMT) is almost doubled compared with control cells, demonstrate that, among the proteins of the “endocannabinoid system,” only CB1 and AMT critically depend on membrane cholesterol content, an observation that may have important implications for the role of CB1 in protecting nerve cells against (endo)cannabinoid-induced apoptosis.[14] This can be a reason, why the use of drugs to lower cholesterol is tied to a higher depression risk, and the correlation between levels and increased death rates from suicide and other violent causes.[15][16]
Activation of CB1 enhances AMT activity through increased
endothelial cells.[17]
As reviewed in 2016; "Many of the AMT (EMT) proposals have fallen by the wayside."[18] To date a transmembrane protein transporter has not been identified.
See also
References
- PMID 22860204.
- PMID 15930521.
- PMID 16461355.
- PMID 15784231.
- PMID 19330032.
- ^ PMID 19307565.
- PMID 19481477.
- PMID 27552286.
- PMID 25666611.
- PMID 23236415.
- PMID 10514316.
- PMID 19330032.
- S2CID 12649901.
- S2CID 23328664.
- ISSN 0362-4331. Retrieved 2017-10-31.
- PMID 24503286.
- PMID 16543970.
- ^ Deutsch DG. A Personal Retrospective: Elevating Anandamide (AEA) by Targeting Fatty Acid Amide Hydrolase (FAAH) and the Fatty Acid Binding Proteins (FABPs). Frontiers in Pharmacology. 2016;7:370. doi:10.3389/fphar.2016.00370.