Cannabinoid Transporters

Cannabinoid transporters, often referred to as anandamide membrane transporters (AMTs) or endocannabinoid membrane transporters (EMTs), are thought to facilitate the reuptake of endocannabinoids into cells. However, their existence is controversial and no transmembrane protein transporter or gene encoding a transporter has been identified to date.

Products
Background
Literature (3)

Inhibitors

Cat. No. Product Name / Activity
3381 AM 1172
Anandamide uptake inhibitor; also FAAH inhibitor and CB receptor partial agonist
1116 AM 404
Anandamide transport inhibitor
1354 Arvanil
Potent CB1 and TRPV1 (VR1) agonist/anandamide transport inhibitor
1570 (-)-Cannabidiol
AMT inhibitor; also GPR55 antagonist, weak CB1 antagonist, CB2 inverse agonist; natural cannabinoid
1481 (-)-5'-DMH-CBD
Metabolically stable anandamide transport inhibitor
2452 LY 2183240
Highly potent anandamide uptake inhibitor; also inhibits FAAH
1446 O-2093
Inhibitor of anandamide uptake
1797 OMDM-2
Potent inhibitor of anandamide uptake
1966 UCM 707
Potent anandamide transport inhibitor

Cannabinoid transporters, or AMTs, transport endocannabinoids into cells and limit their activity at CB1, CB2 and GPR55 receptors. The action of cannabinoid transporters facilitates endocannabinoid breakdown by internalizing the molecule and allowing access to fatty acid amide hydrolase (FAAH).

Two endocannabinoids, Anandamide (also known as AEA, Cat. No. 1339) and 2-arachidonoylglycerol (2-AG, Cat. No. 1298), have been identified and since they are widely distributed, it has been suggested that AMTs should be present in many different tissues, although this has yet to be verified. Cannabinoid transporters are thought to play a vital role in the endocannabinoid system, and there is evidence for their existence from cell uptake studies and the physiological effects of inhibitors. However, some cannabinoid transporter inhibitors have been found to be FAAH inhibitors and endocannabinoids can pass through cell membranes without the need for a protein transporter owing to their lipid nature. Since endocannabinoids are lipids, carrier molecules are required to transport them through the aqueous cytosol, and a range of molecules have been described that function as intra- and extracellular endocannabinoid transporters.


Endocannabinoids - Synthesis, Release and Reuptake

Endocannabinoids - Generation, release and reuptake

Figure 1: Schematic showing the generation, release and reuptake of endocannabinoids. 2-AG, 2-Arachidonylglycerol; AC, adenylyl cyclase; DAG, diacylglycerol; FAAH, fatty acid amide hydrolase; FABP, fatty acid binding protein; MAG, monoacylglycerol; MAPK, mitogen-activated protein kinase; NAPE-PLD, N-acetylphosphatidylethanolamine-hydrolyzing phospholipase D; NArPE, N-arachidonoyl phosphatidylethanolamine.


Several lipid binding proteins or chaperones have been identified that bind, sequester, and/or traffic endocannabinoids. Fatty acid binding proteins (FABPs) (link to new target file) have been found to act as intracellular transporters of endocannabinoids and certain cannabinoid transporter inhibitors also bind to FABPs. It has also been shown that FABP inhibitors attenuate the uptake of the endocannabinoid Anandamide. FABPs also act as intracellular carriers for the naturally occurring cannabinoids THC and Cannabidiol (Cat. No. 1570). These plant-derived cannabinoids compete with anandamide for binding to FABPs, inhibiting the cellular uptake of anandamide and its subsequent catabolism by FAAH, and this may account for the increased levels of circulating anandamide associated with cannabidiol intake.

Other molecules that are likely intracellular transporters of endocannabinoids include heat shock protein 70 (hsp70), Sterol Carrier Protein-2 (SCP-2), albumin and FAAH-like anandamide transporter (FLAT).

External sources of pharmacological information for Cannabinoid Transporters :

    Literature for Cannabinoid Transporters

    Tocris offers the following scientific literature for Cannabinoid Transporters to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


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