Anandamide membrane transporter (AMT) (AMT)

The Anandamide membrane transporter (AMT) is a putative transmembrane protein or transport system that mediates the cellular uptake of the endocannabinoid anandamide (N-arachidonoylethanolamine) from the extracellular space (Beltramo et al., 1997). This transport process is essential for the termination of endocannabinoid signaling, as it facilitates the delivery of anandamide to intracellular degradative enzymes, primarily fatty acid amide hydrolase (FAAH) (Fowler, 2013). AM404 (N-(4-hydroxyphenyl)arachidonamide) is a potent inhibitor of this transporter and is recognized as the active metabolite of paracetamol (acetaminophen) formed in the brain through FAAH-mediated synthesis (Högestätt et al., 2005). By inhibiting the AMT, AM404 increases the concentration and residence time of anandamide at its primary targets, including the cannabinoid CB1 receptor and the transient receptor potential vanilloid 1 (TRPV1) channel (Zygmunt et al., 2000). This mechanism is believed to underlie the analgesic and antipyretic properties of paracetamol and suggests the AMT as a viable therapeutic target for treating chronic pain, inflammation, and anxiety without the direct activation of cannabinoid receptors (Di Marzo et al., 1994). Although the specific molecular identity of the AMT is still debated, its pharmacological characterization remains a cornerstone of endocannabinoid research.

Other names

Endocannabinoid transporterAnandamide transportereCB transporterAnandamide reuptake carrier

Inhibition of the cellular reuptake of anandamide, leading to increased extracellular levels of endocannabinoids and subsequent activation of CB1 and TRPV1 receptors.