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Endocannabinoid reuptake inhibitor

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Title: Endocannabinoid reuptake inhibitor  
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Subject: Endocannabinoid transporters, Neurochemistry, 2-Oleoylglycerol, Palmitoylethanolamide, Docosatetraenoylethanolamide
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Endocannabinoid reuptake inhibitor

Endocannabinoid reuptake inhibitors (eCBRIs), also called cannabinoid reuptake inhibitors (CBRIs), are drugs which limit or completely stop the reabsorption of endocannabinoid neurotransmitters into their corresponding pre-synaptic neurons.


There are several parts to the phrase endocannabinoid reuptake inhibitor. First, a reuptake inhibitor is a substance that prevents its respective neurotransmitters from being reabsorbed into the pre-sypnatic neurones, which makes them continually recycle themselves, thus creating a large increase in neurotransmission. Next, a cannabinoid is simply a class of closely related substances such as Tetrahydrocannabinol and Cannabidiol. 'Endo' is a prefix used to describe a cannabinoid that is naturally found within an animal. In retrospect, an endocannabinoid reuptake inhibitor is a substance that when ingested by an animal prevents reuptake of its endogenous cannabinoids. Endocannabinoid uptake inhibitors that bind to fatty acid binding protons (FABPs) have been described.[1]


The inhibition of endocannabinoid reuptake raises the amount of those neurotransmitters available in the synaptic cleft and therefore increases neurotransmission. Following the increase of neurotransmission in the endocannabinoid system is the stimulation of its functions which, in humans, include: suppression of pain perception (analgesia), increased appetite, mood elevation and inhibition of short-term memory.

Use in medicine

Other than toxicity research and recreational use, eCBRIs could have some potential in fighting tumors and possibly cancer. A study done in 2004 on rats with thyroid tumors showed that reuptake inhibition of the endocannabinoid system using VDM-11 and AA-5-HT reduced the ultimate size of the tumors in the treated rats. These findings suggest that the use of cannabinoids and/or eCBR inhibitors could be used to effectively treat tumors and/or cancer, which only adds to the controversy around cannabinoids and the cannabis plant as medicine.

As one might expect, combining a cannabinoid receptor antagonist with an eCBRI reverses the effects of the reuptake inhibitor, and therefore could hinder treatment. Cannabinoid receptor antagonists aren't something common, so normally this isn't something to worry about. But if smoked cannabis or cannabis extract is to be used as a treatment, it would be necessary to cultivate varieties with little to no amounts of these compounds, as they are found in low concentrations in most varieties. One example of these antagonist compounds which is found in the cannabis plant is THCV (tetrahydrocannabivarin).

Examples of eCBRIs

See also


  2. Costa, B; Siniscalco, D; Trovato, A. E.; Comelli, F; Sotgiu, M. L.; Colleoni, M; Maione, S; Rossi, F; Giagnoni, G (2006). "AM404, an inhibitor of anandamide uptake, prevents pain behaviour and modulates cytokine and apoptotic pathways in a rat model of neuropathic pain". British Journal of Pharmacology 148 (7): 1022–32.  
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