Endocannabinoid reuptake inhibitor

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Endocannabinoid reuptake inhibitors (eCBRI), similar to cannabinoid reuptake inhibitors (CBRI), are substances which limit or completely stop the reabsorption of endocannabinoid neurotransmitters into their corresponding pre-synaptic neurons.

Pharmacology

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: pain perception, increased appetite, mood elevation and short-term memory. If taken in combination with a powerful cannabinoid receptor agonist such as JWH-018, CP 55,940 or the super-potent HU-210, it could greatly increase the aforementioned effects. It is possible that this kind of combination could allow a human to experience a rare and never-before experienced overdose of cannabinoids. Although this could be a potentially dangerous experiment, the use of less potent, natural cannabinoids (like the ones found in cannabis) in combination with eCBRIs could turn out to have some recreational value as cannabis enhancers.

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 compounds which is found in the cannabis plant is THCV (tetrahydrocannabivarin).

List of various eCBR Inhibitors

References

  1. http://www.fasebj.org/cgi/content/full/18/13/1606
  2. http://www.ncbi.nlm.nih.gov/pubmed/16770320

See also