Endocannabinoid reuptake inhibitor
Endocannabinoid reuptake inhibitors (eCBRIs), also called cannabinoid reuptake inhibitors (CBRIs), are drugs which limit the reabsorption of endocannabinoid neurotransmitters by the releasing neuron.
Endocannabinoid uptake inhibitors that bind to fatty acid-binding proteins (FABPs) have been described. 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.
Examples of eCBRIs
- WOBE437 and RX-055
- Endocannabinoid enhancer
- Endocannabinoid system
- Reuptake inhibitor
- Cannabinoid receptor antagonist
- Endocannabinoid transporters
- FAAH inhibitor
- MAGL inhibitor
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- Chicca A, Nicolussi S, Bartholomäus R, Blunder M, Aparisi Rey A, Petrucci V, Reynoso-Moreno IDC, Viveros-Paredes JM, Dalghi Gens M, Lutz B, Schiöth HB, Soeberdt M, Abels C, Charles RP, Altmann KH, Gertsch J. Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake.Proc Natl Acad Sci U S A. 2017 Jun 5. doi: 10.1073/pnas.1704065114. PMID 28584105
- Nicolussi S, Chicca A, Soeberdt M, Abels C, Viveros.Paredes JM, Aparisi-Rey A, Lutz B, Gertsch J. WOBE437 - Prototype of a novel class of potent, selective endocannabinoid reuptake inhibitors. BPS 6th Eur Workshop on Cannabinoid Research 2013.