Endocannabinoid reuptake inhibitor

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Endocannabinoid reuptake inhibitors (eCBRIs), also called cannabinoid reuptake inhibitors (CBRIs), are drugs which limit the reabsorption of endocannabinoid neurotransmitters by the releasing neuron.[1][2]


Endocannabinoid uptake inhibitors that bind to fatty acid-binding proteins (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[edit]

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.[3] 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[edit]

See also[edit]


  1. ^ a b Berger WT, Ralph BP, Kaczocha M, Sun J, Balius TE, Rizzo RC, et al. (2012). "Targeting fatty acid binding protein (FABP) anandamide transporters - a novel strategy for development of anti-inflammatory and anti-nociceptive drugs". PLoS ONE. 7 (12): e50968. PMC 3517626Freely accessible. PMID 23236415. doi:10.1371/journal.pone.0050968. 
  2. ^ a b Costa B, Siniscalco D, Trovato AE, Comelli F, Sotgiu ML, Colleoni M, et al. (2006). "AM404, an inhibitor of anandamide uptake, prevents pain behaviour and modulates cytokine and apoptotic pathways in a rat model of neuropathic pain". Br. J. Pharmacol. 148 (7): 1022–32. PMC 1751928Freely accessible. PMID 16770320. doi:10.1038/sj.bjp.0706798. 
  3. ^ Bifulco M, Laezza C, Valenti M, Ligresti A, Portella G, DI Marzo V (2004). "A new strategy to block tumor growth by inhibiting endocannabinoid inactivation". FASEB J. 18 (13): 1606–8. PMID 15289448. doi:10.1096/fj.04-1754fje. 
  4. ^ Glaser ST, Kaczocha M, Deutsch DG. Anandamide transport: a critical review. Life Sci. 2005 Aug 19;77(14):1584-604. PMID 15979096
  5. ^ Moore SA, Nomikos GG, Dickason-Chesterfield AK, Schober DA, Schaus JM, Ying B., Xu BP , Phebus L, Simmons RMA,Li D,Iyengar S, Felder CC. Proc Natl Acad Sci USA. 2005 Dec 6;102(49):17852-7. PMID 24412246
  6. ^ Nicolussi S, Viveros-Paredes JM, Gachet MS, Rau M, Flores-Soto ME, Blunder M, Gertsch J. Guineensine is a novel inhibitor of endocannabinoid uptake showing cannabimimetic behavioral effects in BALB/c mice. Pharmacol Res. 2014 Feb;80:52-65. PMID 24412246
  7. ^ Nicolussi S, Gertsch J, Reymond JL. Thiazolidinones as cellular anandamide uptake inhibitors and their use in the treatment of psychiatric or neurological disorders and inflammation, in particular neuroinflammation. EP20140171022
  8. ^ 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
  9. ^ 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.