Endocannabinoid Reuptake Inhibitors

Endocannabinoid reuptake inhibitors (eCBRIs), also called cannabinoid reuptake inhibitors (CBRIs), are drugs which limit the reabsorption of endocannabinoidneurotransmitters 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.









WOBE437 and RX-055[6][7]

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  1.  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. doi:10.1371/journal.pone.0050968. PMC 3517626. PMID 23236415.
  2. 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. doi:10.1038/sj.bjp.0706798. PMC 1751928. PMID 16770320.
  3. ^ Glaser ST, Kaczocha M, Deutsch DG. Anandamide transport: a critical review. Life Sci. 2005 Aug 19;77(14):1584-604. PMID 15979096
  4. ^ 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
  5. ^ 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
  6. ^ 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
  7. ^ 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.
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