Английская Википедия:Endocannabinoid reuptake inhibitor

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Шаблон:Short description 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]

Pharmacology

The method of transport of endocannabinoids through the cell membrane and cytoplasm to their respective degradation enzymes has been rigorously debated for nearly two decades, and a putative endocannabinoid membrane transporter was proposed.[3] However, as lipophilic molecules endocannabinoids readily pass through the cell lipid bilayer without assistance and would more likely need a chaperone through the cytoplasm to the endoplasmic reticulum where the enzyme FAAH is located. More recently fatty acid-binding proteins (FABPs) and heat shock proteins (Hsp70s) have been described and verified as such chaperones, and their inhibitors have been synthesized.[1][4] 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.[5][6]

Examples of eCBRIs

See also

References

Шаблон:Reflist

Шаблон:Cannabinoidergics

  1. 1,0 1,1 Шаблон:Cite journal
  2. 2,0 2,1 Шаблон:Cite journal
  3. Шаблон:Cite journal
  4. Шаблон:Cite journal
  5. Шаблон:Cite web
  6. Шаблон:Cite journal
  7. Шаблон:Cite journal
  8. Шаблон:Cite journal
  9. Шаблон:Cite journal
  10. Шаблон:Cite journal
  11. 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.