Reuptake inhibitor

Escitalopram, a selective serotonin reuptake inhibitor (SSRI) used as an antidepressant.

Reuptake inhibitors (RIs) are a type of reuptake modulators. It is a drug that inhibits the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron. This leads to an increase in extracellular concentrations of the neurotransmitter and an increase in neurotransmission. Various drugs exert their psychological and physiological effects through reuptake inhibition, including many antidepressants and psychostimulants.[1]

Most known reuptake inhibitors affect the monoamine neurotransmitters serotonin, norepinephrine (and epinephrine), and dopamine.[1] However, there are also a number of pharmaceuticals and research chemicals that act as reuptake inhibitors for other neurotransmitters such as glutamate,[2] γ-aminobutyric acid (GABA),[3] glycine,[4] adenosine,[5] choline (the precursor of acetylcholine),[6] and the endocannabinoids,[7] among others.[1]

  1. ^ a b c Iversen L. (2006). "Neurotransmitter transporters and their impact on the development of psychopharmacology". Br J Pharmacol. 147 (1): S82–88. doi:10.1038/sj.bjp.0706428. PMC 1760736. PMID 16402124.
  2. ^ West AR, Galloway MP (1997). "Inhibition of glutamate reuptake potentiates endogenous nitric oxide-facilitated dopamine efflux in the rat striatum: an in vivo microdialysis study". Neurosci. Lett. 230 (1): 21–4. doi:10.1016/S0304-3940(97)00465-5. PMID 9259454. S2CID 1425558.
  3. ^ Pollack MH, Roy-Byrne PP, Van Ameringen M, Snyder H, Brown C, Ondrasik J, Rickels K (2005). "The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study". J Clin Psychiatry. 66 (11): 1401–8. doi:10.4088/JCP.v66n1109. PMID 16420077.
  4. ^ Alberati D, Moreau JL, Lengyel J, et al. (February 2012). "Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia". Neuropharmacology. 62 (2): 1152–61. doi:10.1016/j.neuropharm.2011.11.008. PMID 22138164. S2CID 12504169.
  5. ^ Boissard CG, Gribkoff VK (1993). "The effects of the adenosine reuptake inhibitor soluflazine on synaptic potentials and population hypoxic depolarizations in area CA1 of rat hippocampus in vitro". Neuropharmacology. 32 (2): 149–55. doi:10.1016/0028-3908(93)90095-K. PMID 8383814. S2CID 10716297.
  6. ^ Barkhimer TV, Kirchhoff JR, Hudson RA, Messer WS (November 2002). "Evaluation of the inhibition of choline uptake in synaptosomes by capillary electrophoresis with electrochemical detection". Electrophoresis. 23 (21): 3699–704. doi:10.1002/1522-2683(200211)23:21<3699::AID-ELPS3699>3.0.CO;2-E. PMID 12432531. S2CID 11719462.
  7. ^ Costa B, Siniscalco D, Trovato AE, Comelli F, Sotgiu ML, Colleoni M, Maione S, Rossi F, Giagnoni G (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.