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Reuptake enhancer

From Wikipedia, the free encyclopedia

Drug that makes neurotransmitter transporters more active
Coluracetam, a high-affinity choline uptake (HACU) enhancer

Areuptake enhancer (RE), also sometimes referred to as areuptake activator, is a type ofreuptake modulator which enhances theplasmalemmaltransporter-mediatedreuptake of aneurotransmitter from thesynapse into thepre-synapticneuron, leading to a decrease in theextracellularconcentrations of the neurotransmitter and therefore a decrease inneurotransmission.

Theantidepressanttianeptine was once claimed to be a(selective)serotonin reuptake enhancer (SRE or SSRE), but the role of serotonin reuptake in its mechanism is doubtful. Tianeptine has no affinity for theserotonin transporter, neither increases nor decreases extracellular levels of serotonin incortico-limbic structures of conscious rats, and it didn't show any other long-term effect on the serotonin pathway.[1] Ultimately, tianeptine was determined to be a selective mu opioid receptor agonist.

Coluracetam is a choline-reuptake enhancer.[2] Theflavoneluteoline as well as some of itsderivatives enhance the reuptake at thedopamine transporter,[3][4] extracts ofCaulis Sinomenii activate DA/NE transporters.[5]

See also

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References

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  1. ^McEwen, B. S.; Chattarji, S.; Diamond, D. M.; Jay, T. M.; Reagan, L. P.; Svenningsson, P.; Fuchs, E. (March 2010)."The neurobiological properties of tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation".Molecular Psychiatry.15 (3):237–249.doi:10.1038/mp.2009.80.PMC 2902200.PMID 19704408.
  2. ^Bessho, Tomoko; Takashina, Ken; Eguchi, Junichi; Komatsu, Teiko; Saito, Ken-Ichi (July 2008). "MKC-231, a choline-uptake enhancer: (1) long-lasting cognitive improvement after repeated administration in AF64A-treated rats".J Neural Transm.115 (7):1019–25.doi:10.1007/s00702-008-0053-4.PMID 18461272.S2CID 20201642.
  3. ^Zhao G, Qin GW, Wang J, Chu WJ, Guo LH (2010). "Functional activation of monoamine transporters by luteolin and apigenin isolated from the fruit of Perilla frutescens (L.) Britt".Neurochem. Int.56 (1):168–76.doi:10.1016/j.neuint.2009.09.015.PMID 19815045.S2CID 24753206.
  4. ^Zhang J, Liu X, Lei X, et al. (2010). "Discovery and synthesis of novel luteolin derivatives as DAT agonists".Bioorg. Med. Chem.18 (22):7842–8.doi:10.1016/j.bmc.2010.09.049.PMID 20971650.
  5. ^Zhao G, Bi C, Qin GW, Guo LH (2009). "Caulis Sinomenii extracts activate DA/NE transporter and inhibit 5HT transporter".Exp. Biol. Med. (Maywood).234 (8):976–85.doi:10.3181/0903-RM-92.PMID 19491370.S2CID 22915943.
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