Reuptake enhancer

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Coluracetam, a high-affinity choline uptake (HACU) enhancer.

A reuptake enhancer (RE), also sometimes referred to as a reuptake activator, is a type of reuptake modulator which enhances the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron, leading to a decrease in the extracellular concentrations of the neurotransmitter and therefore a decrease in neurotransmission.

The antidepressant tianeptine 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 the serotonin transporter, neither increases nor decreases extracellular levels of serotonin in cortico-limbic structures of conscious rats, and it didn't show any other long-term effect on the serotonin pathway.[1] Thus, tianeptine's role as an SSRE may have been the coincidence of a yet unknown mechanism of action.

Coluracetam is a choline-reuptake enhancer.[2] The flavone luteoline as well as some of its derivatives enhance the reuptake at the dopamine transporter,[3][4] extracts of Caulis Sinomenii activate DA/NE transporters.[5]

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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. ^ "MKC-231, a choline-uptake enhancer: (1) long-lasting cognitive improvement after repeated administration in AF64A-treated rats". J Neural Transm. 115: 1019–25. Jul 2008. doi:10.1007/s00702-008-0053-4. PMID 18461272.
  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.
  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.