Reuptake enhancer
Drug that makes neurotransmitter transporters more active
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] Ultimately, tianeptine was determined to be a selective mu opioid receptor agonist.
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]
See also
- Reuptake inhibitor (RI)
- Releasing agent (RA)
- Serotonin modulator and stimulator (SMS), another term tentatively created to describe the action of a specific drug.
References
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- v
- t
- e
Receptor/signaling modulators
similar/related
- Amino acids and related: GABA receptor modulators
- GABAA receptor positive modulators
- GABA metabolism and transport modulators
- GHB receptor modulators
- Glutamate metabolism and transport modulators
- Glycine receptor modulators
- Ionotropic glutamate receptor modulators
- Metabotropic glutamate receptor modulators
- Monoamines: Adrenergic receptor modulators
- Dopamine receptor modulators
- Histamine receptor modulators
- Melatonin receptor modulators
- Monoamine metabolism modulators
- Monoamine neurotoxins
- Monoamine releasing agents
- Monoamine reuptake inhibitors
- Serotonin receptor modulators
- hTAAR modulators
- Acetylcholine: Acetylcholine metabolism and transport modulators
- Muscarinic acetylcholine receptor modulators
- Nicotinic acetylcholine receptor modulators
- Others: Imidazoline receptor modulators
- Purine receptor modulators
- Sigma receptor modulators
- Thyroid hormone receptor modulators
- Eicosanoids: Cannabinoid receptor modulators
- Leukotriene signaling modulators
- Prostanoid signaling modulators
- Phospholipids: Lysophospholipid signaling modulators
- PAF receptor modulators
- Steroids: Androgen receptor modulators
- Estrogen receptor modulators
- Glucocorticoid receptor modulators
- Mineralocorticoid receptor modulators
- Progesterone receptor modulators
- Steroid metabolism modulators
- Other nuclear receptors: Aryl hydrocarbon receptor modulators
- Estrogen-related receptor modulators
- FXR and LXR modulators
- PPAR modulators
- Retinoid receptor modulators
- Vitamin D receptor modulators
- Xenobiotic-sensing receptor modulators
- Peptides: Angiotensin receptor modulators
- GH/IGF-1 axis signaling modulators
- GnRH and gonadotropin receptor modulators
- Melanocortin receptor modulators
- Neurokinin receptor modulators
- Opioid receptor modulators
- Oxytocin and vasopressin receptor modulators
- Cytokines: Cytokine receptor modulators
- Chemokine receptor modulators
- Interleukin receptor modulators
- TNF receptor superfamily modulators
- Growth factors: Growth factor receptor modulators
- TGFβ receptor superfamily modulators
non-receptor
- Enzymes: Cytochrome P450 modulators
- Histone deacetylase inhibitors
- Phosphodiesterase inhibitors
- Ion channels: Ion channel modulators
- TRP channel modulators
- Transporters: Sodium-glucose transporter modulators
- Symporter inhibitors
- Others: Nitric oxide signaling modulators
 | This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it. |
- v
- t
- e
