Inhibitor preuzimanja
Inhibitor preuzimanja (RI, blokator transportera) je lek koji inhibira transporterom posredovano preuzimanje neurotransmitera iz sinapse u presinaptički neuron, što dovodi do povišenja ekstracelularne koncentracije neurotransmitera i stoga povišenja neurotransmisije. Različiti lekovi koriste inhibiciju preuzimanja za izvršavanje njihovog psihološkog i fiziološkog dejstva, uključujući mnoge antidepresive i psihostimulanse.[1]
Većina poznatih inhibitora preuzimanja utiče na monoaminske neurotransmitore serotonina, norepinefrina (i epinefrina), i dopamina.[1] Međutim postoji i znatan broj lekova i istraživačkih hemikalija koje deluju kao inhibitori preuzimanja za druge neurotransmitere kao što je glutamat,[2] γ-aminobuterna kiselina (GABA),[3] glicin,[4] adenozin,[5] holin (prekurzor acetilholina),[6] i endokanabinoide,[7] između ostalih.[1]
Reference
- ↑ 1,0 1,1 1,2 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Barkhimer TV, Kirchhoff JR, Hudson RA, Messer WS (November 2002). <3699::AID-ELPS3699>3.0.CO;2-E „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.
- ↑ 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.
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2-(1-Heksinil)-N-metiladenozin • 2-Cl-IB-MECA • 2'-MeCCPA • 5'-N-etilkarboksamidoadenozin • ATL-146e • BAY 60-6583 • CCPA • CGS-21680 • CP-532,903 • GR 79236 • LUF-5835 • LUF-5845 • N6-Ciklopentiladenozin • Regadenoson • SDZ WAG 994 • UK-432,097 | |
Antagonisti | 8-Fenil-1,3-dipropilksantin • Acefilin • Aminofilin • Bamifilin • Kofein • CGS-15943 • 8-Hloroteofilin • CPX • CVT-6883 • Dimetazan • DPCPX • Fenetilin • Istradefilin • KF-26777 • MRE3008F20 • MRS-1220 • MRS-1334 • MRS-1706 • MRS-1754 • MRS-3777 • Paraksantin • Pentoksifilin • Preladenant • Propentofilin • PSB-10 • PSB-11 • PSB 36 • PSB-603 • PSB-788 • PSB-1115 • Rolofilin • SCH-442,416 • SCH-58261 • Teobromin • Teofilin • VUF-5574 • ZM-241,385 |
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