SB-269970 is adrug and research chemical developed byGlaxoSmithKline used in scientific studies. It is believed to act as a selective5-HT7receptorantagonist (EC50 = 1.25 nM) (or possiblyinverse agonist). A subsequent study in guinea pig at a concentration of 10 μM showed that it also blocks theα2-adrenergic receptor.[1][2][3] The large difference in test concentrations however confirms the selectivity of SB-269970 for the5-HT7 receptor.
SB-269970 is used to study the 5-HT7 receptors which are thought to be involved in the function of several areas of the brain such as thehippocampus andthalamus,[4] and regulation of dopamine release in theventral tegmental area.[5] Possible therapeutic uses for SB-269970 and other 5-HT7 antagonists include the treatment ofanxiety anddepression,[6][7] andnootropic effects have also been noted in animal studies.[8][9]
^Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (July 2004). "Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors".European Journal of Pharmacology.495 (2–3):97–102.doi:10.1016/j.ejphar.2004.05.033.PMID15249157.
^Lovell PJ, Bromidge SM, Dabbs S, Duckworth DM, Forbes IT, Jennings AJ, et al. (February 2000). "A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970)".Journal of Medicinal Chemistry.43 (3):342–5.doi:10.1021/jm991151j.PMID10669560.
^Thomas DR, Hagan JJ (February 2004). "5-HT7 receptors".Current Drug Targets. CNS and Neurological Disorders.3 (1):81–90.doi:10.2174/1568007043482633.PMID14965246.
^Mnie-Filali O, Dahan L, Zimmer L, Haddjeri N (September 2007). "Effects of the serotonin 5-HT(7) receptor antagonist SB-269970 on the inhibition of dopamine neuronal firing induced by amphetamine".European Journal of Pharmacology.570 (1–3):72–6.doi:10.1016/j.ejphar.2007.05.037.PMID17586491.
^Wesołowska A, Nikiforuk A, Stachowicz K, Tatarczyńska E (September 2006). "Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression".Neuropharmacology.51 (3):578–86.doi:10.1016/j.neuropharm.2006.04.017.PMID16828124.S2CID39928418.
^Gasbarri A, Cifariello A, Pompili A, Meneses A (December 2008). "Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat".Behavioural Brain Research.195 (1):164–70.doi:10.1016/j.bbr.2007.12.020.PMID18308404.S2CID12910296.
^Liy-Salmeron G, Meneses A (2008). "Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model".Hippocampus.18 (9):965–74.doi:10.1002/hipo.20459.PMID18570192.S2CID20937527.
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