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SB-269970 is a drug and research chemical developed by GlaxoSmithKline used in scientific studies. It is believed to act as a selective 5-HT7receptorantagonist (EC50 = 1.25 nM) (or possibly inverse agonist). A subsequent study in guinea pig at a concentration of 10 μM showed that it also blocks the α2-adrenergic receptor.[1][2][3] The large difference in test concentrations however confirms the selectivity of SB-269970 for the 5-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 the hippocampus and thalamus,[4] and regulation of dopamine release in the ventral tegmental area.[5] Possible therapeutic uses for SB-269970 and other 5-HT7 antagonists include the treatment of anxiety and depression,[6][7] and nootropic effects have also been noted in animal studies.[8][9]
References
^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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This page was last edited on 2 June 2022, at 14:09