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SB-269,970 is a drug and research chemical developed by GlaxoSmithKline used in scientific studies. It was previously believed to act as a selective 5-HT7 receptor antagonist (or possibly inverse agonist), but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor. The new finding has raised significant concerns about studies using SB-269,970 as a specific serotonin receptor antagonist.
SB-269,970 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, and regulation of dopamine release in the ventral tegmental area. Possible therapeutic uses for SB-269,970 and other 5-HT7 antagonists include the treatment of anxiety and depression, and nootropic effects have also been noted in animal studies.
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- Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (2004). "Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors". Eur. J. Pharmacol. 495 (2-3): 97–102. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157.
- Lovell PJ, Bromidge SM, Dabbs S; et al. (2000). "A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phenol (SB-269970)". J. Med. Chem. 43 (3): 342–5. doi:10.1021/jm991151j. PMID 10669560.
- Foong JP, Bornstein JC. (2009). "5-HT antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig". Neuroreport. 20 (3): 325–330. doi:10.1097/WNR.0b013e3283232caa. PMID 19190523.
- Thomas DR, Hagan JJ. 5-HT7 receptors. Current Drug Targets. CNS and Neurological Disorders. 2004 Feb;3(1):81-90. PMID 14965246
- Mnie-Filali O, Dahan L, Zimmer L, Haddjeri N. 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. 2007 Sep 10;570(1-3):72-6. PMID 17586491
- Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG. 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern. Biological Psychiatry. 2005 Nov 15;58(10):831-7. PMID 16018977
- Wesołowska A, Nikiforuk A, Stachowicz K, Tatarczyńska E. Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression. Neuropharmacology. 2006 Sep;51(3):578-86. PMID 16828124
- Gasbarri A, Cifariello A, Pompili A, Meneses A. Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat. Behavioural Brain Research. 2008 Dec 16;195(1):164-70. PMID 18308404
- Liy-Salmeron G, Meneses A. Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model. Hippocampus. 2008;18(9):965-74. PMID 18570192