SB-269970 explained

SB-269970 is a drug and research chemical developed by GlaxoSmithKline used in scientific studies. It is believed to act as a selective 5-HT7 receptor antagonist (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]

Notes and References

  1. Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P . 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 . July 2004 . 15249157 . 10.1016/j.ejphar.2004.05.033 .
  2. Lovell PJ, Bromidge SM, Dabbs S, Duckworth DM, Forbes IT, Jennings AJ, King FD, Middlemiss DN, Rahman SK, Saunders DV, Collin LL, Hagan JJ, Riley GJ, Thomas DR . 6 . 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 . February 2000 . 10669560 . 10.1021/jm991151j .
  3. Foong JP, Bornstein JC . 5-HT antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig . NeuroReport . 20 . 3 . 325–30 . February 2009 . 19190523 . 10.1097/WNR.0b013e3283232caa . 25499247 .
  4. Thomas DR, Hagan JJ . 5-HT7 receptors . Current Drug Targets. CNS and Neurological Disorders . 3 . 1 . 81–90 . February 2004 . 14965246 . 10.2174/1568007043482633 .
  5. 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 . 570 . 1–3 . 72–6 . September 2007 . 17586491 . 10.1016/j.ejphar.2007.05.037 .
  6. Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG . 5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern . Biological Psychiatry . 58 . 10 . 831–7 . November 2005 . 16018977 . 10.1016/j.biopsych.2005.05.012 . 10998014 .
  7. 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 . 51 . 3 . 578–86 . September 2006 . 16828124 . 10.1016/j.neuropharm.2006.04.017 . 39928418 .
  8. 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 . 195 . 1 . 164–70 . December 2008 . 18308404 . 10.1016/j.bbr.2007.12.020 . 12910296 .
  9. Liy-Salmeron G, Meneses A . Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model . Hippocampus . 18 . 9 . 965–74 . 2008 . 18570192 . 10.1002/hipo.20459 . 20937527 .

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