Chemistry:SB-269970

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Short description: Chemical compound
SB-269970
SB-269,970 structure.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC18H28N2O3S
Molar mass352.49 g·mol−1
3D model (JSmol)
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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-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]

References

  1. ↑ "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. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157. 
  2. ↑ "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. doi:10.1021/jm991151j. PMID 10669560. 
  3. ↑ "5-HT antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig". NeuroReport 20 (3): 325–30. February 2009. doi:10.1097/WNR.0b013e3283232caa. PMID 19190523. 
  4. ↑ "5-HT7 receptors". Current Drug Targets. CNS and Neurological Disorders 3 (1): 81–90. February 2004. doi:10.2174/1568007043482633. PMID 14965246. 
  5. ↑ "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. doi:10.1016/j.ejphar.2007.05.037. PMID 17586491. 
  6. ↑ "5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern". Biological Psychiatry 58 (10): 831–7. November 2005. doi:10.1016/j.biopsych.2005.05.012. PMID 16018977. 
  7. ↑ "Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression". Neuropharmacology 51 (3): 578–86. September 2006. doi:10.1016/j.neuropharm.2006.04.017. PMID 16828124. 
  8. ↑ "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. doi:10.1016/j.bbr.2007.12.020. PMID 18308404. 
  9. ↑ "Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model". Hippocampus 18 (9): 965–74. 2008. doi:10.1002/hipo.20459. PMID 18570192. 





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