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SB-269970

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SB-269970
SB-269,970 structure.png
Systematic (IUPAC) name
(2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2 -(2-(4-methyl-1-piperidinyl)ethyl)pyrrolidine
Identifiers
CAS Number 201038-74-6 YesY
PubChem CID 6604889
IUPHAR/BPS 3233
ChEMBL CHEMBL282199 N
Chemical data
Formula C18H28N2O3S
Molar mass 352.490 g/mol
 NYesY (what is this?)  (verify)

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 10 uM showed that it also blocks the α2-adrenergic receptor activity.[1][2][3] The significant 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[edit]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ Thomas DR, Hagan JJ (2004). "5-HT7 receptors". Current drug targets. CNS and neurological disorders 3 (1): 81–90. doi:10.2174/1568007043482633. PMID 14965246. 
  5. ^ Mnie-Filali O, Dahan L, Zimmer L, Haddjeri N (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. PMID 17586491. 
  6. ^ Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG (2005). "5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern". Biological Psychiatry 58 (10): 831–7. doi:10.1016/j.biopsych.2005.05.012. PMID 16018977. 
  7. ^ Wesołowska A, Nikiforuk A, Stachowicz K, Tatarczyńska E (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. PMID 16828124. 
  8. ^ Gasbarri A, Cifariello A, Pompili A, Meneses A (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. PMID 18308404. 
  9. ^ 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. PMID 18570192. 



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