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SB-269,970
Systematic (IUPAC) name
(2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2 -(2-(4-methyl-1-piperidinyl)ethyl)pyrrolidine
Identifiers
CAS number 201038-74-6
ATC code  ?
PubChem 6604889
Chemical data
Formula C 18H28N2O3S 
Mol. mass 352.490 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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.[1][2][3] The new finding has raised significant concerns about studies using SB-269,970 as a specific serotonin receptor antagonist.[3]

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,[4] and regulation of dopamine release in the ventral tegmental area.[5] Possible therapeutic uses for SB-269,970 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. ^ 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. ^ a b 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. PMID 19190523.  
  4. ^ Thomas DR, Hagan JJ. 5-HT7 receptors. Current Drug Targets. CNS and Neurological Disorders. 2004 Feb;3(1):81-90. PMID 14965246
  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. 2007 Sep 10;570(1-3):72-6. PMID 17586491
  6. ^ 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
  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. 2006 Sep;51(3):578-86. PMID 16828124
  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. 2008 Dec 16;195(1):164-70. PMID 18308404
  9. ^ 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







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