SB-742457

• CAT Number: I004290
• CAS Number: 607742-69-8
• Molecular Formula: C₁₉H₁₉N₃O₂S
• Molecular Weight: 353.44
• Purity: ≥95%
• Synonyms: 3-(benzenesulfonyl)-8-piperazin-1-ylquinoline
• Target: 5-HT Receptor
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 9.63 (pKi)
• InChI: InChI=1S/C19H19N3O2S/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22/h1-8,13-14,20H,9-12H2
• InChIKey: JJZFWROHYSMCMU-UHFFFAOYSA-N
• SMILES: C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.IC50 Value: 9.63 (pKi)Target: 5-HT6 ReceptorSB-742457, a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer/’s disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. SB-742457 is generally safe and well tolerated and may be efficacious in Alzheimer disease.

Reference

1:The 5-HT₂C receptor agonist, lorcaserin, and the 5-HT₆ receptor antagonist, SB-742457, promote satiety; a microstructural analysis of feeding behaviour. Higgs S, Cooper AJ, Barnes NM.Psychopharmacology (Berl). 2016 Feb;233(3):417-24. doi: 10.1007/s00213-015-4112-x. Epub 2015 Oct 28. PMID: 26507195 Free PMC Article2:SB-742457 and donepezil in Alzheimer disease: a randomized, placebo-controlled study. Maher-Edwards G, Dixon R, Hunter J, Gold M, Hopton G, Jacobs G, Hunter J, Williams P.Int J Geriatr Psychiatry. 2011 May;26(5):536-44. doi: 10.1002/gps.2562. Epub 2010 Sep 24. PMID: 20872778 3:Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer/’s disease. Maher-Edwards G, Zvartau-Hind M, Hunter AJ, Gold M, Hopton G, Jacobs G, Davy M, Williams P.Curr Alzheimer Res. 2010 Aug;7(5):374-85. PMID: 20043816