SB-399885

Summary

SB-399885 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist, with a Ki of 9.0nM. SB-399885 and other 5-HT6 antagonists show nootropic effects in animal studies,[1][2] as well as antidepressant and anxiolytic effects which are comparable to and synergistic with drugs such as imipramine and diazepam,[3][4][5] and have been proposed as potential novel treatments for cognitive disorders such as schizophrenia[6] and Alzheimer's disease.

SB-399885
Identifiers
  • N-(3,5-Dichloro-2-methoxyphenyl)-4-methoxy-3-(1-piperazinyl)benzenesulfonamide
CAS Number
  • 402713-80-8 checkY
PubChem CID
  • 6918649
IUPHAR/BPS
  • 3241
ChemSpider
  • 5293842
ChEMBL
  • ChEMBL1210710 ☒N
CompTox Dashboard (EPA)
  • DTXSID60437717 Edit this at Wikidata
Chemical and physical data
FormulaC18H21Cl2N3O4S
Molar mass446.34 g·mol−1
3D model (JSmol)
  • Interactive image
  • C3CNCCN3c2cc(ccc2OC)S(=O)(=O)Nc(c1OC)cc(Cl)cc1Cl
  • InChI=1S/C18H21Cl2N3O4S/c1-26-17-4-3-13(11-16(17)23-7-5-21-6-8-23)28(24,25)22-15-10-12(19)9-14(20)18(15)27-2/h3-4,9-11,21-22H,5-8H2,1-2H3
  • Key:ATKZKAYWARYLBW-UHFFFAOYSA-N
 ☒NcheckY (what is this?)  (verify)

References edit

  1. ^ Perez-García G, Meneses A (July 2005). "Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task". Pharmacology, Biochemistry, and Behavior. 81 (3): 673–82. doi:10.1016/j.pbb.2005.05.005. PMID 15964617. S2CID 19789219.
  2. ^ Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, et al. (December 2006). "SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models". European Journal of Pharmacology. 553 (1–3): 109–19. doi:10.1016/j.ejphar.2006.09.049. PMID 17069795.
  3. ^ Wesołowska A, Nikiforuk A (April 2007). "Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression". Neuropharmacology. 52 (5): 1274–83. doi:10.1016/j.neuropharm.2007.01.007. PMID 17320917. S2CID 22664564.
  4. ^ Wesołowska A (February 2008). "The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors". European Journal of Pharmacology. 580 (3): 355–60. doi:10.1016/j.ejphar.2007.11.022. PMID 18096153.
  5. ^ Wesołowska A, Nikiforuk A (March 2008). "The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats". European Journal of Pharmacology. 582 (1–3): 88–93. doi:10.1016/j.ejphar.2007.12.013. PMID 18234190.
  6. ^ Li Z, Huang M, Prus AJ, Dai J, Meltzer HY (February 2007). "5-HT6 receptor antagonist SB-399885 potentiates haloperidol and risperidone-induced dopamine efflux in the medial prefrontal cortex or hippocampus". Brain Research. 1134 (1): 70–8. doi:10.1016/j.brainres.2006.11.060. PMID 17207474. S2CID 21162681.