SB-399,885
SB-399885 je lek koji se koristi u naučnim istraživanjima. On deluje kao potentan, selektivan i oralno aktivan antagonist 5-HT6 receptora, sa Ki od 9,0 nM. SB-399885 i drugi 5-HT6 antagonisti pokazuju nootropne efekte u životinjskim studijama,[1][2] kao i antidepresivne i anksiolitičke efekte koji su uporedivi i sinergistički sa drugim lekovima kao što su imipramin i diazepam.[3][4][5] Oni potencijalno mogu da služe kao tretmani za kognitivne poremećaje, kao što je šizofrenija[6] i Alchajmerova bolest.
IUPAC ime | |
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N-(3,5-Dihloro-2-metoksifenil)-4-metoksi-3-(1-piperazinil)benzensulfonamid | |
Identifikatori | |
CAS broj | 402713-80-8 |
ATC kod | none |
PubChem | CID 6918649 |
ChEMBL | CHEMBL1210710 |
Hemijski podaci | |
Formula | C18H21Cl2N3O4S |
Molarna masa | 446,347 g/mol |
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Reference уреди
- ^ Perez-García, G; Meneses, A (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. PMID 15964617. doi:10.1016/j.pbb.2005.05.005.
- ^ Hirst, WD; Stean, TO; Rogers, DC; Sunter, D; Pugh, P; Moss, SF; Bromidge, SM; Riley, G; Smith, DR (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. PMID 17069795. doi:10.1016/j.ejphar.2006.09.049.
- ^ Wesołowska, A; Nikiforuk, A (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. PMID 17320917. doi:10.1016/j.neuropharm.2007.01.007.
- ^ Wesołowska, A (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. PMID 18096153. doi:10.1016/j.ejphar.2007.11.022.
- ^ Wesołowska, A; Nikiforuk, A (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. PMID 18234190. doi:10.1016/j.ejphar.2007.12.013.
- ^ Li, Z; Huang, M; Prus, AJ; Dai, J; Meltzer, HY (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. PMID 17207474. doi:10.1016/j.brainres.2006.11.060.