"目录号: HY-14339
GPCR/G ProteinNeuronal Signaling-
SB742457是5-HT6受体拮抗剂，pKi为9.63，比对其它受体的抑制性高100倍以上。
5-HT Receptor
相关产品
Clozapine N-oxide-Chlorpromazine hydrochloride-Pimavanserin-Brexpiprazole-Lorcaserin Hydrochloride-Scopolamine hydrobromide-Cariprazine hydrochloride-Harmine-Lu AE58054 Hydrochloride-TG6-10-1-Perphenazine-Aripiprazole-Ferulic acid sodium-Olanzapine-Sertindole-
生物活性
Description
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.
Clinical Trial
NCT02585934
Axovant Sciences Ltd.
Alzheimer's Disease
October 2015
Phase 3
NCT02928445
Axovant Sciences Ltd.
Dementia With Lewy Bodies
October 2016
Phase 2-Phase 3
NCT02586909
Axovant Sciences Ltd.
Alzheimer's Disease
April 2016
Phase 3
NCT02910102
Axovant Sciences Ltd.
Alzheimer's Disease-Dementia With Lewy Bodies-Parkinson's Disease Dementia
October 2016
Phase 2
NCT02669433
Axovant Sciences Ltd.
Dementia With Lewy Bodies
January 2016
Phase 2
NCT00710684
GlaxoSmithKline
Mild-to-moderate Alzheimer's Disease-Alzheimer's Disease
July 2008
Phase 2
NCT00348192
GlaxoSmithKline
Alzheimer's Disease
May 2006
Phase 2
NCT00551772
GlaxoSmithKline
Alzheimer's Disease
August 2007
Phase 1
NCT00708552
GlaxoSmithKline
Alzheimer's Disease
July 2008
Phase 2
NCT00224497
GlaxoSmithKline
Alzheimer's Disease
September 2005
Phase 2
View MoreCollapse
References
[1].Callaghan CK, Hok V, Della-Chiesa A, et al. Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457. Neuropharmacology. 2012 Oct;63(5):890-7.
[2].Codony X, Vela JM, Ramírez MJ. 5-HT(6) receptor and cognition. Curr Opin Pharmacol. 2011 Feb;11(1):94-100.
[3].Maher-Edwards G, Dixon R, Hunter J, et al. SB-742457 and donepezil in Alzheimer disease: a randomized, placebo-controlled study. Int J Geriatr Psychiatry. 2011 May;26(5):536-44.
[4].Maher-Edwards G, Zvartau-Hind M, Hunter AJ, et al. Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Alzheimer's disease. Curr Alzheimer Res. 2010 Aug;7(5):374-85.
[5].Upton N, Chuang TT, Hunter AJ, Virley DJ. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics. 2008 Jul;5(3):458-69.
[6].SB-742457