"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

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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

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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