SB 742457

Research use only, not for human use.

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63.

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.(In Vitro):Intepirdine (SB742457), 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. Intepirdine (SB742457) is generally safe and well tolerated and may be efficacious in Alzheimer disease.

Intepirdine (SB742457), 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. Intepirdine (SB742457) is generally safe and well tolerated and may be efficacious in Alzheimer disease.

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GSK742457

Endocrinology/Hormones

5-HT Receptor

5-HT6

Neurological Disease

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607742-69-8

353.44

C19H19N3O2S

>98% (HPLC)

Ethanol: 2 mg/mL (5.65 mM); DMSO: 78 mg/mL (220.68 mM)

O=S(C1=CC2=CC=CC(N3CCNCC3)=C2N=C1)(C4=CC=CC=C4)=O

3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline

(-20℃)

With Ice Pack

≥ 2 years