Name | SB742457 |
Synonyms | SB742457 Sb-742457 Sb 742457 Gsk 742457 Intepirdine(SB742457) 3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)- |
CAS | 607742-69-8 |
Molecular Formula | C19H19N3O2S |
Molar Mass | 353.44 |
Density | 1.292 |
Boling Point | 608.3±45.0 °C(Predicted) |
Solubility | Soluble in DMSO, not in water |
pKa | 8?+-.0.10(Predicted) |
Storage Condition | -20℃ |
Use | Intepirdine, also known as SB-742457 and RVT-101, is a selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects. It was under development by GlaxoSmithKline for the treatment of Alzheimer's disease and demonstrated some preliminary efficacy in phase II clinical trials. SB742457 can reverse age-related declines in delayed non-match-to-sample performance (DNMS). SB742457 shows increasing pro-cognitive effects in patients with AD. |
In vitro study | SB-742457 is a selective 5-HT6 receptor antagonist with cognitive, memory, and learning-enhancing effects. SB-742457 is a novel cognitive enhancer for the treatment of Alzheimer's disease. SB-742457 is a potential agent to enhance the stability of Donepezil in the treatment of mild to moderate Alzheimer's disease. |
In vivo study | SB-742457 is a potent, selective 5-HT6 receptor antagonist that reverses Scopolamine-induced learning deficits in the novel object recognition test and improves learning performance in the water maze task in aged rats. |
Reference Show more | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.829 ml | 14.147 ml | 28.293 ml |
5 mM | 0.566 ml | 2.829 ml | 5.659 ml |
10 mM | 0.283 ml | 1.415 ml | 2.829 ml |
5 mM | 0.057 ml | 0.283 ml | 0.566 ml |