| Identification | Back Directory | [Name]
Sb-742457 | [CAS]
607742-69-8 | [Synonyms]
CS-579
RVT-101
CS-2723
Sb 742457
Sb-742457
Gsk 742457
SB-742457(RVT-101)
Sb-742457 USP/EP/BP
RVT101. intepirdine.
SB742457:Intepirdine
SB 742457/GSK 742457
Intepirdine(SB742457)
Intepirdine (SB-742457, RVT-101）
SB 742457;RVT 101;SB742457;RVT101
3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline
3-(BENZENESULFONYL)-8-(PIPERAZIN-1-YL)QUINOLINE
Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)-
SB742457; SB 742457; SB-742457; RVT-101; RVT 101; RVT101. INTEPIRDINE. | [Molecular Formula]
C19H19N3O2S | [MDL Number]
MFCD12828872 | [MOL File]
607742-69-8.mol | [Molecular Weight]
353.44 |
| Chemical Properties | Back Directory | [Boiling point ]
608.3±45.0 °C(Predicted) | [density ]
1.292 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥17.65 mg/mL in DMSO; ≥2.13 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
8?+-.0.10(Predicted) |
| Hazard Information | Back Directory | [Description]
SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).1,2 SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.3 SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells.2 In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.1 It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.4 | [Uses]
SB 742457 is a selective 5-HT6 receptor antagonist which is known to be involved in improving cognitive function. | [target]
5-HT6 | [References]
[1] aaron t. t. chuang, andrew foley, perdita l. pugh, david sunter, xin tong, ciaran regan, lee a. dawson, andrew d. medhurst, neil upton.5-ht6 receptor antagonist sb-742457 as a novel cognitive enhancing agent for alzheimer’s disease. alzheimer's & dementia: the journal of the alzheimer's association volume 2, issue 3, supplement, pages s631–s632, july 2006 |
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