A 5-HT6 antagonist (Ki = 1.4 nM); binds to 5-HT1B

SB-742457 – 5 mg

Brand:
Cayman
CAS:
607742-69-8
Storage:
-20
UN-No:
De Minimis - 3077 / 6.1|9

SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).{40729,40731} SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.{40730} 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.{40731} In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.{40729} 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.{40732}  

 

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Description

A 5-HT6 antagonist (Ki = 1.4 nM); binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity; reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner (EC50 = 21 nM); reverses scopolamine-induced novel object recognition deficits and age-induced impairments in spatial memory in rats (1.5 mg/kg); has a satiating effect on rats (3.0 mg/kg, i.p.), reducing licking bouts by 24% compared to control in rats trained to lick a glucose solution

Formal name: 3-(phenylsulfonyl)-8-(1-piperazinyl)-quinoline

Synonyms:  GSK742457

Molecular weight: 353.4

CAS: 607742-69-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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