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    SB 271046 HCl (SB-271046A)
    SB 271046 HCl (SB-271046A)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0980
    CAS #: 209481-24-3 Purity ≥98%

    Description: SB271046 HCl (SB 271046; SB-271046), the hydrochloride salt of SB 271046, is a novel, potent, selective and orally bioactive 5-HT6 receptor antagonist with potential anticonvulsant activity. It inhibits 5-HT6 with a pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes. 

    References: Br J Pharmacol. 2000 Aug;130(7):1606-12; J Med Chem. 1999 Jan 28;42(2):202-5.

    Related CAS: 209481-20-9 (free base)

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    Molecular Weight (MW)488.45 
    CAS No.209481-24-3 (HCl salt);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 40 mg/mL (81.9 mM)  
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% methylcellulose: ~30 mg/mL 
    SynonymsSB-271046; SB 271046; SB271046; SB-271046 HCl; SB-271046 hydrochloride
    SMILES CodeO=S(C1=C(C)C2=CC(Cl)=CC=C2S1)(NC3=CC=C(OC)C(N4CCNCC4)=C3)=O.[H]Cl

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    In Vitro

    In vitro activity: SB-271046 also potently displaces [125I]-SB-258585 from rat and pig striatal and human caudate putamen membranes with pKis of 9.02, 8.55 and 8.81, respectively. SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71. SB-271046 is found to be a competitive antagonist with a pA2 of 8.7 in the functional adenylyl cyclase assay which is in good agreement with its binding affinity. SB-271046 demonstrates no significant inhibitory activity at the major human P450 enzymes.

    Kinase Assay: SB271046 Hcl is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. IC50 Value: 8.9(pKi). SB 271046 hydrochloride is a sulfonamidal benzothiophene derivative that has been shown to act as a selective 5-HT6 antagonist with pKi values of 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 for 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively, and is > 200-fold selective over 55 other receptors, enzymes and ion channels. 

    In VivoSB-271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of 0.1 mg/kg p.o. and maximum effect at 4 hours post-dose. The level of anticonvulsant activity achieves correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01 μM–0.04 μM at Cmax. SB-271046 is moderately brain penetrant (10%), subject to low blood clearance (7.7 mL/min/kg) with a good half-life in rats (4.8 hours), and has excellent oral bioavailability (>80%). SB-271046 produces 3-fold and 2-fold increases in extracellular glutamate levels in both frontal cortex and dorsal hippocampus of rats, respectively, which may be used for the treatment of cognitive and memory dysfunction. SB-271046 (20 mg/kg, orally gavage) 30 min prior to training Wistar rats, is found to reverse significantly the amnesia produced by administering scopolamine (0.8 mg/kg, i.p.) in the 6 hours post-training period. SB-271046 progressively and significantly decreases platform swim angle and escape latencies over the five sequential trials on four consecutive daily sessions compared to vehicle-treated controls in aged rats. SB-271046 also improves task recall as measured by significant increases in the searching of the target quadrant on post-training days 1 and 3. SB-271046 (10 mg/kg, s.c.) produces a significant, tetrodotoxin-dependent, increase in extracellular levels of both glutamate and aspartate within the frontal cortex of rats, reaching maximum values of 375.4% and 215.3% of preinjection values, respectively. 
    Animal modelMale Sprague Dawley rats 
    Formulation & DosageDissolved in 1% methyl cellulose in water; 30 mg/kg; Oral gavage 
    ReferencesBr J Pharmacol. 2000 Aug;130(7):1606-12; J Med Chem. 1999 Jan 28;42(2):202-5. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    SB 271046 HCl

    (a) Stimulation of adenylyl cyclase activity in HeLa cells stably expressing human 5-HT6 receptors by 5-HT alone and in the presence of increasing concentrations of SB-271046. Br J Pharmacol. 2000 Aug;130(7):1606-12.
    SB 271046 HCl
    Time course profile of anticonvulsant activity in the MEST test and blood concentration of SB-271046 in rats. Br J Pharmacol. 2000 Aug;130(7):1606-12.
    SB 271046 HCl
    Relationship between SB-271046 blood concentration and seizure threshold. Br J Pharmacol. 2000 Aug;130(7):1606-12.


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