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    SB269970 HCl (SB-269970A)
    SB269970 HCl (SB-269970A)

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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 #: V1019
    CAS #: 261901-57-9Purity ≥98%

    Description: SB269970 HCl (SB 269970; GR125743; GR-125743; SB-269970), the hydrochloride salt form of SB-269970, is a novel and potent 5-HT7 receptor antagonist with antianxiety-like effects. In inhibits 5-HT7 with pKi of 8.3, and exhibits >50-fold selectivity for 5-HT7 over other receptors.  

    References: Br J Pharmacol. 2000 Jun;130(3):539-48; Behav Pharmacol. 2008 Mar;19(2):153-9.

    Related CAS#: 201038-74-6 (free base) 

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    Molecular Weight (MW)388.95 
    FormulaC18H28N2O3S.HCl 
    CAS No.261901-57-9 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 11 mg/mL (28.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsSB269970; GR125743; SB 269970; GR125743; GR-125743; SB-269970; SB269970 HCl.


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    In Vitro

    In vitro activity: SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. SB-269970 (0.03 μM, 0.1 μM, 0.3 μM and 1 μM) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no significant alteration in the maximal response to 5-CT. SB-269970 (1 μM) has any effect on 5-HT efflux when superfused alone.


    Kinase Assay: SB269970 is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

    In VivoSB-269970 (10 mg/kg and 30 mg/kg) significantly reduces the effects of amphetamine by 25 and 27%, respectively, and blocks the effects of ketamine by 38% (10 mg/kg) and 30% (30 mg/kg). SB-269970 significantly reduces amphetamine-induced hyperactivity in wild-type mice and is without effects in 5-HT7 knockout mice. Systemic administration of SB-269970 (30 mg/kg) significantly reverses amphetamine disruption of PPI and did not enhance PPI by itself compared to control. SB-269970 significantly reverses the deficits induced by MK-801, but not by scopolamine. SB-269970 normalizes MK-801-induced glutamate but not dopamine release in the cortex. SB-269970 (in one medium dose of 0.5 or 1 mg/kg) exerts a specific antianxiety-like effect in the Vogel drinking test in rats, in the elevated plus-maze test in rats and in the four-plate test in mice. Moreover, SB-269970 (in one medium dose of 5 or 10 mg/kg) reveals antidepressant-like activity in the forced swimming and the tail suspension tests in mice. SB-269970 at doses of 0.3, 1 and 3 μg exhibits an anticonflict effect which is weaker than that of diazepam (40 μg), whereas SB-269970 at doses of 3 and 10 μg had marked anti-immobility action comparable to that of imipramine (0.1 μg).  
    Animal modelC57BL6/J mice 
    Formulation & DosageDissolved in saline; 10 mg/kg, 30 mg/kg; i.p.injection 
    ReferencesBr J Pharmacol. 2000 Jun;130(3):539-48; Behav Pharmacol. 2008 Mar;19(2):153-9. 


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

     
    SB269970 HCl
    Stimulation of adenylyl cyclase activity in human 5-HT7/HEK293 membranes by 5-CT alone and in the presence of SB-269970-A (0.03, 0.1, 0.3 and 1 μM). Br J Pharmacol. 2000 Jun;130(3):539-48.
     
    SB269970 HCl
    Stimulation of adenylyl cyclase activity in guinea-pig hippocampal membranes by 5-CT alone and in the presence of SB-269970-A (0.3 μM). Br J Pharmacol. 2000 Jun;130(3):539-48.
     
    SB269970 HCl
    Effect of SB-269970-A on 5-CT-induced hypothermia in guinea-pigs. Br J Pharmacol. 2000 Jun;130(3):539-48.
     
    SB269970 HCl
    Time course of the effects of SB-269970-A on 5-CT-induced hypothermia in guinea-pigs. Br J Pharmacol. 2000 Jun;130(3):539-48.
     
    SB269970 HCl
    Effect of SB-269970-A on sleep stage distribution during the normal sleep phase. Br J Pharmacol. 2000 Jun;130(3):539-48.


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