SB 258741 hydrochloride
SB 258741 hydrochloride is a specific 5-HT7 receptor antagonist and can be used for the research of schizophrenia.
For research use only. We do not sell to patients.
- Formula: C19H31ClN2O2S
- Molecular Weight:386.98
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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5-HT7 Receptor |
In Vitro
SB-258741 behaves as a partial inverse agonist, the antagonist potency (apparent pKB) is 8.47[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats, 250 –300 g in the phencyclidine (PCP)-disrupted prepulse inhibition (PPI) and PCP-disrupted social interaction (SIT) paradigm, 200 – 250 g in the catalepsy, motility, and D-amphetamine hyperactivity paradigms[1]
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Dosage:0.56, 2.3, 4.6 and 9.1 mg/kg
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Administration:Subcutaneous injection, once or daily for 3 days (social interaction test)
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Result:Reversed hyperactivity induced by D-amphet-amine over 0.56 mg/kg, and reduced motility at 4.6 and 9.1 mg/kg.
Did not reverse D-Amphetamine-disrupted PPI, but enhanced PCP-disrupted PPI.
Reduced PCP (2 mg/kg)-induced hyperactivity.
Chemical Information
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Molecular Weight 386.98
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Formula C19H31ClN2O2S
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SMILES
O=S(N1[C@@H](CCN2CCC(C)CC2)CCC1)(C3=CC=CC(C)=C3)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Pouzet B, et al. Effects of the 5-HT(7) receptor antagonist SB-258741 in animal models for schizophrenia. Pharmacol Biochem Behav. 2002 Apr;71(4):655-65. [Content Brief]
[2]. Mahé C, et al. Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors. Eur J Pharmacol. 2004 Jul 14;495(2-3):97-102. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)