Biological Activity
Potent 5-HT2B/2C receptor antagonist (pKi values are 8.3, 7.66 and 6.77 for 5-HT2B, 5-HT2C and 5-HT2A respectively). Increases wakefulness and motor activity in rats. Orally active.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
M. Wt | 337.81 |
Formula | C19H16ClN3O |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 162100-15-4 |
PubChem ID | 10449757 |
InChI Key | HOVMHIRTZYQSKM-UHFFFAOYSA-N |
Smiles | O=C(NC3=CC=CC4=C3C=CC=N4)N(CC2)C1=C2C=C(C)C(Cl)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 33.78 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 337.81. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.96 mL | 14.8 mL | 29.6 mL |
5 mM | 0.59 mL | 2.96 mL | 5.92 mL |
10 mM | 0.3 mL | 1.48 mL | 2.96 mL |
50 mM | 0.06 mL | 0.3 mL | 0.59 mL |
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References
References are publications that support the products' biological activity.
Kennett et al (1998) Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated. Neuropharmacology 37 1603 PMID: 9886683
Reavill et al (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br.J.Pharmacol. 126 572 PMID: 10188965
Kantor et al (2004) Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. Br.J.Pharmacol. 142 1332 PMID: 15265808
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