Biological Activity
Potent and selective 5-HT2C receptor agonist (pEC50 values are 9.96, 7.19 and 6.81 for human 5-HT2C, 5-HT2B and 5-HT2A receptors respectively). Displays antipsychotic activity; suppresses condition avoidance responding (CAR) and inhibits PCP and amphetamine-stimulated hyperactivity in rats following subcutaneous administration.
Technical Data
| M. Wt | 341.24 |
| Formula | C15H17N4OCl.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1215721-40-6 |
| PubChem ID | 56972220 |
| InChI Key | NMUNRTCTDLORDR-UHFFFAOYSA-N |
| Smiles | ClC1=CC(COC2=NC(N3CCNCC3)=CN=C2)=CC=C1.Cl |
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 | 34.12 | 100 | |
| water | 6.82 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 341.24. 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 | 2.93 mL | 14.65 mL | 29.3 mL |
| 5 mM | 0.59 mL | 2.93 mL | 5.86 mL |
| 10 mM | 0.29 mL | 1.47 mL | 2.93 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.59 mL |
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References
References are publications that support the products' biological activity.
Siuciak et al (2007) CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity. Neuropharmacology 52 279 PMID: 16949622
Kalgutkar et al (2007) Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation. Drug Metab.Dispos. 35 848 PMID: 17344339
Jensen et al (2013) Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT2A/5-HT2C receptor agonists with pro-cognitive J.Med.Chem 56 1211 PMID: 23301527
Keywords: CP 809101 hydrochloride, supplier, Potent, selective, 5-HT2C, agonists, Serotonin, Receptors, CP809101, hydrochloride, 5-HT2C, Receptors, 5-HT2C, Receptors, Tocris Bioscience
