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Submit ReviewCP 809101 hydrochloride
Description: Potent and selective 5-HT2C agonist
Chemical Name: 2-[(3-Chlorophenyl)methoxy]-6-(1-piperazinyl)pyrazine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for CP 809101 hydrochloride
CP 809101 hydrochloride is a 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.
Compound Libraries for CP 809101 hydrochloride
CP 809101 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CP 809101 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CP 809101 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 6.82 | 20 | |
| DMSO | 34.12 | 100 |
Preparing Stock Solutions for CP 809101 hydrochloride
The following data is based on the product molecular weight 341.24. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for CP 809101 hydrochloride
References for CP 809101 hydrochloride
References are publications that support the biological activity of the product.
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
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Keywords: CP 809101 hydrochloride, CP 809101 hydrochloride supplier, Potent, selective, 5-HT2C, agonists, Serotonin, Receptors, CP809101, hydrochloride, 3041, Tocris Bioscience
5 Citations for CP 809101 hydrochloride
Citations are publications that use Tocris products. Selected citations for CP 809101 hydrochloride include:
Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641
Yamamoto (2017) Loss of GluN2D subunit results in social recognition deficit, social stress, 5-HT2C receptor dysfunction, and anhedonia in mice. Neuropharmacology 112 188 PMID: 27480795
Goda et al (2013) Serotonergic hallucinogens differentially modify gamma and high frequency oscillations in the rat nucleus accumbens. Psychopharmacology (Berl) 228 271 PMID: 23525524
Schulz et al (2012) First and second generation antipsychotics influence hippocampal gamma oscillations by interactions with 5-HT3 and D3 receptors. Br J Pharmacol 167 1480 PMID: 22817643
Austgen et al (2012) 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii. Oncotarget 108 2292 PMID: 22855775
Do you know of a great paper that uses CP 809101 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.