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Submit ReviewSarpogrelate hydrochloride
Description: Selective 5-HT2A antagonist
Alternative Names: MCI 9042
Chemical Name: Succinic acid mono-(1-dimethylaminomethyl-2-(2-[2-(3-methoxyphenyl)ethyl]phenoxy)ethyl) ester hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for Sarpogrelate hydrochloride
Sarpogrelate hydrochloride is a selective 5-HT2A receptor antagonist (pKi values are 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively). Displays selectivity over 5-HT1, 5-HT3, 5-HT4 H1, H2, M3, α1-adrenergic, α2-adrenergic and β-adrenergic receptors. Displays cardioprotective activity in vivo.
Technical Data for Sarpogrelate hydrochloride
| M. Wt | 465.97 |
| Formula | C24H31NO6.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 135159-51-2 |
| PubChem ID | 444005 |
| InChI Key | POQBIDFFYCYHOB-UHFFFAOYSA-N |
| Smiles | O=C(CCC(O)=O)OC(CN(C)C)COC1=CC=CC=C1CCC2=CC(OC)=CC=C2.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 Sarpogrelate hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 11.65 | 25 | |
| DMSO | 46.6 | 100 |
Preparing Stock Solutions for Sarpogrelate hydrochloride
The following data is based on the product molecular weight 465.97. 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 | 2.15 mL | 10.73 mL | 21.46 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.29 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets for Sarpogrelate hydrochloride
References for Sarpogrelate hydrochloride
References are publications that support the biological activity of the product.
Rashid et al (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci. 73 193 PMID: 12738034
Brasil et al (2002) Blockade of 5-HT(2A) receptors by sarpogrelate protects the heart against myocardial infarction in rats. J.Cardiovasc.Pharmacol.Ther. 7 53 PMID: 12000979
Nishiyama (2009) Acute effects of sarpogrelate, a 5-HT2A receptor antagonist on cytokine production in endotoxin shock model of rats. Eur.J.Pharmacol. 614 122 PMID: 19318092
If you know of a relevant reference for Sarpogrelate hydrochloride, please let us know.
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Citations for Sarpogrelate hydrochloride
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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.