Sarpogrelate hydrochloride

Catalog #: 3739 Datasheet / COA / SDS

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Sarpogrelate hydrochloride | CAS No. 135159-51-2 | 5-HT2A Receptor Antagonists

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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%

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Biological Activity

Sarpogrelate hydrochloride is a selective 5-HT_2A receptor antagonist (pK_i values are 8.52, 7.43 and 6.57 for 5-HT_2A, 5-HT_2C and 5-HT_2B 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

M.Wt:

465.97

Formula:

C₂₄H₃₁NO₆.HCl

Solubility:

Soluble to 25 mM in water and to 100 mM in DMSO

Purity:

≥99%

Storage:

Desiccate at RT

CAS No:

135159-51-2

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.

Background References

Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT₂ antagonist, to human 5-HT_2A, 5-HT_2B and 5-HT_2C receptor subtypes by molecular modeling.
Rashid et al.
Life Sci., 2003;73:193
Blockade of 5-HT(2A) receptors by sarpogrelate protects the heart against myocardial infarction in rats.
Brasil et al.
J.Cardiovasc.Pharmacol.Ther., 2002;7:53
Acute effects of sarpogrelate, a 5-HT_2A receptor antagonist on cytokine production in endotoxin shock model of rats.
Nishiyama
Eur.J.Pharmacol., 2009;614:122

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