Home Neuronal Signaling 5-HT Receptor antagonist Sarpogrelate hydrochloride

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Sarpogrelate hydrochloride 5-HT Receptor antagonist

Cat.No.S3706

Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.
Sarpogrelate hydrochloride 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 465.97

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Chemical Information, Storage & Stability

Molecular Weight 465.97 Formula

C24H31NO6.HCl

 Storage (From the date of receipt)
CAS No. 135159-51-2 Download SDF Storage of Stock Solutions

Synonyms MCI-9042 Smiles CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O.Cl

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (199.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 93 mg/mL

Ethanol : 31 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
5-HT2A [1]
(Cell-free)
0.2 nM(Kd)
5-HT2C [1]
(Cell-free)
1.1 nM(Kd)
5-HT2B [1]
(Cell-free)
2.1 nM(Ki)
5-HT2B [1]
(Cell-free)
2.1 nM(Kd)
In vitro
Sarpogrelate inhibits thrombus formation, lowers platelet aggregation, inhibits both serotonin-induced coronary artery spasm and contraction in porcine model as well as vascular smooth muscle cell proliferation. Sarpogrelate exibit specificity toward 5-HT2 receptors, since it has lack of significant 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 antagonistic activity[1]. Sarpogrelate specifically inhibited the serotonin-induced cytokine trigger but did not influence platelet-derived growth factor–, endothelin–, or angiotensin II–induced cell proliferation. Sarpogrelate inhibited the serotonin-induced increase in intracellular free ionized calcium concentration, prevented mitogen-activated protein kinase activation, and down-regulated expression of the protooncogenes c-fos and c-jun. Sarpogrelate acted at the G1 phase of the cell cycle[2].
In vivo
Sarpogrelate can fully protect albino BALB/c retinas, both structurally and functionally, from light-induced retinopathy[3]. It is used clinically for the treatment of vascular inflammation and atherosclerosis. Sarpogrelate mitigates albuminuria in diabetic nephropathy by hindering glomerular platelet activation. Sarpogrelate ameliorates diabetic nephropathy not only by suppressing macrophage infiltration, but also by anti-inflammatory and anti-fibrotic effects[4].
References

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