Sarpogrelate hydrochloride (Synonyms: MCI-9042) |
| Catalog No.GC16202 |
Inhibidor del receptor 5-HT2A
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 135159-51-2
Sample solution is provided at 25 µL, 10mM.
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Ki: 8.39 nM
Sarpogrelate (MCI-9042) was shown to have the same affinity as ritanserin for 5-HT2A receptors, [1].
The blockade of 5-HT2A receptors can inhibit thrombus formation suppresses platelet aggregation and inhibits vascular smooth muscle cell proliferation [2].
In vitro: The major metabolite (R,S)-M-1, and M-1 enantiomers of sarpogrelate specifically blocked 5-HT at 5-HT2A receptors. The stereochemical configuration of the ligands does not obviously play a key role at binding to the 5-HT2A receptor [2].
In vivo: PAD patients were divided into two groups. One group treated with 100 mg sarpogrelate in oral 3 times one day for 12 weeks (n = 10), while the other group who remained on conventional therapy as control group (n = 11). Forearm blood flow (FBF) and leg blood flow (LBF) responses to reactive hyperemia (RH) and sublingual administration of nitroglycerin (NTG) were measured by strain-gauge plethysmography. After twelve weeks of its administration, FBF and LBF responses during RH exhibited significant increases from 13.2 6 1.7 to 18.1 6 2.2 mL/min every 100 mL tissue (P , 0.01) and from 8.2 6 0.9 to 14.2 6 2.1 mL/min every 100 mL tissue (P , 0.05), respectively. Augmentation of FBF and LBF induced by sarpogrelate responses to RH was maintained at 24 weeks. The control group had no change observed in at each follow-up time point. The changes in FBF and LBF after sublingual NTG were similar during follow-up periods in the two groups. These findings suggest that longterm oral administration of sarpogrelate improves vascular function in patients with PAD [3].
Clinical trial: Clinical study has been conducted.
References:
[1] Nishio H1, Inoue A, Nakata Y. Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Arch Int Pharmacodyn Ther. 1996 Mar-Apr;331(2):189-202.
[2] Pertz H1, Elz S. In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery. J Pharm Pharmacol. 1995 Apr;47(4):310-6.
[3] Miyazaki M1, Higashi Y, Goto C, Chayama K, Yoshizumi M, Sanada H, Orihashi K, Sueda T. Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease. J Cardiovasc Pharmacol. 2007 Apr;49(4):221-7.
| Cas No. | 135159-51-2 | SDF | |
| Sinónimos | MCI-9042 | ||
| Canonical SMILES | O=C(CCC(O)=O)OC(CN(C)C)COC1=CC=CC=C1CCC2=CC(OC)=CC=C2.Cl | ||
| Formula | C24H32ClNO6 | M.Wt | 465.97 |
| Solubility | ≥ 23.3mg/mL in DMSO | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1461 mL | 10.7303 mL | 21.4606 mL |
| 5 mM | 0.4292 mL | 2.1461 mL | 4.2921 mL |
| 10 mM | 0.2146 mL | 1.073 mL | 2.1461 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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