Sarpogrelate hydrochloride

Mfr.No.	T4978
Description	Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.
Alternative Names	MCI-9042
Molecular Formula	C24H32ClNO6
Signaling Pathways	GPCR/G Protein, Neuroscience
Smiles	Cl.COc1cccc(CCc2ccccc2OCC(CN(C)C)OC(=O)CCC(O)=O)c1
Cas Number	135159-51-2
Molecular Weight	465.97
Target	5-HT Receptor

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BHB20429472	T4978	1 mL	$47	Add to Cart
BHB20429472	T4978	5 mg	$41	Add to Cart
BHB20429472	T4978	10 mg	$66	Add to Cart
BHB20429472	T4978	25 mg	$122	Add to Cart
BHB20429472	T4978	50 mg	$195	Add to Cart
BHB20429472	T4978	100 mg	$288	Add to Cart
BHB20429472	T4978	500 mg	$688	Add to Cart