Sarpogrelate-d4 (hydrochloride)

Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride) . Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3][4].

Product Specifications

Product Name Alternative

MCI-9042-d4

UNSPSC

12352005

Target

5-HT Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Neuronal Signaling; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Smiles

[2H]C(C(OC(COC1=CC=CC=C1CCC2=CC=CC(OC)=C2)CN(C)C)=O)([2H])C([2H])([2H])C(O)=O.Cl

Molecular Formula

C24H28D4ClNO6

Molecular Weight

469.99

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]Rashid M, et al. 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. 2003 May 30;73 (2) :193-207.|[3]Maruyama K, et al. MCI-9042: high affinity for serotonergic receptors as assessed by radioligand binding assay. J Pharmacobiodyn. 1991 Apr;14 (4) :177-81.