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Metopimazine-d6

Metopimazine-d6 (EXP999-d6; RP9965-d6) is the deuterium labeled Metopimazine. Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks[1][2][3][4].

Product Specifications

CAS Number

1215315-86-8

Product Name Alternative

EXP999-d6; RP9965-d6

UNSPSC

12352005

Target

Dopamine Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Neuronal Signaling; Others

Field of Research

Neurological Disease

Solubility

10 mM in DMSO

Smiles

C(C(C(N1CCC(C(N)=O)CC1)([2H])[2H])([2H])[2H])(N2C=3C(SC=4C2=CC=CC4)=CC=C(S(C)(=O)=O)C3)([2H])[2H]

Molecular Formula

C22H21D6N3O3S2

Molecular Weight

451.64

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Victoire Roussel, et al. Estimating the excess of inappropriate prescriptions of anti-dopaminergic anti-emetics during acute gastroenteritis epidemics in France. Pharmacoepidemiol Drug Saf. 2013 Oct;22 (10) :1080-5.|[3]Mozgova O, et al. A new spectrophotometric method for the quantitative determination of Metopimazine based on the absorbance of its sulfoxide[J]. Chemical Papers, 2024, 78 (11) : 6585-6591.|[4]Jolliet P, et al. Evidence of lowest brain penetration of an antiemetic drug, metopimazine, compared to domperidone, metoclopramide and chlorpromazine, using an in vitro model of the blood-brain barrier. Pharmacol Res. 2007 Jul;56 (1) :11-7.

Shipping Conditions

Room temperature

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Isoform

D2 Receptor

Available Sizes

Frequently Asked Questions

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