1216522-89-2

1216522-89-2 structure

Name: Metoclopramide-d3
Chemical Name: 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-(trideuteriomethoxy)benzamide
CAS Number: 1216522-89-2
Molecular Formula: C₁₄H₁₉D₃ClN₃O₂
Molecular Weight: 302.81
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2016-08-13 05:56:04
Modify Date: 2024-01-11 21:01:05
Metoclopramide-d3 is deuterium labeled Metoclopramide. Metoclopramide is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis[1][2].

Name	4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-(trideuteriomethoxy)benzamide
Synonyms	Gastromax-d3 Meclopran-d3 Metoclopramide-d3 Draclamid-d3 Gastrese-d3 Reliveran-d3 Gastrotem-d3 Gastrosil-d3 Clopromate-d3 Gastrobid-d3

Description	Metoclopramide-d3 is deuterium labeled Metoclopramide. Metoclopramide is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis[1][2].
Related Catalog	Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
In Vitro	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Hirokawa Y, et, al. Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist. Chem Pharm Bull (Tokyo). 2002 Jul;50(7):941-59. [3]. Rao AS, et, al. Review article: metoclopramide and tardive dyskinesia. Aliment Pharmacol Ther. 2010 Jan;31(1):11-9. [4]. Edwards CR, et, al. In vivo and in vitro studies on the effect of metoclopramide on aldosterone secretion. Clin Endocrinol (Oxf). 1980 Jul;13(1):45-50. [5]. Bhosale KB, et, al. Dose-dependent response of central dopaminergic systems to metoclopramide in mice. Indian J Exp Biol. 1997 Jun;35(6):618-22. [6]. Gomes RCT, et, al. Effects of metoclopramide on the mouse anterior pituitary during the estrous cycle. Clinics (Sao Paulo). 2011;66(6):1101-4.

Molecular Formula	C₁₄H₁₉D₃ClN₃O₂
Molecular Weight	302.81
Exact Mass	302.15900
PSA	71.08000
LogP	3.15840

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