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| | Metoclopramide-d3 Basic information |
| | Metoclopramide-d3 Chemical Properties |
| Melting point | 143-148°C | | storage temp. | -20°C Freezer | | solubility | Chloroform (Slightly), Methanol (Slightly) | | form | Solid | | color | White |
| | Metoclopramide-d3 Usage And Synthesis |
| Description | Metoclopramide-d3 is intended for use as an internal standard for the quantification of metoclopramide by GC- or LC-MS. Metoclopramide is an orally bioavailable serotonin (5-HT) receptor 5-HT3 antagonist with Ki and IC50 values of 995 and 308 nM, respectively, in rat cortical membranes. It is also a dopamine D2 receptor antagonist (IC50 = 483 nM in rat brain synaptic membranes). Oral administration of metoclopramide inhibits emesis induced by cisplatin and apomorphine in ferrets and dogs with ED50 values of 6.17 and 0.45 mg/kg, respectively. Metoclopramide reversibly inhibits human acetylcholinesterase (AChE) isolated from the caudate nucleus (Kis = 9.3 and 82 μM for competitive and non-competitive inhibition, respectively). Formulations containing metoclopramide have been used as anti-emetic and antipsychotic agents. | | Chemical Properties | White Crystalline Solid | | Uses | Labelled dopamine D2 receptor antagonist. A labelled substituted benzamide with neuroleptic activity. Antiemetic. | | References | [1] Y. HIROKAWA. 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.[J]. Chemical & pharmaceutical bulletin, 2002, 110 1: 941-959. DOI: 10.1248/cpb.50.941
[2] JRG-MICHAEL CHEMNITIUS . INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF METOCLOPRAMIDE: REVERSIBLE INHIBITION OF CHOLINESTERASES FROM HUMAN CENTRAL NERVOUS SYSTEM AND BLOOD[J]. Pharmacological research, 1996, 34 1: Pages 65-72. DOI: 10.1006/phrs.1996.9999
[3] R. D. YOUSSEFYEH. Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides[J]. Journal of Medicinal Chemistry, 1992, 35 5: 895-903. DOI: 10.1021/jm00083a014
[4] C A ALTAR. Dopamine neurochemical profile of atypical antipsychotics resembles that of D-1 antagonists.[J]. Naunyn-Schmiedeberg’s archives of pharmacology, 1988, 338 2: 162-168. DOI: 10.1007/bf00174864 |
| | Metoclopramide-d3 Preparation Products And Raw materials |
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