| Identification | Back Directory | [Name]
METOCLOPRAMIDE-D3 | [CAS]
1216522-89-2 | [Synonyms]
METOCLOPRAMIDE-D3
[2H3]-Metoclopramide
4-AMino-5-chloro-N-[2-(diethylaMino)ethyl]-2-(Methoxy-d3)benzaMide
4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-(trideuteriomethoxy)benzamide
Metoclopramide D3Q: What is
Metoclopramide D3 Q: What is the CAS Number of
Metoclopramide D3 Q: What is the storage condition of
Metoclopramide D3 Q: What are the applications of
Metoclopramide D3 | [Molecular Formula]
C14H19ClD3N3O2 | [MDL Number]
MFCD08063630 | [MOL File]
1216522-89-2.mol | [Molecular Weight]
302.81 |
| Chemical Properties | Back Directory | [Melting point ]
143-148°C | [storage temp. ]
-20°C Freezer | [solubility ]
Chloroform (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
White |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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] J?RG-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 |
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TOSUN PHARM
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Energy Chemical
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