Metoclopramide dihydrochloride hydrate
Based on 3 publication(s) in Google Scholar
Metoclopramide dihydrochloride hydrate is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide dihydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
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- CAS No.: 5581-45-3
- Formule: C14H26Cl3N3O3
- Masse moléculaire:390.73
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Metoclopramide dihydrochloride hydrate
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Activité biologique
Description
IC50 & Target
[1]|
5-HT3 Receptor 308 nM (IC50) |
D2 Receptor 483 nM (IC50) |
In Vitro
Metoclopramide (0.01-10 μM) dihydrochloride hydrate stimulates aldosterone release in isolated perfused rat zona glomerulosa cells[3].
Metoclopramide dihydrochloride hydrate results in prokinesis by four mechanisms: inhibition of presynaptic D2 receptors and stimulation of presynaptic excitatory 5-HT4 receptors, thereby allowing acetylcholine (ACh) release from intrinsic cholinergic motor neurons; inhibition of D2 postsynaptic receptors; and antagonism of the presynaptic inhibition of muscarinic receptors, leading to further augmentation of ACh release[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Metoclopramide (5-40 mg/kg; i.p.) dihydrochloride hydrate induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice[5].
Metoclopramide (1.25-2.5 mg/kg; i.p.) dihydrochloride hydrate induces stereotyped cage climbing behaviour in mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult, virgin female mice of the Swiss EPM-1 strain[4]
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Dosage:6.7 µg/g
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Administration:S.c. daily for 50 days
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Result:Increased the number but also stimulated the metabolic activity of lactotrophs.
Chemical Information
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CAS No. 5581-45-3
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Masse moléculaire 390.73
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Formule C14H26Cl3N3O3
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SMILES
O=C(C1=CC(Cl)=C(C=C1OC)N)NCCN(CC)CC.Cl.O.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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ACS Omega
Computational Approaches to Identify Molecules Binding to Mycobacterium tuberculosis KasA. [Abstract]2020 Nov 15;5(46):29935-29942. PMID: 33251429 -
Eur J Drug Metab Pharmacokinet
Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans. [Abstract]2022 Sep;47(5):639-652. PMID: 35733077
Pureté et documentation
Références
[1]. 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. [Content Brief]
[2]. Rao AS, et, al. Review article: metoclopramide and tardive dyskinesia. Aliment Pharmacol Ther. 2010 Jan;31(1):11-9. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]
[5]. Gomes RCT, et, al. Effects of metoclopramide on the mouse anterior pituitary during the estrous cycle. Clinics (Sao Paulo). 2011;66(6):1101-4. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Metoclopramide dihydrochloride hydrate Related Classifications
HY-17382D Related Classifications
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