| Bioactivity | Metoclopramide hydrochloride hydrate is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis[1][2]. |
| Invitro | Metoclopramide (0.01-10 μM) hydrochloride hydrate stimulates aldosterone release in isolated perfused rat zona glomerulosa cells[3].Metoclopramide hydrochloride 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]. |
| In Vivo | Metoclopramide (6.7 µg/g; s.c. daily for 50 days) hydrochloride hydrate significantly increases the number and the volume of lactotroph cells of the pituitary gland during all phases of the estrous cycle[4].Metoclopramide (5-40 mg/kg; i.p.) hydrochloride hydrate induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice[5].Metoclopramide (1.25-2.5 mg/kg; i.p.) hydrochloride hydrate induces stereotyped cage climbing behaviour in mice[5]. Animal Model: |
| Name | Metoclopramide hydrochloride hydrate |
| CAS | 54143-57-6 |
| Formula | C14H25Cl2N3O3 |
| Molar Mass | 354.27 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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 ( [2]. Rao AS, et, al. Review article: metoclopramide and tardive dyskinesia. Aliment Pharmacol Ther. 2010 Jan;31(1):11-9. [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. [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. [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. |