Metoclopramide hydrochloride 

Metoclopramide hydrochloride is a potent and orally active antagonist of 5-HT₃ and dopamine D2 receptor, with IC₅₀s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis^[1][2].

Metoclopramide (0.01-10 μM) hydrochloride stimulates aldosterone release in isolated perfused rat zona glomerulosa cells^[3].
Metoclopramide hydrochloride 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.

Metoclopramide (6.7 μg/g; s.c. daily for 50 days) hydrochloride 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 induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice^[5].
Metoclopramide (1.25-2.5 mg/kg; i.p.) hydrochloride induces stereotyped cage climbing behaviour in mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

336.26

C₁₄H₂₃Cl₂N₃O₂

7232-21-5

Solid

White to off-white

O=C(NCCN(CC)CC)C1=CC(Cl)=C(N)C=C1OC.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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]