Metoclopramide (hydrochloride hydrate)

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]. In Vitro: 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].