Metoclopramide

SKU: orb1225193

Description

A potent dopamine D2 receptor antagonist with Ki of 28 nM; also is a mixed 5-HT3 receptor antagonist/5-HT4 receptor agonist; commonly used to treat nausea and vomiting caused by chemotherapy.Chemotherapeutic Agents Phase 2 Discontinued(In Vitro):Metoclopramide (0.01-10 μM) stimulates aldosterone release in isolated perfused rat zona glomerulosa cells.Metoclopramide 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.(In Vivo):Metoclopramide (6.7 μg/g; s.c. daily for 50 days) significantly increases the number and the volume of lactotroph cells of the pituitary gland during all phases of the estrous cycle.Metoclopramide (5-40 mg/kg; i.p.) induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice.Metoclopramide (1.25-2.5 mg/kg; i.p.) induces stereotyped cage climbing behaviour in mice.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 364-62-5
• MW: 299.7964
• Purity: >98% (HPLC)
• Formula: C₁₄H₂₂ClN₃O₂
• SMILES: O=C(NCCN(CC)CC)C1=CC(Cl)=C(N)C=C1OC
• Target: Dopamine Receptor
• Solubility: DMSO: ≥ 41 mg/mL

Bioactivity

• In Vivo:
  Metoclopramide (6.7 μg/g; s. c. daily for 50 days) significantly increases the number and the volume of lactotroph cells of the pituitary gland during all phases of the estrous cycle. Metoclopramide (5-40 mg/kg; i.p.) induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice. Metoclopramide (1.25-2.5 mg/kg; i.p.) induces stereotyped cage climbing behaviour in mice. Animal model: Adult, virgin female mice of the Swiss EPM-1 strain. Dosage: 6.7 μg/g. Administration: S. c. daily for 50 days. Result: Increased the number but also stimulated the metabolic activity of lactotrophs.
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• In Vitro:
  Metoclopramide (0.01-10 μM) stimulates aldosterone release in isolated perfused rat zona glomerulosa cells. Metoclopramide 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Metoclopramide, Afipran, Maxolon, Reglan, Maxeran, Cerucal

Quick Database Links

Gene Symbol

Dopamine Receptor