Medetomidine

SKU: orb1909168

Description

Medetomidine (MPV785 free base) is a potent, orally active α2-adrenoceptor agonist (Ki=1.08 nM) with sedative and analgesic properties. It is a valuable research tool for in vivo anesthetic studies in veterinary models and for in vitro investigations of adrenergic receptor signaling and vasoconstriction mechanisms.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 86347-14-0
• MW: 200.28
• Formula: C₁₃H₁₆N₂
• SMILES: C(C)(C1=C(C)C(C)=CC=C1)C2=CN=CN2
• Target: Others
• Solubility: H2O:< 1 mg/mL (insoluble);DMSO:200 mg/mL (998.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (24.97 mM)

Bioactivity

• Target IC50:
  α2-adrenoceptor:1.08 nM (Ki)|α1-adrenoceptor:1750 nM (Ki)
• In Vivo:
  In rat models, Medetomidine exhibits dose-dependent sedative and analgesic effects. High doses (>100 μg/kg) can result in loss of righting reflex and hypothermia. In anesthetized rats, Medetomidine induces transient hypotension and bradycardia. In denervated rats, it shows potent vasopressor activity (PD₅₀ = 1.7 μg/kg) and suppresses sympathetic nerve activity (ID₅₀ = 1.6 μg/kg).
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• In Vitro:
  Both enantiomers of Medetomidine (dex- and levoMedetomidine) inhibit cytochrome P450-dependent drug-metabolizing activity in rat and human liver microsomes(100 μg/kg ;from 17 to 23 min.; both enantiomers). In Rainbow trout(i.p. injection;<5 μmol/kg) or water exposure (<50 nM) caused a 2–7 fold increase in hepatic EROD activity.
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Storage & Handling

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

Alternative Names

MPV785 free base, Medetomidine

Compound Identifiers

PubChem CID

68602