Medetomidine

SKU: orb1909168

Description

Medetomidine (MPV785 free base) is a selective and orally available α2-adrenoceptor agonist, Ki=1.08 nM, with sedative and analgesic effects and vasoconstrictive hypoxic side effects, and is commonly used in small animal anesthesia.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 86347-14-0
• MW: 200.28
• Purity: 99.88%
• Formula: C₁₃H₁₆N₂
• SMILES: N1=CNC(=C1)C(C=2C=CC=C(C2C)C)C
• Target: Adrenergic Receptor
• 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 hypothermi. 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.
• In Vitro:
  Both enantiomers of Medetomidine (dex- and levoMedetomidine) inhibit cytochrome P450-dependent drug-metabolizing activity in rat and human liver microsome (100 μg/kg ;from 17 to 23 min.; both enantiomers. In Rainbow trout(i.p. injection < μM L/kg) or water exposure < 0 nM) caused a 2–7 fold increase in hepatic EROD activit.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

MPV785 free base, Medetomidine

Compound Identifiers

PubChem CID

68602