Medetomidine hydrochloride

SKU: orb1300641

Description

Medetomidine hydrochloride is a potent and highly selective α2-adrenoceptor agonist (Ki = 1.08 nM), demonstrating 1620-fold selectivity versus α1-adrenoceptors. It is widely used in research as a sedative and analgesic agent in both in vivo animal models and in vitro receptor binding studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 86347-15-1
• MW: 236.74
• Purity: 99.96% (May vary between batches)
• Formula: C₁₃H₁₆N₂·HCl
• SMILES: Cl.CC(c1c[nH]cn1)c1cccc(C)c1C
• Target: Adrenergic Receptor
• Solubility: DMSO:60 mg/mL (253.44 mM);H2O:23.7 mg/mL (100.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.45 mM)

Bioactivity

• Target IC50:
  α2-adrenoceptor:1.08 nM(Ki)|α1-adrenoceptor:1750 nM (Ki)
• In Vivo:
  In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover.
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• In Vitro:
  Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors.
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Storage & Handling

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

Alternative Names

anxiolysis, analgesia, Adrenergic Receptor, AdrenergicReceptor, central nervous system, Beta Receptor, Domitor, Medetomidine, Medetomidine HCl, Medetomidine hydrochloride, Medetomidine Hydrochloride, Inhibitor, inhibit, muscle relaxation, MPV 785, MPV785, MPV-785, sedation, peripheral nervous system, α2-adrenoceptor

Compound Identifiers

PubChem CID

68601