ChemicalBook CAS DataBase List 79944-56-2

79944-56-2

Name	IDAZOXAN HYDROCHLORIDE
CAS	79944-56-2
Molecular Formula	C11H13ClN2O2
MDL Number	MFCD00069293
Molecular Weight	240.69
MOL File	79944-56-2.mol

Chemical Properties

Melting point	207-208°
storage temp.	Store at RT
solubility	H₂O: 300 mg/mL
form	Powder
color	White to off-white
Water Solubility	Soluble to 100 mM in water
Stability:	Hygroscopic
InChI	InChI=1S/C11H12N2O2.ClH/c1-2-4-9-8(3-1)14-7-10(15-9)11-12-5-6-13-11;/h1-4,10H,5-7H2,(H,12,13);1H
InChIKey	MYUBYOVCLMEAOH-UHFFFAOYSA-N
SMILES	C1(COC2C=CC=CC=2O1)C1=NCCN1.Cl

Safety Data

Hazard Codes	Xn
Risk Statements	22 less more
Safety Statements	7 less more
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
Storage Class	6.1C - Combustible, acute toxic Cat.3 toxic compounds or compounds which causing chronic effects
Hazard Classifications	Acute Tox. 3 Oral

Hazard Information

Chemical Properties

mp 207-209°C

Uses

An α-adrenoceptor antagonist; in rat brain Idazoxan is a pure antagonist and it has a selectivity for α2- over α1-receptors markedly superior to Piperoxane, Yohimbine, or Rauwolscine. Antiparkinsonian.

Uses

Antiparkinsonian;Alpha2 agonist

Biological Activity

α 2 -adrenoceptor antagonist, and I 2 ligand, selective over I 1 sites (pK i values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I 1 , I 2 , α 2A , α 2B , and α 2C receptors respectively).

Biochem/physiol Actions

α2-adrenoceptor antagonist; I2?imidazoline receptor agonist; I1?imidazoline receptor antagonist. Idazoxan can antagonize various behaviors generated by ethanol in a preclinical setting. It possesses neuroprotective activity against spinal cord injury, resulted due to experimental autoimmune encephalomyelitis (EAE) in mouse, an animal modal of multiple sclerosis (MS).

in vivo

Idazoxan (0.16-5 mg/kg; subcutaneous injection; for 1 hour; male CD-COBS rats) treatment potently reverses haloperidol-induced catalepsy with an ED₅₀ of 0.25?mg/kg. Idazoxan (0.3 and 2.5?mg/kg) has no effect on extracellular DA and do not modify the rise of extracellular DA induced by haloperidol^[1].

Animal Model:	Male CD-COBS rats injected with 1?mg/kg haloperidol^[1]
Dosage:	0.16 mg/kg, 0.31 mg/kg, 0.63 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5.0?mg/kg
Administration:	Subcutaneous injection; for 1 hour
Result:	Potently reversed haloperidol-induced catalepsy with an ED₅₀ of 0.25?mg/kg.

IC 50

α adrenergic receptor

Spectrum Detail

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