Identification | Back Directory | [Name]
IDAZOXAN HYDROCHLORIDE | [CAS]
79944-56-2 | [Synonyms]
RX 781094A IdazoxanHCl IDAZOXAN HYDROCHLORIDE (+/-)-Idazoxan Monohydrochloride 2-(1,4-BENZODIOXAN-2-YL)-2-IMIDAZOLINE HYDROCHLORIDE RX 781094, (±)-2-[1,4-Benzodioxan-2-yl]-2-imidazoline hydrochloride Idazoxan hydrochloride,2-(1,4-Benzodioxan-2-yl)-2-imidazolinehydrochloride 2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-iMidazole Hydrochloride 2-(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-iMidazole hydrochloride | [Molecular Formula]
C11H13ClN2O2 | [MDL Number]
MFCD00069293 | [MOL File]
79944-56-2.mol | [Molecular Weight]
240.69 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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 |
|
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