IDAZOXAN HYDROCHLORIDE
IDAZOXAN HYDROCHLORIDE Basic information
- Product Name:
- IDAZOXAN HYDROCHLORIDE
- Synonyms:
-
- (+/-)-Idazoxan Monohydrochloride
- 2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-iMidazole Hydrochloride
- RX 781094A
- 2-(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-iMidazole hydrochloride
- IDAZOXAN HYDROCHLORIDE
- 2-(1,4-BENZODIOXAN-2-YL)-2-IMIDAZOLINE HYDROCHLORIDE
- IdazoxanHCl
- RX 781094, (±)-2-[1,4-Benzodioxan-2-yl]-2-imidazoline hydrochloride
- CAS:
- 79944-56-2
- MF:
- C11H13ClN2O2
- MW:
- 240.69
- Product Categories:
-
- Adrenoceptor
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 79944-56-2.mol
IDAZOXAN HYDROCHLORIDE 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
MSDS
- Language:English Provider:SigmaAldrich
IDAZOXAN HYDROCHLORIDE Usage And Synthesis
Chemical Properties
mp 207-209°C
Uses
Idazoxan hydrochloride has been used to study the efficacy of antidepressant treatments that interact with multiple neurotransmitter systems.
Uses
Antiparkinsonian;Alpha2 agonist
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.
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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