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
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; I2imidazoline receptor agonist; I1imidazoline 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 0.25mg/kg. Idazoxan (0.3 and 2.5mg/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 1mg/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 5.0mg/kg
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| Administration: | Subcutaneous injection; for 1 hour |
| Result: | Potently reversed haloperidol-induced catalepsy with an ED50 of 0.25mg/kg.
|
IC 50
α adrenergic receptor
