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| Routes of administration | By mouth |
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| Formula | C11H12N2O2 |
| Molar mass | 204.229 g·mol−1 |
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| Chirality | Racemic mixture |
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Idazoxan (INN) is adrug which is used inscientific research. It acts as both a selectiveα2-adrenergic receptorantagonist, and an antagonist for theimidazoline receptor.[1][2][3][4] Idazoxan has been under investigation as anantidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment inschizophrenia. Due to its α2 receptor antagonism, it is capable of enhancing therapeutic effects ofantipsychotics, possibly by enhancingdopamineneurotransmission in theprefrontal cortex of the brain, a brain area thought to be involved in thepathogenesis of schizophrenia.[citation needed]
Mice treated with idazoxan, which blocks theα2A-adrenergic receptor, behaved similarly to control animals despite still having amyloid-beta plaques in the brain, as a proof-of-concept experiment that dramatically reducedAlzheimer's disease pathology and symptoms in two mouse models, potentially offering an immediate treatment for this devastating disease.[5]
Note that the literature method claims that the old original patented procedure gives a different reaction product formed through a rearrangement.
The reaction of catechol (1) with 2-Chloroacrylonitrile [920-37-6] (2) gives 2-cyano-1,4-benzodioxan [1008-92-0] (3).Pinner reaction with alcoholic hydrogen chloride leads to the iminoether,[11] (4). Treatment withethylenediamine [107-15-3] (5) gives the imidazoline ring affordingIdazoxin (6).
