Idazoxan

Idazoxan
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • (±)-2-(2,3-dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC11H12N2O2
Molar mass204.229 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • C1CN=C(N1)C2COC3=CC=CC=C3O2
  • InChI=1S/C11H12N2O2/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) ☒N
  • Key:HPMRFMKYPGXPEP-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Idazoxan (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.[1][2][3][4] Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its α2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia.

  1. ^ Bousquet P, Bruban V, Schann S, Greney H, Ehrhardt JD, Dontenwill M, Feldman J (June 1999). "Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs". Annals of the New York Academy of Sciences. 881 (1): 272–8. Bibcode:1999NYASA.881..272B. doi:10.1111/j.1749-6632.1999.tb09369.x. PMID 10415925. S2CID 38772290.
  2. ^ Clarke RW, Harris J (2002). "RX 821002 as a tool for physiological investigation of alpha(2)-adrenoceptors". CNS Drug Reviews. 8 (2): 177–92. doi:10.1111/j.1527-3458.2002.tb00222.x. PMC 6741674. PMID 12177687.
  3. ^ Yakubu MA, Hamilton CA, Howie CA, Reid JL (1988). "Idazoxan and brain alpha2-adrenoceptor in the rabbit". Brain Research. 436: 289–296. doi:10.1016/0006-8993(88)90402-7. PMID 2848612.
  4. ^ Hamilton CA, Yakubu MA, Jardine E, Reid JL (1991). "Imidazole binding sites in rabbit kidney and forebrain membranes". J Auton Pharmacol. 11 (4): 277–83. doi:10.1111/j.1474-8673.1991.tb00325.x. PMID 1939285.