An antagonist of α2-adrenergic and imidazoline I1 and I2 receptors
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Idazoxan (hydrochloride)

Item No. 41310

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(2,3-dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole, monohydrochloride
CAS Number
79944-56-2
Synonyms
  • RX 781094
Molecular Formula
C11H12N2O2 • HCl
Formula Weight
240.7
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Soluble: ≥ 10 mg/ml
SMILES
C1(OCC(C2=NCCN2)O3)=C3C=CC=C1.Cl
InChi Code
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
InChi Key
MYUBYOVCLMEAOH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $60

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    10 mg

    $102

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    25 mg

    $179

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    Product Description

    Idazoxan is an antagonist of α2-adrenergic receptors (α2-ARs) and imidazoline I1 and I2 receptors (IC50s = 69, 66, and 61 nM, respectively).1 It selectively binds to α2A- and α2C-ARs over α2B-ARs (Kds = 67, 69, and 407 nM, respectively), as well as α2-ARs over α1-ARs (IC50s = 0.7 and 4,000 µM, respectively).2,3 Idazoxan (0.1-5 mg/kg) increases mean arterial pressure and decreases heart rate in rabbits.3 It reverses the anti-hyperalgesic activity of 2-BFI (Item No. 42338) in rat models of inflammatory and neuropathic pain and the antidepressant-like activity of 2-BFI in the tail suspension test in mice.4,5 Idazoxan (7.5 and 10 mg/kg) reduces L-DOPA-induced dyskinesia in a cynomolgus monkey model of MPTP-induced Parkinson’s disease.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Flamez, A., De Backer, J.P., Czerwiec, E., et al. Pharmacological characterization of I1 and I2 imidazoline receptors in human striatum. Neurochem. Int. 30(1), 25-29 (1997).

    2. Proudman, R.G.W., Pupo, A.S., and Baker, J.G. The affinity and selectivity of α-adrenoceptor antagonists, antidepressants, and antipsychotics for the human α1A, α1B, and α1D-adrenoceptors. Pharmacol. Res. Perspect. 8(4), e00602 (2020).

    3. Hannah, J.A.M., Hamilton, C.A., and Reid, J.L. RX781094, a new potent α2 adrenoceptor antagonist. In vivo and in vitro studies in the rabbit. Naunyn Schmiedebergs Arch. Pharmacol. 322(3), 221-227 (1983).

    4. Li, J.-X., Thorn, D.A., Qiu, Y., et al. Antihyperalgesic effects of imidazoline I2 receptor ligands in rat models of inflammatory and neuropathic pain. Br. J. Pharmacol. 171(6), 1580-1590 (2014).

    5. Tonello, R., Villarinho, J.G., da Silva Sant'Anna, G., et al. The potential antidepressant-like effect of imidazoline I2 ligand 2-BFI in mice. Prog. Neuropsychopharmacol. Biol. Psychiatry 37(1), 15-21 (2012).

    6. Grondin, R., Tahar, A.H., Doan, V.D., et al. Noradrenoceptor antagonism with idazoxan improves L-dopa-induced dyskinesias in MPTP monkeys. Naunyn Schmiedebergs Arch. Pharmacol. 361(2), 181-186 (2000).