Idazoxan (hydrochloride)

Idazoxan is an antagonist of alpha2-adrenergic receptors (alpha2-ARs) and imidazoline I1 and I2 receptors (IC50s = 69, 66, and 61 nM, respectively). It selectively binds to alpha2A- and alpha2C-ARs over alpha2B-ARs (Kds = 67, 69, and 407 nM, respectively), as well as alpha2-ARs over alpha1-ARs (IC50s = 0. and 4,000 µM, respectively). Idazoxan (0.1-5 mg/kg) increases mean arterial pressure and decreases heart rate in rabbits. It reverses the anti-hyperalgesic activity of 2-BFI (Cay-42338) in rat models of inflammatory and neuropathic pain and the antidepressant-like activity of 2-BFI in the tail suspension test in mice. Idazoxan (7. and 10 mg/kg) reduces L-DOPA-induced dyskinesia in a cynomolgus monkey model of MPTP-induced Parkinson's disease.. Solulibility: DMSO: Soluble: = 10 mg/ml: Ethanol: Sparingly soluble: 1-10 mg/ml, PBS (pH 7.2): Soluble: = 10 mg/ml.