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BU 224 is an agonist of the imidazoline I1 and -I2 receptors.1 It selectively binds to imidazoline I1 and -I2 receptors over a2-adrenergic receptors (a2-ARs; IC50s = 0.034, 0.026, and 15 µM, respectively). BU 224 (10 and 17.8 mg/kg) reduces complete Freund’s adjuvant-induced thermal and mechanical hyperalgesia in rats.2 It decreases the latency to seizure onset and increases the percentage of animals with grade V seizures to a greater extent in female than male mice.3 BU 224 (5 mg/kg) reverses cognitive deficits in the 5XFAD transgenic mouse model of Alzheimer’s disease.4
WARNING This product is not for human or veterinary use.
1. Pharmacological characterization of I1 and I2 imidazoline receptors in human striatum. Neurochem. Int. 30(1), 25-29 (1997).
2. Antihyperalgesic effects of imidazoline I2 receptor ligands in rat models of inflammatory and neuropathic pain. Br. J. Pharmacol. 171(6), 1580-1590 (2014).
3. Gender difference in epileptogenic effects of 2-
4. Imidazoline ligand BU224 reverses cognitive deficits, reduces microgliosis and enhances synaptic connectivity in a mouse model of Alzheimer’s disease. Br. J. Pharmacol. 178(3), 654-671 (2021).