An imidazoline receptor agonist
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BU 224 (hydrochloride)

Item No. 42451

Technical Information
Formal Name
2-(4,5-dihydro-1H-imidazol-2-yl)-quinoline, monohydrochloride
CAS Number
205437-64-5
Molecular Formula
C12H11N3 • HCl
Formula Weight
Purity
≥95%
Formulation
A solid
PBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
C1(C2=CC=C(C=CC=C3)C3=N2)=NCCN1.Cl
InChi Code
InChI=1S/C12H11N3.ClH/c1-2-4-10-9(3-1)5-6-11(15-10)12-13-7-8-14-12;/h1-6H,7-8H2,(H,13,14);1H
InChi Key
DDFHQXAQWZWRSQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.

    References & Product Citations
    Product Description References

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

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

    3. Min, J.-W., Peng, B.-W., He, X., et alGender difference in epileptogenic effects of 2-BFI and BU224 in mice. Eur. J. Pharmacol. 718(1-3), 81-86 (2013).

    4. Mirzaei, N., Mota, B.C., Birch, A.M., et alImidazoline 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).