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BU 224 hydrochloride

Catalog No.GC15700

Antagonist of I2 Imidazoline receptor,potent and selective

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BU 224 hydrochloride Chemical Structure

Cas No.: 205437-64-5

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10mg
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Sample solution is provided at 25 µL, 10mM.

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Background

BU 224 hydrochloride is a selective ligand of the imidazoline I2 receptor with Ki value of 2.1 nM [1].

Imidazoline receptor is the primary receptor for clonidine and other imidazolines. Imidazoline I2 receptor is an allosteric binding site of monoamine oxidase and plays a critical role in neuroprotection and pain modulation.

BU 224 hydrochloride is a selective ligand of the imidazoline I2 receptor. In the rat forced swim test (FST), BU224 significantly inhibited immobility and increased mild swimming. Also, BU224 increased adrenocorticotrophic hormone (ACTH) response to FST and 5-hydroxytryptamine (5-HT) levels in frontal cortex and reduced 5-HT turnover in the hypothalamus and frontal cortex. These results showed the antidepressant-like activity of BU224 [2]. In rats with unilateral lesion of the nigrostriatal tract, BU224 (14 mg/kg) significantly increased ipsiversive rotations [3]. In rats with warm water tail withdrawal procedure, BU224 inhibited the enhancement of morphine and tramadol antinociception induced by 2-BFI and agmatine [4].

References:
[1].  Hudson AL, Gough R, Tyacke R, et al. Novel selective compounds for the investigation of imidazoline receptors. Ann N Y Acad Sci, 1999, 881: 81-91.
[2].  Finn DP, Martí O, Harbuz MS, et al. Behavioral, neuroendocrine and neurochemical effects of the imidazoline I2 receptor selective ligand BU224 in naive rats and rats exposed to the stress of the forced swim test. Psychopharmacology (Berl), 2003, 167(2): 195-202.
[3].  Macinnes N, Duty S. Locomotor effects of imidazoline I2-site-specific ligands and monoamine oxidase inhibitors in rats with a unilateral 6-hydroxydopamine lesion of the nigrostriatal pathway. Br J Pharmacol, 2004, 143(8): 952-959.
[4].  Thorn DA, Zhang Y, Peng BW, et al. Effects of imidazoline I₂ receptor ligands on morphine- and tramadol-induced antinociception in rats. Eur J Pharmacol, 2011, 670(2-3): 435-440.

Chemical Properties

Cas No. 205437-64-5 SDF
Chemical Name 2-(4,5-dihydro-1H-imidazol-2-yl)quinoline hydrochloride
Canonical SMILES C12=CC=CC=C1N=C(C3=NCCN3)C=C2.Cl
Formula C12H11N3.HCl M.Wt 233.7
Solubility <2.34mg/ml in DMSO Storage Desiccate at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.279 mL 21.395 mL 42.7899 mL
5 mM 0.8558 mL 4.279 mL 8.558 mL
10 mM 0.4279 mL 2.1395 mL 4.279 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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