BU 224 hydrochloride

Product NameBU 224 hydrochloride
CAS205437-64-5
MFC12H12ClN3
MW233.7
EINECS
MOL File205437-64-5.mol

Chemical Properties

solubility	Soluble to 10 mM in DMSO
form	Solid
color	Brown to gray

Usage And Synthesis

Description

BU-224 is a Putative I2 antagonist; and a high affinity ligand for the imidazoline I2 binding site (Ki = 2.1 nM). BU224 reverses cognitive deficits, reduces microgliosis and enhances synaptic connectivity in a mouse model of Alzheimer's disease.

Uses

BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research[1][2][3].

in vivo

BU224 hydrochloride (5 mg/kg, IP, twice a day for 10 days) improves behavioural performance and memory function in 5XFAD mice^[1].
BU224 hydrochloride (5 mg/kg, IP, twice a day for 10 days) reduces levels of the microglial marker Iba1 and pro-inflammatory cytokines IL-1β and TNF-α and increased the expression of astrocytic marker GFAP in 5XFAD mice^[1].
BU224 hydrochloride (10 mg/kg, IP, once) reduces immobility of rats in the FST (forced swim test), indicative of antidepressant-like activity^[2].

Animal Model:	5XFAD mice and and WT littermates (6-month-old)^[1]
Dosage:	0 mg/kg, 5 mg/kg
Administration:	IP, twice a day for 10 days
Result:	Significantly increased immobility (54% increased freezing), and reversed memory deficits secondary to the deposition of Aβ in the brain.

storage

Desiccate at RT

References

[1] Mirzaei N, et al. Imidazoline ligand BU224 reverses cognitive deficits, reduces microgliosis and enhances synaptic connectivity in a mouse model of Alzheimer's disease. Br J Pharmacol. 2021 Feb;178(3):654-671. DOI:10.1111/bph.15312
[2] Finn DP, 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 May;167(2):195-202. DOI:10.1007/s00213-003-1392-3
[3] Qiu Y, et al. Discriminative stimulus effects of the imidazoline I2 receptor ligands BU224 and phenyzoline in rats. Eur J Pharmacol. 2015 Feb 15;749:133-41. DOI:10.1016/j.ejphar.2015.01.013

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