CR4056 (CR 4056, CR-4056) is a novel, orally active imidazoline-2 receptor (I2R) ligand with binding IC50 of 596 nM, also selectively inhibits the enzymatic activity of MAO-A with IC50 of 202.7 nM; increases norepinephrine (NE) tissue levels both in the rat cerebral cortex and lumbar spinal cord, shows ED50 of 5.8 mg/kg in CFA rat model of inflammatory pain; shows high effectivity against bortezomib-induced painful neuropathy in rats.
Cat.No
DC12396
Name
CR4056
Chemical Properties
CAS
1004997-71-0
Formula
C17H12N4
MW
272.311
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
[1]. Ferrari F, et al. Analgesic efficacy of CR4056, a novel imidazoline-2 receptor ligand, in rat models of inflammatory and neuropathic pain. J Pain Res. 2011;4:111-25.
[2]. Meregalli C, et al. CR4056, a new analgesic I2 ligand, is highly effective against bortezomib-induced painful neuropathy in rats. J Pain Res. 2012;5:151-67.
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