2,6-dimethyl-3,5-bis(2'-propoxyethoxycarbonyl)-4-(2''-difluoromethoxyphenyl)-1,4-dihydropyridine Chemical Properties

form 

Solid

color 

Off-white to light yellow

2,6-dimethyl-3,5-bis(2'-propoxyethoxycarbonyl)-4-(2''-difluoromethoxyphenyl)-1,4-dihydropyridine Usage And Synthesis

Description

Cerebrocrast, also known as IOS-11212, is a calcium channel antagonist potentially for the treatment of cerebral vasospasm and cognition disorder. As Cerebrocrast decreased glucose levels in normal and streptozotocin (STZ)-induced diabetic rats, it also promoted glucose uptake by the brain, intensified insulin action and formation de novo of insulin receptors. Cerebrocrast did not alter current kinetics in either investigated channel, and the inhibition of calcium current was partly reversible or irreversible. As Cerebrocrast inhibited L- and T-type calcium channels, it can prevent vasoconstriction of kidney arterioles and aldosterone secretion that have significant roles in the development of hypertension and diabetic nephropathy.

Uses

Cerebrocrast (IOS-1.1212) is a 1,4-dihydropyridine (DHP) derivative. Cerebrocrast has a high affinity for the membrane lipid bilayer and it can easily penetrate the blood-brain barrier and incorporate into the plasma and organelle membranes, including those of mitochondria. Cerebrocrast promotes the cotransport of H+ and Cl- in rat liver mitochondria. Cerebrocrast also exhibits neuroprotective and cognition enhancer properties[1][2].

References

[1] Fernandes MA, et al. Cerebrocrast promotes the cotransport of H+ and Cl- in rat liver mitochondria. Mitochondrion. 2005 Oct;5(5):341-51. DOI:10.1016/j.mito.2005.06.004

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