Isradipine

Isradipine (PN 200-110) is an orally active and blood-brain barrier permeability L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease^[1][2][3]. IC50 & Target:L-type calcium channel^[1][2] In Vitro:Isradipine has much higher (＞40 fold) affinity for Cav1.3 channels as well as good brain bioavailability. Isradipine has nearly equal potency at Cav1.2 and Cav1.3 channels^[1]. In Vivo:Isradipine (0.1~3 mg/kg; p.o.) makes sodium excretion increase in a dose-dependent manner^[3].
Isradipine pre-treatment reduces 6-hydroxydopamine induced neurotoxicity at the striatal level. Protective effect of isradipine at the striatal level is dose-dependent as shown from 6 mice. Isradipine pre-treatment increases the number of surviving SNc DA cells after 6-hydroxydopamine induced degeneration. Isradipine is capable of protecting striatal dopaminergic terminals and SNc dopaminergic cell bodies against a slow, progressive insult created by intrastriatal injection of 6-hydroxydopamine^[1].