Isradipine-d₇  (Synonyms: PN 200-110-d₇)

Isradipine-d₇ is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active 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].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Isradipine (0.1~3 mg/kg; p.o.) makes sodium excretion increase in a dose-dependent manner^[4].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

378.43

C₁₉H₁₄D₇N₃O₅

75695-93-1

O=C(C1=C(C)NC(C)=C(C(OC([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=O)C1C2=CC=CC3=NON=C23)OC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Ilijic E, et al. The L-type channel antagonist isradipine is neuroprotective in a mouse model of Parkinson's disease. Neurobiol Dis. 2011;43(2):364-371.  [Content Brief]

  [3]. Campbell CA, et al. Effects of isradipine, an L-type calcium channel blocker on permanent and transient focal cerebral ischemia in spontaneously hypertensive rats. Exp Neurol. 1997;148(1):45-50.  [Content Brief]

  [4]. Hof RP, et al. Selective effects of PN 200-110 (isradipine) on the peripheral circulation and the heart. Am J Cardiol. 1987;59(3):30B-36B.  [Content Brief]