Isradipine Chemical Properties

Melting point:

166-1680C

Boiling point:

501.9±60.0 °C(Predicted)

Density 

1.249±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: ~26 mg/mL

form 

solid

pka

2.56±0.70(Predicted)

color 

yellow

Merck 

14,5240

BCS Class

2/4

Stability:

Stable for 2 years from date of purchsae as supplied. Protect from moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

InChIKey

HMJIYCCIJYRONP-UHFFFAOYSA-N

CAS DataBase Reference

75695-93-1(CAS DataBase Reference)

NIST Chemistry Reference

Isradipine(75695-93-1)

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

HS Code 

2934990002

MSDS

• Language:English Provider:4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester
• Language:English Provider:SigmaAldrich

Isradipine Usage And Synthesis

Description

Isradipine is a long-acting calcium blocker effective in the treatment of essential hypertension. The advantages of isradipine as compared with other dihydropyridine calcium antagonists include a "gentle" onset and fewer contraindications. It can be taken by patients with diabetes mellitus, chronic obstructive airway diseases, gout, congestive heart failure or ischemic heart disease.

Chemical Properties

Yellow Solid

Originator

Sandoz (Switzerland)

Uses

Isradipine is a L-type calcium channel blocker, Isradipine has anti-atherosclerotic effects in animals and improves endothelium-mediated nitric oxide (NO)-dependent vasodilation in vitro. Additional studies indicate that Isradipine may provide a neuroprotective effect in a rat model of focal ischemia and that Isradipine produces a dose-dependent sparing of dopamine neuronal fibers and cell bodies.

Uses

nonsedating H1-antihistamine

Uses

Dihydropyridine calcium channel blocker. Antihypertensive; antianginal

Definition

ChEBI: Isradipine is an isopropyl ester, a methyl ester, a dihydropyridine and a benzoxadiazole.

brand name

Dynacirc (Reliant);Prescal.

General Description

Isradipine, 4-(4-benzofuranazyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylic acid methyl 1-methylethyl ester (DynaCirc), is another second-generationdihydropyridine-type channel blocker. This drug, like theother second-generation analogs, is more selective for vascularsmooth muscle than for myocardial tissue. It is effectivein the treatment of stable angina, reducing the frequencyof anginal attacks and the need to use nitroglycerin.

Biological Activity

Potent and selective L-type voltage-gated Ca 2+ channel blocker. EC 50 and pA 2 values are 1.4 nM and 10.3 for relaxation of depolarization- and Ca 2+ -induced contractions of rabbit aorta respectively; EC 25 = 0.45 nM for reduction in rate of spontaneously beating guinea pig right atria. Long-acting antihypertensive agent in vivo , exerting primary effects on vascular tissue with secondary negative chronotropic action.

Biochem/physiol Actions

L-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.

storage

Room temperature

References

1) Bracht et al. (2001), Isradipine improves endothelium-dependent vasodilation in normotensive coronary artery disease patients with hypercholesterolemia; J. Hyperten., 19 899 2) Chandra et al. (1999), Use of diffusion-weighted MRI and neurological deficit scores to demonstrate beneficial effects of isradipine in a rat model of focal ischemia ; Pharmacology, 58 292 3) Merck 14:5240

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