Isradipine

Isradipine Basic information
Product Name:Isradipine
Synonyms:PN-200-110;Presca;Prescal;4-(4-Benzofurazanyl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester;4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic [chemical name] acid methyl 1-methylethyl ester;Dynacrine;Iomir;Rebfiden
CAS:75695-93-1
MF:C19H21N3O5
MW:371.39
EINECS:630-420-5
Product Categories:ALLEGRA;Ion Channels;Intermediates & Fine Chemicals;Pharmaceuticals;Calcium channel;API
Mol File:75695-93-1.mol
Isradipine Structure
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
pka2.56±0.70(Predicted)
form solid
color yellow
Merck 14,5240
BCS Class2/4
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.
InChIKeyHMJIYCCIJYRONP-UHFFFAOYSA-N
CAS DataBase Reference75695-93-1(CAS DataBase Reference)
NIST Chemistry ReferenceIsradipine(75695-93-1)
Safety Information
Safety Statements 22-24/25
WGK Germany 3
HS Code 2934990002
Isradipine Usage And Synthesis
DescriptionIsradipine 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 PropertiesYellow Solid
OriginatorSandoz (Switzerland)
UsesIsradipine 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.
Usesnonsedating H1-antihistamine
UsesDihydropyridine calcium channel blocker. Antihypertensive; antianginal
DefinitionChEBI: Isradipine is an isopropyl ester, a methyl ester, a dihydropyridine and a benzoxadiazole.
Brand nameDynacirc (Reliant);Prescal.
General DescriptionIsradipine, 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 ActivityPotent 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 ActionsL-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.
storageRoom temperature
References1) 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
Isradipine Preparation Products And Raw materials
Raw materialsMethyl 3-aminocrotonate-->Isopropyl acetoacetate-->Benzofuroxan
Bendamustine Oxiracetam Lercanidipine ISRADIPINE 2-PROPANOLE-D7 Benzofuroxan Isradipine N,N-Dimethylformamide ETHANE Pranidipine Dimethyl fumarate Dimethyl sebacate Dimethyl sulfoxide Dimethyl ether Dimethyl carbonate Dihydromyrcenol 2,6-DIMETHYL-3,5-PYRIDINEDICARBOXYLIC ACID Dimethyl phthalate

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