Isradipine

Bezeichnung:Isradipine

CAS-Nr75695-93-1

Englisch Name:Isradipine

CBNumberCB2268682

SummenformelC19H21N3O5

Molgewicht371.39

MOL-Datei75695-93-1.mol

Isradipine physikalisch-chemischer Eigenschaften

Schmelzpunkt	166-1680C
Siedepunkt	501.9±60.0 °C(Predicted)
Dichte	1.249±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: ~26 mg/mL
Aggregatzustand	solid
pka	2.56±0.70(Predicted)
Farbe	yellow
Merck	14,5240
BCS Class	2/4
Stabilität	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 Datenbank	75695-93-1(CAS DataBase Reference)
NIST chemische Informationen	Isradipine(75695-93-1)

Sicherheit

S-Sätze:	22-24/25
WGK Germany	3
HS Code	2934990002

Gefahreninformationscode (GHS)

Isradipine Chemische Eigenschaften,Einsatz,Produktion Methoden

S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
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.
Chemische Eigenschaften
Yellow Solid
Originator
Sandoz (Switzerland)
Verwenden
nonsedating H1-antihistamine
Verwenden
Dihydropyridine calcium channel blocker. Antihypertensive; antianginal
Verwenden
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.
Definition
ChEBI: Isradipine is an isopropyl ester, a methyl ester, a dihydropyridine and a benzoxadiazole.
Trademarks
Dynacirc (Reliant);Prescal.
Allgemeine Beschreibung
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.
Biologische Aktivität
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.
Lager
Room temperature
Einzelnachweise
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

Isradipine Upstream-Materialien And Downstream Produkte

Isradipine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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