Lacidipine

Bezeichnung:Lacidipine

CAS-Nr103890-78-4

Englisch Name:Lacidipine

CBNumberCB5296310

SummenformelC26H33NO6

Molgewicht455.54

MOL-Datei103890-78-4.mol

Lacidipine physikalisch-chemischer Eigenschaften

Schmelzpunkt	174-175°C
Siedepunkt	558.4±50.0 °C(Predicted)
Dichte	1.127±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble20mg/mL, clear
pka	3.00±0.70(Predicted)
Aggregatzustand	powder
Farbe	white to beige
Merck	14,5331
InChIKey	GKQPCPXONLDCMU-CCEZHUSRSA-N
CAS Datenbank	103890-78-4(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3
RTECS-Nr.	US7970200
Toxizität	mouse,LD50,intraperitoneal,80200ug/kg (80.2mg/kg),SKIN AND APPENDAGES (SKIN): HAIR: OTHERSENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYEBEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY),Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 22, Pg. 335, 1994.

Gefahreninformationscode (GHS)

Lacidipine Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Lacidipine is a new second-generation dihydropyridine calcium antagonist introduced as a once a day treatment for mild to moderate hypertension. It is reported to have high selectivity for vascular smooth muscle and also a long duration of action. The use of lacidipine as an antiatherosclerotic agent is currently under investigation.
Beschreibung
Lacidipine is a dihydropyridine L-type calcium channel blocker. It induces relaxation of isolated rat aorta and inhibits calcium-induced contraction of rabbit ear artery (pA₂ = 9.4). It also induces relaxation of calcium-induced contractions in isolated rat colon and bladder and guinea pig trachea (IC₅₀s = 6.7, 6, and 7.8 nM, respectively). Lacidipine induces negative inotropy in isolated guinea pig ventricular strips (IC₅₀ = 110 nM). It reduces mean blood pressure in spontaneously hypertensive rats (ED₂₅ = 0.35 mg/kg) and in renal hypertensive dogs (ED₂₅ = 0.22 mg/kg) with a transient increase in heart rate. Lacidipine inhibits copper-induced oxidation of isolated human LDL when used at concentrations of 1 and 5 μM. It reduces the extension of aortic atheromatous lesions and decreases renal injury in ApoE^-/- mice in a model of Western diet-induced atherosclerosis.
Chemische Eigenschaften
White-to-Off-White Crystalline Solid
Originator
Glaxo (United Kingdom)
Verwenden
A dihydropyridine calcium channel blocker. Antihypertensive.
Verwenden
antihypertensive;dihydropyridinr calcium channel blocker
Definition
ChEBI: Lacidipine is a cinnamate ester and a tert-butyl ester.
Trademarks
Lacipil; Lacirex; Viapres
Biochem/physiol Actions
Lacidipine is a long-acting calcium antagonist that is used in the management of hypertension. Lacidipine is a L-type Ca(2+) channel blocker belonging to 1,4-dihydropyridine class. Also, Lacidipine inhibits ryanodine receptors on the ER membrane that enhances folding, trafficking and lysosomal activity of ERAD (ER-associated degradation) misfolded lysosomal glucocerebrosidase (GS).

Lacidipine Upstream-Materialien And Downstream Produkte

Lacidipine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

103890-78-4, Lacidipine Verwandte Suche:

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