Manidipine
Manidipine (Manyper) · Artedil · Iperten · Manidipine · Franidipine · Manidipine 6300 · Manidipine（base） · Manidipine(CV-4093)
Identifikatoren & physikalische Daten
| CAS No. | 89226-50-6 |
|---|---|
| Summenformel | C35H38N4O6 |
| Durchschnittliche Molmasse | 610,7 g/mol |
| Monoisotopische Masse | 610,27913494 g/mol |
| SMILES | COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)C1c1cccc([N+](=O)[O-])c1 |
| InChIKey | ANEBWFXPVPTEET-UHFFFAOYSA-N |
| PubChem CID | 4008 |
| ChEMBL | CHEMBL1085699 |
| ChEBI | CHEBI:135849 |
| EC No. | 855-394-4 |
| DTXSID | DTXSID2043745 |
Chemische & physikalische Eigenschaften
| XLogP | 5,6 |
|---|---|
| Polarare Oberfläche (TPSA) | 117 |
| H-Brücken-Donoren | 1 |
| H-Brücken-Akzeptoren | 9 |
| Frei drehbare Bindungen | 11 |
| Schwere Atome | 45 |
| Formalladung | 0 |
| Komplexität | 1.090 |
| Löslichkeit | <1mg/mLSoluble in DMSO > 10 mM |
| Schmelzpunkt | 125-128°C |
| Siedepunkt | 722.0±60.0 °C(Predicted) |
| Dichte | 1.232±0.06 g/cm3(Predicted) |
| Lagerbedingungen | Sealed in dry,2-8°C |
| Aggregatzustand | Powder |
| pKa (Säurekonstante) | 6.12±0.10(Predicted) |
| Farbe | Light yellow to yellow |
| LogP (Verteilungskoeffizient) | 4.135 |
Sicherheit & Vorschriften
| GHS-Einstufung | DangerH301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]P264, P270, P301+P316, P321, P330, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 3 reports by companies from 1 notifications to the ECHA C&L Inventory.Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown. For more detailed information, please visit ECHA C&L website. |
|---|---|
| Regulatorische Informationen | Status: Active Update: 11-04-2022 https://echa.europa.eu/registration-dossier/-/registered-dossier/33372 |
| Hazard Classes and Categories | Acute Tox. 3 (100%) |
| Drug Induced Liver Injury | Drug-Induced Liver Injury Severity and Toxicity (DILIst)ManidipineDILI PositiveDOI:10.1016/j.drudis.2019.09.022 |
| Alarmwort | Warnung |
| Gefahrenhinweise | Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code H302 |
Anwendungen & Verwendung
Beschreibung
Manidipine is a dihydropyridine L- and T-type calcium channel blocker. It blocks recombinant rabbit L-type (α1Cα2/δβ1a) and human T-type (α1H) calcium channels expressed in Xenopus oocytes and native L-type channels in dissociated guinea pig cardiac ventricular cells (IC50 = 2.6 nM). Manidipine inhibits intracellular calcium increases induced by endothelin-1 (ET-1; ) in A7r5 rat vascular smooth muscle cells (ED50 = 1 nM) and potassium-induced contraction of isolated dog femoral and portal veins (IC50s = 24 and 2.1 nM, respectively). In vivo, it lowers blood pressure in spontaneously hypertensive rats (SHRs) when administered at a dose of 10 mg/kg and inhibits left ventricular hypertrophy in rats induced by isoproterenol when administered at a dose of 3 mg/kg. Formulations containing manidipine have been used in the treatment of hypertension.
Verwenden
Manidipine (Manyper) is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. It causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. It