CAS NO: | 75695-93-1 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 371.39 |
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Formula | C19H21N3O5 |
CAS No. | 75695-93-1 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 74 mg/mL (199.3 mM) |
Water: <1 mg/mL | |
Ethanol: 74 mg/mL (199.3 mM) | |
Solubility (In vivo) | 2% DMSO+Corn oil: 10mg/mL |
Synonyms | PN 200-110; DynaCirc, Prescal, Lomir, PN-200-110, PN-205-033, PN-205-034 |
In Vitro | In vitro activity: Isradipine produces inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. Isradipine is found to be the most potent derivative in both, in growth cultures (I50 = 20.8 mM) and in vivo oxygen uptake (I50 = 31.1 mM). |
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In Vivo | Isradipine reduces hypoxia-induced activation of calcium dependent xanthine oxidases, monoamine oxidases, cytosolic phospholipase A(2) and cyclooxygenases (COX-2) along with concomitant decrease in free radical generation and cytochrome c release. Isradipine prevents hypobaric hypoxia along with augmented neurodegeneration and memory impairment induced increased expression of calpain and caspase 3. Isradipine (at the dose of 1 mg/kg three times a day) reduces ethanol intake by over 70% in ethanol-preferring rats, the reduction in ethanol intake is compensated by a proportional increase in water consumption and the inhibitory effect persisted throughout the 5 days of treatment. Isradipine significantly reduces the arterial wall collagen contents in both strains, with marked increases in the elastin content in the carotid but not in the aortic wall in spontaneously hypertensive rats. Isradipine suppresses the reinforcing properties of morphine and cocaine and may be an effective pharmacotherapy for treatment of cocaine and heroin abuse in mice. |
Animal model | Mice |
Formulation & Dosage | 1 mg/kg |
References | Gen Pharmacol. 1998 Jan;30(1):85-7; Neurobiol Dis. 2009 May;34(2):230-44. |