product name Isradipine
Description: Isradipine (also known as PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker. Isradipine is classified as a calcium channel blocker of the dihydropyridine class. It is commonly prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack. More recent research in animal models suggests that isradipine may have potential uses for treating Parkinsons disease.
References: Gen Pharmacol. 1998 Jan;30(1):85-7; Neurobiol Dis. 2009 May;34(2):230-44.
371.39
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
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403506
| 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). Kinase Assay: Cell Assay: |
|---|---|
| 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 | |
| Formulation & Dosage | |
| References | Gen Pharmacol. 1998 Jan;30(1):85-7; Neurobiol Dis. 2009 May;34(2):230-44. |
Related Posts
product name Isradipine
Description: Isradipine (also known as PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker. Isradipine is classified as a calcium channel blocker of the dihydropyridine class. It is commonly prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack. More recent research in animal models suggests that isradipine may have potential uses for treating Parkinsons disease.
References: Gen Pharmacol. 1998 Jan;30(1):85-7; Neurobiol Dis. 2009 May;34(2):230-44.
371.39
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
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403506
| 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). Kinase Assay: Cell Assay: |
|---|---|
| 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 | |
| Formulation & Dosage | |
| References | Gen Pharmacol. 1998 Jan;30(1):85-7; Neurobiol Dis. 2009 May;34(2):230-44. |