Pharmaceutical Grade CAS 105628-07-7 Fasudil HCl Raw Materials Fasudil
Product Description
Product Details
| Product Name |
Fasudil Hydrochloride |
| Cas number |
203911-27-7 |
| Appearance |
White Powder |
| MF |
C14H17N3O2S.2ClH.H2O |
| MW |
327.83 |
asudil hydrochloride is a protein kinase inhibitor or intracellular calcium antagonist. The contraction of vascular smooth muscle is due to the activation of key enzymes by significantly increased Ca2+ concentration in smooth muscle cells. When Ca2+ reaches a certain concentration, it binds to Ca2+ binding protein calmodulin, activates myosin light chain phosphorylase, phosphorylates myosin light chain, and causes muscle contraction. During subarachnoid hemorrhage, various vasoconstricting substances released from the blood vessels participate in vasospasm and eventually cause vasoconstriction through myosin light chain phosphorylation. Fasudil hydrochloride dilates blood vessels and inhibits vasospasm by blocking the final stage of the vasoconstriction process, myosin light chain phosphorylation.
Application&Function
pharmacokinetics
Absorption: When the radio-labeled product is administered intravenously to rats and monkeys, the concentration of radioactivity in the blood rapidly decreases after self-medication. In the case of continuous intravenous administration, the blood concentration decreased after the end of self-administration, and the half-life of the rats was about 1.4 hours, and the AUC increased with the increase of the dose, which was linear with the plasma concentration.
Distribution: Rapid metastasis to tissues after administration, with high concentrations of the drug in liver, kidney, spleen and intestine. Metastasis to the brain is also seen.
Metabolism: After the administration of this product, 80% of the original drug and the main metabolite of isoquinoline skeleton L-position hydroxide and its combination. The total number of metabolites was 6 in rats and 5 in monkeys.
Excretion: 41.1%, 6.4% and 38.4% were excreted in urine, stool and bile, respectively. Plasma protein binding rate: The binding rate of plasma protein of this product is about 80% in vitro, about 34% to 62% in vivo. Animal experiments have shown that this product can pass the placenta and transfer to the milk. In healthy human experiments, when 0.2mg/kg and 0.4mg/kg of this product are administered intravenously continuously, the disappearance half-life after the end of administration is about 15 minutes. The AUC and the maximum blood concentration increased with the increase of dosage. After subarachnoid hemorrhage patients were given 30mg intravenous drip/time, the evolution of plasma drug concentration was not significantly different from that of healthy people.
Specification
About US
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