规格: | 98% |
分子量: | 244.2 |
包装 | 价格(元) |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Background:
Carbidopa is a peripherally-restricted inhibitor of dopamine decarboxylase, the enzyme that converts L-DOPA to dopamine.1Carbidopa (100 mg/kg) pretreatment in dog increases the plasma concentration of L-DOPA by 186% and prolongs the half-life in plasma by 48% and skeletal muscle extracellular fluid by 66%.2Carbidopa also binds to and potentiates the activity of the aryl hydrocarbon receptor (AhR), which is a ligand-dependent transcription factor that mediates the toxicity of certain xenobiotics and polyaromatic hydrocarbons.3It inhibits the proliferation of pancreatic cancer cellsin vitroand tumor growthin vivo. Formulations containing carbidopa are used in combination with L-DOPA in the treatment of Parkinson's disease to increase the amount of dopamine in the brain and reduce peripheral side effects associated with L-DOPA administration.
1.Clark, W.G., Oldendorf, W.H., and Dewhurst, W.G.Blood-brain barrier to carbidopa (MK -486) and Ro 4-4602, peripheral dopa decarboxylase inhibitorsJ. Pharm. Pharmacol.25(5)416-418(1973) 2.Deleu, D., Sarre, S., Ebinger, G., et al.The effect of carbidopa on the pharmacokinetics and metabolism of intravenously administered levodopa in blood plasma and skeletal muscleNaunyn Schmiedebergs Arch. Pharmacol.348(6)576-581(1993) 3.Ogura, J., Miyauchi, S., Shimono, K., et al.Carbidopa is an activator of aryl hydrocarbon receptor with potential for cancer therapyBiochem J.474(20)3391-3402(2017)