Apovincaminicacidhydrochloridesalt是Vinpocetine(VP)的一种具有口服活性和可透过血脑屏障的主要活性代谢产物。Apovincaminicacidhydrochloridesalt具有神经保护作用。
Apovincaminic acid hydrochloride salt is an orally active and brain-penetrant main active metabolite of Vinpocetine (VP). Apovincaminic acid hydrochloride salt exerts a neuroprotective type of action[1][2].
Apovincaminic acid (10 mg/kg; i.p. twice daily for 4 days) effectively attenuates the behavioral deficits, and significantly decreases lesion size and the region of microglia activation[1].Apovincaminic acid (10 mg/kg; p.o.) is absorbed 50% of the dose comparing with i.v. administration in rats[2]. Animal Model: Male Harlan‐Wistar rats (300-400 g) are injected NMDA[1]
[1]. Nyakas C, et, al. Neuroprotective effects of vinpocetine and its major metabolite cis-apovincaminic acid on NMDA-induced neurotoxicity in a rat entorhinal cortex lesion model. CNS Neurosci Ther. Summer 2009;15(2):89-99. [2]. Pudleiner P, et, al. Study on the absorption of vinpocetine and apovincaminic acid. Eur J Drug Metab Pharmacokinet. Oct-Dec 1993;18(4):317-21. [3]. Wang M, et, al. Simultaneous Determination of Vinpocetine and its Major Active Metabolite Apovincaminic Acid in Rats by UPLC-MS/MS and its Application to the Brain Tissue Distribution Study. J Chromatogr Sci. 2018 Mar 1;56(3):225-232.
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