Abcb1a but not Abcg2 played a predominant role in limiting the brain distribution of HUPERZINE (cas 116-28-9) A in mice
-
Add time:08/25/2019 Source:sciencedirect.com
HUPERZINE (cas 116-28-9) A has been used for improving symptoms of Alzheimer's disease. Its cholinergic side effect is thought to be an exaggerated pharmacological outcome linked to its high brain or CNS concentrations. Although Huperzine A is brain penetrable, its interaction with efflux transporters (ABCB1 and ABCG2) has not been fully investigated. The aim of the present study was to characterize roles of ABCB1 and ABCG2 in the transmembrane transport of Huperzine A and identify a rate limiting step in its brain distribution. Data obtained from stably transfected MDCK II cells showed that Huperzine A is a substrate of ABCB1 but not ABCG2. ABCB1 inhibitors significantly inhibited ABCB1 mediated efflux of Huperzine A. In Abcb1a−/− mice, the brain to plasma concentration ratio of Huperzine A was significantly increased as compared to the wild type mice, while there were no obvious differences between the wild type and Abcg2−/− mice. Taken together, the present study demonstrated that ABCB1 but not ABCG2 played a predominant role in the efflux of Huperzine A across BBB. The current finding is clinically relevant as changes in ABCB1 activity in the presence of ABCB1 inhibitors or genetic polymorphism may affect efficacy and safety of Huperzine A.
We also recommend Trading Suppliers and Manufacturers of HUPERZINE (cas 116-28-9). Pls Click Website Link as below: cas 116-28-9 suppliers
Prev:ABAD/17β-HSD10 reduction contributes to the protective mechanism of HUPERZINE (cas 116-28-9) a on the cerebral mitochondrial function in APP/PS1 mice
Next:Microbial transformation of (−)-HUPERZINE (cas 116-28-9) A) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Administration of HUPERZINE (cas 116-28-9) A exerts antidepressant-like activity in a rat model of post-stroke depression08/31/2019
- Simultaneously preparative purification of HUPERZINE (cas 116-28-9) A and HUPERZINE (cas 116-28-9) B from Huperzia serrata by macroporous resin and preparative high performance liquid chromatography08/30/2019
- Structural analogs of HUPERZINE (cas 116-28-9) A improve survival in guinea pigs exposed to soman08/29/2019
- A combination of [+] and [−]-HUPERZINE (cas 116-28-9) A improves protection against soman toxicity compared to [+]-HUPERZINE (cas 116-28-9) A in guinea pigs08/28/2019
- Variations of HUPERZINE (cas 116-28-9) A content in Lycopodiaceae species from tropics08/27/2019
- Microbial transformation of (−)-HUPERZINE (cas 116-28-9) A08/26/2019
- ABAD/17β-HSD10 reduction contributes to the protective mechanism of HUPERZINE (cas 116-28-9) a on the cerebral mitochondrial function in APP/PS1 mice08/24/2019
- Original ArticleHUPERZINE (cas 116-28-9)-A response to cognitive impairment and task switching deficits in patients with Alzheimer's disease08/23/2019
- HUPERZINE (cas 116-28-9) a loaded multiparticulate disintegrating tablet: Drug release mechanism of ethyl cellulose microparticles and pharmacokinetic study08/22/2019