A functional study of SERT coding variants  

出　　处：《中国药理学通报》2015年第B11期49-49,共1页Chinese Pharmacological Bulletin

摘　　要：Aim To characterize the SSRIs sensitivity in C57 and DBA mouse strain and identify the protein struc- tural determinants that contribute to the SSRIs sensitivity. Methods Multiple behavioral assays were conducted to characterize the SSRIs sensitivity in C57 and DBA mouse strain . We performed in vitro binding and uptake assays to assess the pharmacological properties differences of the SSRIs in C57 and DBA mouse strain. Results The ma- jor difference between the 5-HT transport kinetics of the SERTs was found in their maximal transport capacity rather than the transporter＇ s apparent affinity for 5-HT in two mouse strains. C57 mice displayed a significant loss in cita- lopram sensitivity. DBA mice displayed a significant loss in fluoxetine sensitivity. Paroxetine and YL-0919 displayed the same sensitivity in tow mouse strain. Conclusion Results suggest that the two mouse strain have different re- sponses activity to the treatment of SSRIs. The Kd values for 5-HT transporter binding were significantly different a- mong the five compounds of SSRIs we studied in C57 and DBA mouse strain as well as reuptake assays.

关 键 词：SEROTONIN TRANSPORTER antidepressants REUPTAKE 

分 类 号：R[医药卫生]