ISSN:
1435-1463
Keywords:
Uptake
;
inhibition
;
dopamine transporter
;
1-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline
;
1,2-dimethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline
;
1,2-dimethyl-6,7-dihydroxyisoquinolinium ion
;
neuroblastoma SH-SY5Y cells
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary Uptake of catechol isoquinolines to dopamine cells was studied using human dopaminergic neuroblastoma SH-SY5Y cells. Only (R)-1,2-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline [(R)-1,2-DiMeDHTIQ] was transported by dopamine uptake system, while (S)-1,2-DiMeDHTIQ, (R)- and (S)-1-methyl-6,7-dihydroxy-tetrahydroisoquinoline, and 1,2-dimethyl-6,7-dihydroxyisoquinolinum ion were not. Kinetical study showed that the uptake of (R)-1,2-DiMeDHTIQ followed the Michaelis-Menten equation, and the values of the Michaelis constant and the maximal velocity were obtained to be 102.6 ± 36.9 μM and 66.0 ± 2.8 pmol/min/mg protein. Dopamine was found to inhibit (R-1-DiMeDHTIQ uptake competitively. These results suggest that the selective uptake by dopamine transporter may account for the specific neurotoxicity of (R)-1,2-DiMeDHTIQ to dopamine neurons.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01277014
