ISSN:
1432-1912
Keywords:
(+)-amphetamine
;
Neuronal uptake
;
Sympathomimetic amines
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary PC-12 cells (a clonal line of rat phaeochromocytoma cells) take up noradrenaline by a transport system which is identical with the neuronal amine transport system (“uptake1”). The uptake of 3H-noradrenaline into reserpine-pretreated PC-12 cells (monoamine oxidase inhibited) was saturable (Km=0.6±0.1 μmol/l), dependent on sodium and chloride, and competitively inhibited by (+)-amphetamine (Ki=0.18±0.04 μmol/l), cocaine (Ki=0.55±0.15 μmol/l) and desipramine (Ki=4.3±0.6 nmol/l). The uptake and accumulation of 3H (+)-amphetamine showed characteristics comparable to those of 3H-noradrenaline, since the uptake of 3H (+)-amphetamine (0.1 μmol/l) was reduced by omission of sodium or chloride from the incubation medium. The sodium-sensitive component of uptake and accumulation of 3H (+)-amphetamine was fully inhibited by cocaine and desipramine. The IC50 of desipramine for inhibition of the sodium-sensitive component of the 1-min uptake of 3H (+)-amphetamine (20 nmol/l) was about 2 nmol/l, i.e., identical with the Ki for inhibition of uptake of 3H-noradrenaline. At concentrations above 1 μmol/l, desipramine additionally caused an inhibition of the sodium-independent permeation of 3H (+)-amphetamine into PC-12 cells. Hence, by using a homogeneous population of cells endowed with “uptake1”, it is possible to demonstrate — besides a pronounced lipophilic entry — a carrier-mediated uptake of 3H (+)-amphetamine.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00506235
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