The transport of (+)-amphetamine by the neuronal noradrenaline carrier

Naunyn Schmiedebergs Arch Pharmacol. 1984 Oct;327(4):267-72. doi: 10.1007/BF00506235.


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 mumol/l), dependent on sodium and chloride, and competitively inhibited by (+)-amphetamine (Ki = 0.18 +/- 0.04 mumol/l), cocaine (Ki = 0.55 +/- 0.15 mumol/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 mumol/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 mumol/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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenal Gland Neoplasms / metabolism
  • Animals
  • Biological Transport / drug effects
  • Cell Line
  • Cocaine / pharmacology
  • Desipramine / pharmacology
  • Dextroamphetamine / metabolism*
  • Kinetics
  • Neurons / metabolism*
  • Norepinephrine / metabolism*
  • Pheochromocytoma / metabolism
  • Rats


  • Cocaine
  • Desipramine
  • Dextroamphetamine
  • Norepinephrine