The present results showed that uptake of dopamine (DA) by rat isolate
d hepatocytes was mediated, in addition to simple diffusion, mainly by
a transporter-involved process, with K-m of 66.8 mu mol and V-max of
52.3 pmol.min(-1)/10(5) cells. The procesg was pH- and temperature-dep
endent and required an activation energy of 4.12 kcal.mol(-1)(Q(10) =
1.25) in the range of 2.0-12.7 C and 13.0 kcal.mol(-1)(Q(10) = 2.0) in
the range of 12.7-39.0 C. Cysteine residue having free thiol group wa
s unrelated to the activity of the transporter. Catecholamines, seroto
nin, and cocaine inhibited the DA transport but tyramine (TA) and tryp
tamine as well as benztropine and imipramine (which are potent inhibit
ors for hepatic TA transporter and neuronal DA transporter), had no in
hibitory effect on the transport of DA in these cells; These results i
ndicated that DA was taken up into hepatocytes by a distinct carrier.
NaF and mastoparan influenced the transport activity in these cells fu
rther, suggesting that signal transducing G-proteins may be involved i
n the regulation of DA transporter in rat hepatocytes.