Abstract
We detected specific binding of 3H-ketanserin (0.6 nM) in rat renal cortical membrane preparations (4.70 ± 0.57 fmol/mg protein) and mesangial cells (7.55 ± 0.92 fmole/10 6 cells). Thus, the value in the renal cortical membrane corresponded to 15% of that in the cerebral cortical membranes (30.0 ± 2.9 fmole/mg protein). The affinity of 3H-ketanserin binding displacement activities by sarpogrelate, a selective 5-HT 2A receptor antagonist, in the renal cortical membrane (IC 50; 0.448 ± 0.061 μM) and mesangial cells (IC 50; 0.656 ± 0.187 μM) were almost 100-fold less than that in the cerebral cortical membrane (IC 50; 4.62 ± 1.02 nM). In the renal cortical membranes and mesangial cells, methysergide displaced a tiny fraction of 3H-ketanserin binding at concentrations up to 10 μM. These results did not explain the functional activity of 5-HT in the mesangial cells, and we conclude that specific 3H-ketanserin binding sites in the mesangial cells consisted of methysergide-resistant and non-serotonergic sites with low affinity for sarpogrelate.
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