Binding affinity of sarpogrelate to 5-HT2A receptor ligand recognition sites in rat renal cortical and mesangial cells in culture

被引:4
|
作者
Nishio, H [1 ]
Yoshikawa, S
Morimoto, Y
Chen, ZQ
Nakata, Y
机构
[1] Fukuyama Univ, Fac Pharm & Pharmaceut Sci, Dept Pharmacol, Hiroshima 7290292, Japan
[2] Hiroshima Univ, Sch Med, Inst Pharmaceut Sci, Dept Pharmacol, Hiroshima 7348551, Japan
来源
GENERAL PHARMACOLOGY | 1999年 / 33卷 / 01期
关键词
5-hydroxytryptamine; 5-HT2A receptors; mesangial cells; ketanserin; sarpogrelate; recognition sites;
D O I
10.1016/S0306-3623(98)00266-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
We detected specific binding of H-3-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 H-3-ketanserin binding displacement activities by sarpogrelate, a selective 5-HT2A receptor antagonist, in the renal cortical membrane. (IC50; 0.448 +/- 0.061 mu M) and mesangial cells (IC50; 0.656 +/- 0.187 mu M) were almost 100-fold less than that in the cerebral cortical membrane (IC50; 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 mu M. These results did not explain the functional activity of 5-HT in the mesangial cells, and we conclude that specific H-3-ketanserin binding sites in the mesangial cells consisted of methysergide-resistant and non-serotonergic sites with low affinity for sarpogrelate. (C) 1999 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:51 / 57
页数:7
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