Inhibitory effect of KW-3902, an adenosine A(1) receptor antagonist, on p-aminohippurate transport in OK cells.
Inhibitory effect of KW-3902, an adenosine A(1) receptor antagonist, on p-aminohippurate transport in OK cells.
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KW-3902（一种腺苷 A(1) 受体拮抗剂）对 OK 细胞中 p-氨基马尿酸转运的抑制作用。
DOI：
10.1016/s0005-2736(99)00061-9
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发表时间：
1999
期刊：
影响因子：
--
通讯作者：
K. Inui
中科院分区：
文献类型：
--
作者：
J. Nagai;I. Yano;Y. Habu;T. Katsura;Y. Hashimoto;K. Inui
KW-3902（8-（noradamantan-3-yl）-1，3-dipropylxanthine）是一种新型的腺苷A1受体拮抗剂。我们研究了KW-3902对负鼠肾（OK）上皮细胞中对氨基马尿酸（PAH）转运的影响。KW-3902预处理3 h可抑制PAH从基底到顶侧跨OK细胞单层的跨细胞转运。KW-3902预处理可抑制OK细胞基底外侧膜对PAH的摄取，并呈时间和浓度依赖性。动力学分析表明，KW-3902对基底外侧PAH摄取的抑制作用是由于米氏常数（Km）的增加以及最大摄取速率（Vmax）的降低，表明抑制是混合型的。用腺苷脱氨酶或另一种选择性腺苷A1受体拮抗剂8-环戊基-1，3-二丙基黄嘌呤预处理，也可降低基底外侧PAH摄取。KW-3902预处理对细胞内α-酮戊二酸浓度无影响，α-酮戊二酸通过OK细胞基底外侧膜与PAH交换。这些结果表明KW-3902对OK上皮细胞中PAH转运具有抑制作用。
KW-3902 (8-(noradamantan-3-yl)-1,3-dipropylxanthine) is a novel potent and selective adenosine A1receptor antagonist. We examined the effect of KW-3902 on p-aminohippurate (PAH) transport in opossum kidney (OK) epithelial cells. Pretreatment for 3 h with KW-3902 inhibited the transcellular transport of PAH across OK cell monolayers from the basal to the apical side. The uptake of PAH across the basolateral membrane of OK cells was inhibited by KW-3902 pretreatment in a time- and concentration-dependent manner. A kinetic analysis revealed that the inhibitory effect of KW-3902 on the basolateral PAH uptake was due to an increase in the Michaelis constant (Km) as well as a decrease in the maximum uptake rate (Vmax), showing that the inhibition was a mixed type. Pretreatment with adenosine deaminase or 8-cyclopentyl-1,3-dipropylxanthine, another selective adenosine A1receptor antagonist, also decreased the basolateral PAH uptake. KW-3902 pretreatment had no effect on the concentration of intracellular α-ketoglutarate which exchanges for PAH across the basolateral membrane of OK cells. These results suggest that KW-3902 has an inhibitory effect on PAH transport in OK epithelial cells.
腺苷刺激负鼠肾上皮细胞中的磷酸盐和葡萄糖转运。
DOI：
10.1152/ajprenal.1991.260.6.f921
发表时间：
1991
期刊：
The American journal of physiology
影响因子：
--
作者：
Coulson,R;Johnson,RA;Olsson,RA;Cooper,DR;Scheinman,SJ
通讯作者：
Scheinman,SJ