AHC-93(AHC-93) - 药物靶点：P-gp x chloride channel_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

P-gp x chloride channel

作用机制

P-gp抑制剂(P-糖蛋白-1抑制剂)、chloride channel阻滞剂(氯离子通道阻滞剂)

治疗领域

心血管疾病其他疾病

在研适应症-

非在研适应症

围手术期缺血再灌注损伤

原研机构

Toho University

在研机构-

非在研机构

Toho University

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 AHC-93 相关的临床结果

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100 项与 AHC-93 相关的转化医学

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100 项与 AHC-93 相关的专利（医药）

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1

项与 AHC-93 相关的文献（医药）

1999-12-01·Experimental Cell Research3区 · 医学

Role of P-glycoprotein in Human Natural Killer-Like Cell Line-Mediated Cytotoxicity

3区 · 医学

Article

作者: Yoshiki Misawa ; Hikaru Tanaka ; Yoshiro Kobayashi ; Munehisa Takahashi ; Koki Shigenobu ; Naoko Watanabe ; Toru Kawanishi

Natural killer (NK) cells express the highest amount of P-glycoprotein (Pgp), a product of the multidrug resistance (MDR) 1 gene, among lymphoid cells, and our previous studies demonstrated that Pgp is required for NK cell-mediated cytotoxicity. In this study we examined the role of Pgp in NK cell-mediated cytotoxicity using a human NK-like cell line, i.e., YTN cells and two MDR reversing agents, nicardipine and its structural analog, AHC-93. These two agents inhibited the Pgp function (rhodamine-123 excretion) as well as cell-mediated cytotoxicity, confirming that Pgp is critical for NK cell-mediated cytotoxicity. As revealed by video-rate ultraviolet laser-scanning confocal microscopy, AHC-93 did not inhibit the increase in the intracellular calcium concentration upon binding to target cells, whereas nicardipine did, as reported previously. These two reagents relocated acridine orange dye from lysosomes to the cytoplasm at concentrations similar to those required for the inhibition of cell-mediated cytotoxicity. These results suggest that Pgp is directly or indirectly involved in pH regulation in lysosomes, but not in calcium homeostasis.

100 项与 AHC-93 相关的药物交易

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