Kurokawa T, Matsumoto T, Ashida Y, Sasada R, Iwasa S
DDS Research Laboratories, Takeda Chemical Industries, Ltd., Osaka, Japan.
Biol Pharm Bull. 1994 Mar;17(3):383-5. doi: 10.1248/bpb.17.383.
The human thromboxane A2 receptor (TXA2-R)-coding gene was introduced into Chinese hamster ovary cells and a cell line (TCHO-25) stably expressing TXA2-R, at a level of 3 x 10(5)/cell, was obtained. An anti-asthmatic agent AA-2414 [(+-)-7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7- phenylheptanoic acid] competitively inhibited the specific binding of a TXA2 mimic ([3H]U-46619) to the TCHO-25 cells, with an IC50 of 6.0 x 10(-8) M, indicating that the drug is an antagonist of human TXA2-R. The TCHO-25 cells offer a tool for the screening and characterization of human TXA2-R antagonists.
将人血栓素A2受体（TXA2-R）编码基因导入中国仓鼠卵巢细胞，获得了稳定表达TXA2-R的细胞系（TCHO-25），其表达水平为3×10⁵/细胞。抗哮喘药AA-2414 [（±）-7-（3,5,6-三甲基-1,4-苯醌-2-基）-7-苯基庚酸]竞争性抑制TXA2类似物（[³H]U-46619）与TCHO-25细胞的特异性结合，IC50为6.0×10⁻⁸ M，表明该药物是人TXA2-R的拮抗剂。TCHO-25细胞为筛选和鉴定人TXA2-R拮抗剂提供了一种工具。
