Ni Ni 發問時間: 社會與文化語言 · 1 0 年前



Methotrexate Uptake. To evaluate the time-dependent

uptake of methotrexate in S2 hOAT1, S2 hOAT3 and S2

hOAT4, S2 cell monolayers were incubated in a solution

MTX Transport and Its Drug Interaction 667

containing 1 _M methotrexate (hOAT1) or 100 nM methotrexate

(hOAT3 and hOAT4) for various periods at 37°C. As

shown in Fig. 1, when the amount of methotrexate uptake in

mock was subtracted from those in S2 hOAT1, S2 hOAT3, and

S2 hOAT4, the specific uptake in S2 hOAT1 (Fig. 1A) and S2

hOAT4 (Fig. 1C) increased in a time-dependent manner and

reached steady state, whereas that in S2 hOAT3 (Fig. 1B)

decreased after reaching peak. The latter may be due to the

observation that nonspecific methotrexate efflux overwhelmed

hOAT3-mediated methotrexate uptake depending

on the nature of monoclonal cells into which hOAT3 cDNA

was transfected.

The kinetics of methotrexate uptake was examined to evaluate

the pharmacological characteristics of hOAT1, hOAT3,

and hOAT4 on methotrexate transport. The concentrationdependent

uptake of methotrexate was observed in S2

hOAT1, S2 hOAT3, and S2 hOAT4 after subtraction of uptake

by mock (data not shown). As shown in Fig. 2, Eadie-Hofstee

plot analysis of hOAT1-, hOAT3-, and hOAT4-mediated

methotrexate uptake gave a single straight line. The estimated

Km values of methotrexate uptake by hOAT1, hOAT3,

and hOAT4 were 553.8 _ 43.2 _M, 21.1 _ 2.8 _M, and 17.8 _

1.6 _M, respectively (from three determinations in one typical

experiment of two separate experiments). These results

suggest that hOAT1, hOAT3, and hOAT4 mediate transport

of methotrexate.

1 個解答

  • 1 0 年前


    Methotrexate 舉起。評估非定常

    methotrexate 舉起在S2 hOAT1, S2 hOAT3 和S2

    hOAT4, S2 細胞單層被孵化了在解答

    MTX 運輸和它的藥物互作用667

    包含1 _ M methotrexate (hOAT1) 或100 毫微米methotrexate

    (hOAT3 和hOAT4) 因為各種期間在37.C 。

    顯示在圖1, 當相當數量methotrexate 舉起

    嘲笑被減去了從那些在S2 hOAT1, S2 hOAT3, 和

    S2 hOAT4 、具體舉起在S2 hOAT1 (圖1A) 並且S2

    hOAT4 (圖1.C) 增加了以非定常方式和

    被到達的穩定狀態, 但是那在S2 hOAT3 (圖1B)


    未指明的methotrexate 廢氣流淹沒的觀察

    hOAT3 斡旋的methotrexate 舉起依靠

    在monoclonal 細胞的本質hOAT3 DNA

    是transfected 。

    methotrexate 舉起動能學被審查評估

    hOAT1 的藥物學特徵, hOAT3,

    並且hOAT4 在methotrexate 運輸。concentrationdependent

    methotrexate 舉起被觀察了在S2

    hOAT1 、S2 hOAT3, 和S2 hOAT4 在舉起的減法以後

    由嘲笑(資料沒被顯示) 。依照被顯示在圖2, Eadie-Hofstee

    密謀對hOAT1 的分析-, hOAT3 -, 和hOAT4 斡旋

    methotrexate 舉起給了一條唯一直線。估計

    methotrexate 舉起的公里價值由hOAT1, hOAT3,

    並且hOAT4 是553.8 _ 43.2 _ M, 21.1 _ 2.8 _ M, 和17.8 _

    1.6 _ M, 各自地(從三決心在一個典型

    二個不同實驗的實驗) 。這些結果

    建議, hOAT1 、hOAT3, 和hOAT4 斡旋運輸

    methotrexate 。

    參考資料: me