The stability of L-phenylalanine mustard in bile.

The stability of L-phenylalanine mustard in bile.
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L-苯丙氨酸芥末在胆汁中的稳定性。

DOI:
10.1016/0024-3205(78)90469-1
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发表时间:
1978
期刊:
影响因子:
6.1
通讯作者:
I. Sipes
I. Sipes
中科院分区:
医学2区
文献类型:
--
作者:
S. Chang;T. L. Evans;D. Alberts;I. Sipes

文献摘要

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摘要 L-苯丙氨酸芥末 (L-PAM) 在牛、犬和人的胆汁中于 37°C 下孵育。对于犬胆汁(0-3 小时),L-PAM 从胆汁中的回收率常数为 0.1/小时;牛胆汁0.18/小时;人胆汁 0.45/小时。在37°C下,在3至6小时内,犬胆汁中的L-PAM没有明显水解。在牛磺胆酸钠溶液(1000摩尔过量)中温育L-PAM,在37°C下,得到的回收率常数为0.15/小时。然而,在37°C下,将L-PAM在胆红素溶液(2.5mg/ml H 2 O)中温育,得到的回收率常数为0.52/小时。 37°C。静脉内给药后在犬胆汁中体内观察到的母体化合物L-PAM的高浓度可能与其在犬胆汁中的体外降解率低有关。
Abstract L-phenylalanine mustard (L-PAM) was incubated at 37° C in bile of bovine, canine and human origin. Recovery rate constants of L-PAM from bile were 0.1/hr for canine bile (0–3 hours); 0.18/hr for bovine bile; 0.45/hr for human bile. No significant hydrolysis of L-PAM in canine bile was noted for the period of 3 to 6 hours at 37° C. The incubation of L-PAM in sodium taurocholate solution (1000 molar excess) gave a recovery rate constant 0.15/hr at 37° C. However, the incubation of L-PAM in bilirubin solution (2.5 mg/ml H 2 O) gave a recovery rate constant of 0.52/hr at 37° C. The high concentration of the parent compound L-PAM seen in vivo in canine bile after iv administration may be related to its low in vitro degradation rate in canine bile.