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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Kajbaf M, Rossato P, Barnaby J R, Pellegatti M

Glaxo Wellcome S.p.A., Medicines Research Centre, Verona, Italy.

Xenobiotica. 1998 Feb;28(2):167-78. doi: 10.1080/004982598239669.

The in vitro metabolism of a novel CCK-B antagonist ((+)-N-[1-adamantane-1-methyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H- 1, 5-benzodiazepin-3-yl]N'-phenyl-urea; GV150013X) was investigated using rat, dog and human liver microsomes. 2. Four monohydroxy and four dihydroxy metabolites of GV150013X in rat and man were identified by comparison with authentic standards using HPLC and mass spectrometry. 3. The dihydroxy metabolite M1 was not detected in dog liver microsomes mixtures. 4. The formation of dihydroxylated metabolites proceeds via monohydroxylated metabolites M5 and M8 and not directly from GV150013X. 5. A monohydroxy metabolite M5 was the major metabolite in rat and dog, with M5 and dihydroxy metabolites M2 and M3 major metabolites in man.

使用大鼠、犬和人肝微粒体研究了一种新型CCK - B拮抗剂（(+)-N-[1-金刚烷-1-甲基)-2,4-二氧代-5-苯基-2,3,4,5-四氢-1H-1,5-苯并二氮杂卓-3-基]N'-苯基脲；GV150013X）的体外代谢。2. 通过使用高效液相色谱法（HPLC）和质谱法与标准品比较，鉴定了大鼠和人肝脏微粒体中GV150013X的四种单羟基代谢物和四种二羟基代谢物。3. 在犬肝微粒体混合物中未检测到二羟基代谢物M1。4. 二羟基化代谢物的形成是通过单羟基化代谢物M5和M8进行的，而非直接来自GV150013X。5. 单羟基代谢物M5是大鼠和犬中的主要代谢物，而在人中M5以及二羟基代谢物M2和M3是主要代谢物。

Kajbaf M, Rossato P, Barnaby J R, Pellegatti M

Glaxo Wellcome S.p.A., Medicines Research Centre, Verona, Italy.

Xenobiotica. 1998 Feb;28(2):167-78. doi: 10.1080/004982598239669.

The in vitro metabolism of a novel CCK-B antagonist ((+)-N-[1-adamantane-1-methyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H- 1, 5-benzodiazepin-3-yl]N'-phenyl-urea; GV150013X) was investigated using rat, dog and human liver microsomes. 2. Four monohydroxy and four dihydroxy metabolites of GV150013X in rat and man were identified by comparison with authentic standards using HPLC and mass spectrometry. 3. The dihydroxy metabolite M1 was not detected in dog liver microsomes mixtures. 4. The formation of dihydroxylated metabolites proceeds via monohydroxylated metabolites M5 and M8 and not directly from GV150013X. 5. A monohydroxy metabolite M5 was the major metabolite in rat and dog, with M5 and dihydroxy metabolites M2 and M3 major metabolites in man.

使用大鼠、犬和人肝微粒体研究了一种新型CCK - B拮抗剂（(+)-N-[1-金刚烷-1-甲基)-2,4-二氧代-5-苯基-2,3,4,5-四氢-1H-1,5-苯并二氮杂卓-3-基]N'-苯基脲；GV150013X）的体外代谢。2. 通过使用高效液相色谱法（HPLC）和质谱法与标准品比较，鉴定了大鼠和人肝脏微粒体中GV150013X的四种单羟基代谢物和四种二羟基代谢物。3. 在犬肝微粒体混合物中未检测到二羟基代谢物M1。4. 二羟基化代谢物的形成是通过单羟基化代谢物M5和M8进行的，而非直接来自GV150013X。5. 单羟基代谢物M5是大鼠和犬中的主要代谢物，而在人中M5以及二羟基代谢物M2和M3是主要代谢物。