Pharmacokinetics of the novel, high-affinity and selective dopamine D3 receptor antagonist SB-277011 in rat, dog and monkey:: in vitro/in vivo correlation and the role of aldehyde oxidase
Pharmacokinetics of the novel, high-affinity and selective dopamine D3 receptor antagonist SB-277011 in rat, dog and monkey:: in vitro/in vivo correlation and the role of aldehyde oxidase
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DOI：
10.1080/00498250110056531
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发表时间：
2001-08-01
期刊：
影响因子：
1.8
通讯作者：
Jeffrey, P
中科院分区：
文献类型：
--
作者：
Austin, NE;Baldwin, SJ;Jeffrey, P
1.在大鼠、犬、食蟹猴和人的肝微粒体和匀浆中进行了选择性多巴胺D3受体拮抗剂SB-277011的体外研究，以将代谢速率与化合物在大鼠、犬和食蟹猴中的体内药代动力学相关联。在存在NADPH的情况下，SB-277011在存在大鼠、犬、食蟹猴和人肝微粒体的情况下相对稳定，固有清除率（CL（i））为
1. In vitro studies with the selective dopamine D3 receptor antagonist SB-277011 were conducted in liver microsomes and homogenates from rat, dog, cynomolgus monkey and human to correlate the rate of metabolism with the in vivo pharmacokinetics of the compound in rat, dog and cynomolgus monkey.2. In the presence of NADPH, SB-277011 was relatively stable in the presence of liver microsomes from rat, dog, cynomolgus monkey and human with an intrinsic clearance (CL(i)) of