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4. Looking at the following table and structures, why I-387 has the longest rete

ID: 480015 • Letter: 4

Question

4. Looking at the following table and structures, why I-387 has the longest retention time? I-387 is new antitubulin agent with potent in vivo and in vitro antitumor activity. Summary of the metabolite profile generated after incubation of I-387 with liver microsomes of mouse, rat, dog, monkey, and human Retention Time (M Hj Fragment lons Compound min 388 192 11.3-11.4 I-387 Demethylation in C ring 192 10.6 375 10.8 M4 Reduction of ketone 390.5 154, 194, 222 10.5 M2 Demethylation in C ring and hydroxylation in A/B ring 208 390.5 9.5 M5 9.7 M6 11.4 Hydroxylation in A/B ring 404.5 208 M8 10.2-10.3 M3 10.6 M9

Explanation / Answer

A longer retention time is because of greater uptake and slower efflux. Different substances / drugs remain in a person's system for varying periods of time. Many factors determine how long a drug is detectible, and varying tests are used to determine use of drugs for either a period of days or period of months.

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