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首页> 外文期刊>Life sciences >Incorporation of phencyclidine and its hydroxylated metabolites into hair.
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Incorporation of phencyclidine and its hydroxylated metabolites into hair.

机译：将苯环利定及其羟基化代谢物掺入头发中。

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The incorporation of phencyclidine(PCP) and its three major hydroxylated metabolites, 1-(1-phenylcyclohexyl)-4-hydroxypiperidine(PCHP), trans-4-phenyl-4-piperidinocyclohexanol(t-PPC) and trans-1-phenyl-1-(4'-hydroxypiperidino)-4-cyclohexanol(t-PCPdiol) into rat hair was studied. Three Dark Agouti male rats were intraperitoneally administered with PCP x HCl at a dose of 0.5 or 1.0 mg/kg once a day for 10 successive days. The plasma samples were collected from 5 min to 360 min after injection of each drug. The hair samples were collected 28 days after the first administration. The hair samples were extracted with methanol-5N hydrochloric acid(20:1) for 1 h under sonication. The plasma and hair extracts were extracted or purified with Bond Elut Certify and the extracts were silylated for the determination of PCP and its metabolites by GC/MS. The plasma AUCs were as follows; PCP(2.03 microg x min/ml) > t-PCPdiol(0.60 microg x min/ml) > PCHP(0.11 microg x min/ml) > t-PPC (0.065 microg x min/ml), while the hair concentrations were as follows; PCP(7.51 ng/mg) > PCHP (1.22 ng/mg) > t-PPC(0.10 ng/mg) > t-PCPdiol (0.05 ng/mg). In view of their AUCs, the hair concentration of t-PCPdiol was quite low, whereas that of PCP was so high. PCHP, t-PPC or t-PCPdiol was separately administered as the parent drug to the rats, and then the plasma and hair samples were analyzed in the same manner as PCP experiments. The incorporation rates ([hair concentration]/[AUC]) of PCP and its hydroxylated metabolites were as follows; PCP(2.29) > PCHP(0.79) > t-PPC(0.36) > t-PCPdiol(0.32). These data suggest that the decrease in lipophilicity caused by the hydroxylation of PCP suppresses the incorporation of the metabolites from blood into hair and the hydroxylation on cyclohexane ring(t-PPC) induces the decrease of the drug incorporation into hair more than that on piperidine ring(PCHP).
机译：苯环利定（PCP）及其三种主要的羟基化代谢产物1-（1-苯基环己基）-4-羟基哌啶（PCHP），反式-4-苯基-4-哌啶子基环己醇（t-PPC）和反式-1-苯基-研究了1-（4'-羟基哌啶子基）-4-环己醇（t-PCPdiol）进入大鼠毛发的过程。每天一次以0.5或1.0 mg / kg的剂量腹膜内给三只黑暗的Agouti雄性大鼠腹膜内施用PCP x HCl，连续10天。每种药物注射后5分钟至360分钟收集血浆样品。第一次给药后28天收集头发样品。在超声处理下，用甲醇-5N盐酸（20：1）提取头发样品1小时。用Bond Elut Certify提取或纯化血浆和毛发提取物，然后对提取物进行甲硅烷基化，以通过GC / MS测定PCP及其代谢产物。血浆AUC如下： PCP（2.03微克x分钟/毫升）> t-PCP二醇（0.60微克x分钟/毫升）> PCHP（0.11微克x分钟/毫升）> t-PPC（0.065微克x分钟/毫升），而头发浓度为跟随; PCP（7.51 ng / mg）> PCHP（1.22 ng / mg）> t-PPC（0.10 ng / mg）> t-PCP二醇（0.05 ng / mg）。考虑到它们的AUC，t-PCPdiol的头发浓度很低，而PCP的头发浓度却很高。将PCHP，t-PPC或t-PCPdiol分别作为母体药物给予大鼠，然后以与PCP实验相同的方式分析血浆和毛发样品。 PCP及其羟基化代谢物的掺入率（[头发浓度] / [AUC]）如下： PCP（2.29）> PCHP（0.79）> t-PPC（0.36）> t-PCPdiol（0.32）。这些数据表明由PCP的羟基化引起的亲脂性降低抑制了血液中代谢物向头发中的掺入，而环己烷环（t-PPC）上的羟基化导致的药物向头发中的掺入的减少比在哌啶环上的减少更多。 （PCHP）。

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