《藥物代謝》 (2)ppt課件

1、213主要反響類型：主要反響類型：RH + NADPH + H+ + O2P450ROH + NADP+ + H2O普萘洛爾普萘洛爾 苯乙雙胍苯乙雙胍 R= H 原形藥物原形藥物 R= OH 代謝產(chǎn)物代謝產(chǎn)物 RONHCH3OHCH3NHNHNH2NHNHR丙磺舒丙磺舒 R= H 地西泮地西泮 R= OH 4-羥基地西泮羥基地西泮 SNOOCH3CH3ClRNNH3COOHORORROHROHOHROSO3HOHRSGOHRMOHH2OH2SO4MROHSOOHNHAcGSHM:生生物物大大分分子子GSH:谷谷胱胱甘甘肽肽硫硫醚醚氨氨酸酸結(jié)結(jié)合合物物重重排排OHHOOHONHOHHONHNNN

2、O苯苯并并（）芘芘核核糖糖NONH2NONH2NONH2OHOOH卡卡馬馬西西平平H3CH3CCOOHCH3H3CHOH2CCOOHCH3H3CH3CCOOHCH3OHH3CH3CCOOHCH3OH氧氧化化- -1 1氧氧化化芐芐位位氧氧化化布布洛洛芬芬NHSNHCH3OONHSNHCH3OOOHOOOO醋磺己脲醋磺己脲CH3OHNNH2CH3CH3OHNNCH3CH3CH3CH3OHNNHCH3CH3對對中中樞樞神神經(jīng)經(jīng)系系統(tǒng)統(tǒng)的的毒毒副副作作用用較較大大利利多多卡卡因因NNCH3CH3NNHCH3丙丙米米嗪嗪地地昔昔帕帕明明活活性性代代謝謝產(chǎn)產(chǎn)物物OH3COOHN CH3OHOOHN CH

3、3可可待待因因嗎嗎啡啡NNNHNNNNHNSCH3SH6 6- -甲甲硫硫嘌嘌呤呤H3CNHHNCH3OSOH3CNHHNCH3OOOH3CH3C硫硫噴噴妥妥HNNSHNHNCH3CH3NCNHNNSHNHNCH3CH3NCNO西西咪咪替替丁丁RNO2RNONHOHR NH2ROOHOHOHOHCOOHOOHOOHOHCOOHP POHNHHNOOHHXR藥藥物物OOHOHOHCOOHXRU UD DP P- -葡葡醛醛酸酸轉(zhuǎn)轉(zhuǎn)移移酶酶OHOHO-O-OO+UDP葡葡萄萄糖糖醛醛酸酸尿尿苷苷- -5 5- -二二磷磷酸酸- - - -D D- -葡葡醛醛酸酸( (U UD DP PG GA A

4、) )（葡葡萄萄糖糖醛醛酸酸的的活活化化形形式式）HNgluH2NO2SNNS-gluOHn-C3H7 磺胺-N-葡萄糖醛酸苷 丙基硫氧嘧啶-S-葡萄糖醛酸苷 沙丁胺醇硫酸酯 異丙腎上腺素硫酸酯HNHOOOHSHOOOH3CCH3CH3HNHOOOHSHOOOCH3CH3RCOOH + ATP + CoARCO-S-CoA +AMP乙乙酰酰合合成成酶酶RCO-S-CoA + RNH2RCO-NHR + CoASHN N- -酰酰基基轉(zhuǎn)轉(zhuǎn)移移酶酶R = -CH2COOH甘甘氨氨酸酸R = -CH(CH2CH2CONH2)COOH 谷谷氨氨酰酰胺胺?；o酶A藥物氨基酸?；o酶A（活化）N N- -脫脫烷