1、苯二氮卓類NNR4123456791/2/3/4/5/6/ABCR1O8R2R3NNClNHCH3O氯氮卓NNClCH3O地西泮NR1NOR3R1=H, R2=H, R3=NO2, 硝西泮R1=H, R2=Cl, R3=NO2,氯硝西泮R1=(CH2)2N(C2H5)2, R2=F, R3=Cl 氟西泮R2NHNOClOHR1R1 = H 奧沙西泮R1 = Cl 勞拉西泮NNSClFCH2CF3夸西泮NNClFNH3C咪達唑倫NHNOBrOF鹵f唑侖SNNNNCH3 依替唑倫ClCH3NNNClR2NR1R1=H R2=H 艾司唑倫R1=CH3 R2=H 阿普唑倫R1=CH3 R2=Cl 三唑

2、倫NNClCH3O地西泮NNClCH3ONNClCH3OHHHHabNNClCH3ONNClCH3OHCH3CH3HSR穩定,活性強NNOClCH3diazepanNHNOClOH4hydroxydesoxydemoxepamNHNOClnordazepamNHNOClOH9-hydroxydesoxydemoxepamNHNOClOHoxazepamNNCH3OCl（CH3)2SO4CH3C6H5Fe , HClC2H5OHClON3-苯-5-氯嗯呢ClON+CH3ClNHCH3OClCH2COClC6H12ClNCOCH2ClOCH3NNCH3OCl(CH2)6N4.HClCH3OHIII

3、NHNOCl2) NaNO2, HCl3)-萘酚ClNONHO1)H+NNCH3OClH+OH-ClNHCH3O+ H2NCH2COOH2-甲氨基-5-氯-二苯甲酮ONCH3OClNH2H+NNHCH3ClCOOHNHNOR2 R2=H, R3=NO2, 硝西泮 R2=Cl, R3=NO2,氯硝西泮R1NNNClR2NR1R1=H R2=H 艾司唑倫R1=CH3 R2=H 阿普唑倫R1=CH3 R2=Cl 三唑倫NNClFNH3C咪達唑倫NNCH3OClNH2NCH3OClOClNOCH3NHNH2OONH2Ro7355肽酶前藥Ro7355NNNClNHNNNClNHONNClNHH+NH3+

4、NNCH3H3CN(CH3)2ONNNONN CH3NClOCOHNNHOOO124563R1R2HNNHOOONNHOOHONNOHOHONNOHOHHO巴比妥酸單內酰亞胺雙內酰亞胺三內酰亞胺124563HNNHOOO124563R1R2R3NNHOXO124563R1R2名稱名稱pKa分子態藥物分子態藥物離子態藥物離子態藥物巴比妥酸巴比妥酸4.120.0599.955-苯基巴比妥苯基巴比妥酸酸3.750.0299.98苯巴比妥苯巴比妥7.2943.7056.30海索比妥海索比妥8.4090.919.09HNNHOOO124563R1R2NHNHC6H5C2H5OOONHNHC2H5OOOH

5、ONHNHC2H5OOONHNHC2H5OOOOHNHNHR1R2OOOCHCNHCNH2R1R2OOCR1R2CONH2CONH2NHNHC2H5OSOH3CNHNHC2H5OOOH3CNNHH3COOOCH3NHNHH3COOONHNHR1R2OO(S)OH2CCOOC2H5COOC2H5R1XC2H5ONa CHCOOC2H5COOC2H5R1R2XC2H5ONa CCOOC2H5COOC2H5R1R2NHNHR1R2OO(S)OH2NCNH2C2H5ONaO(S)IIIIIINNHOOONaR1R2CHCONHCONH2R1R2+ NaHCO3CHCOONa + NH3R1R2室溫NH

6、NHC6H5C2H5OOONHNHC6H5C2H5OOOC6H5CH2COOC2H5COOC2H5COOC2H5C2H5ONa CHCOCOOC2H5COOC2H5C6H5CO CHCOOC2H5COOC2H5C6H5C2H5BrC2H5ONa CCOOC2H5COOC2H5C6H5C2H5H2NCONH2C2H5ONaHClNHNHC6H5C2H5OOOIIIIIICHOHOHCl3C 水合氯醛安全的催眠、抗驚厥藥代謝CH2OHCl3CCH2OPO3H2Cl3C三氯乙醇膦酸酯CHNHCOOC2H5Cl3C氨基甲酸乙酯水合氯醛OH三氯乙醇活性前藥CCH2OCONH2CH2OCONH2H3CCH

7、3CH2CH2NNCH3OH3CNHNHC6H5C2H5OO撲米酮（撲癇酮） NHNHC6H5C2H5OOO苯巴比妥NHNHC6H5C6H5OO苯妥英ONH3CH3COOCH3 三甲雙酮 毒性大（f唑烷雙酮類） 失神性小發作NHC2H5H3COO 乙琥胺（丁二酰亞胺類） 癲癇小發作NHNHC6H5C2H5OO5-乙基-5-苯基-乙內酰脲 毒性大生物電子等排v抑制大腦皮層運動中樞，提高驚厥的閾值。NHNC6H5C6H5OONa135NHNC6H5C6H5OONaNHCONH2COOHC6H5C6H5NH2COOHC6H5C6H5NaOH+ NH3NHNC6H5C6H5OONaNHNHC6H5OO

8、HONHNHC6H5OOGluONHCONH2COOHC6H5C6H5+NH2COOHC6H5C6H5NNClCH3OONCONH2NCONH2NCONH2ONCONH2OHOH環氧化物酶卡馬西平CYP450CHCORCH3CH2CH2CH3CH2CH2R = HR=ONaR = NH2丙戊酸丙戊酸鈉丙戊酰胺H2NOHOv作用機理可能是通過抑制腦內興奮性介質谷氨酸和天門冬氨酸的過量釋放，產生抗癲癇作用。NNNClClNH2紋狀體中NSCH2CH2CH2NRRRNSCH2CHN(CH3)2CH3異丙嗪NSCH2CH2CH2N(CH3)2Cl12345678910氯丙嗪 NSCH2CH2CH2R1

9、R2NNCH2CH2OHNNCH3NNCH2CH2OHClCF3CF3 奮乃靜氟奮乃靜 三氟拉嗪NSCH2CH2CH2CF3NNCH2CH2OCOC6H13氟奮乃靜庚酸酯23周注射一次 R1 R2N(CH3)2 COCH3 乙乙酰酰丙丙嗪嗪N(CH3)2 CF3 三三氟氟丙丙嗪嗪1045013NHRSI2NHSR+NHSR少量NaNH2Cl(CH2)3NR2/NSCH2CH2CH2NR2/ClNSCH2CH2CH2NRRRNSCH2CH2CH2N(CH3)2.HClClNSCH2CH2CH2ClNNCH2CH2OHXRCl -N(CH3)2 氯普噻噸CF3NNCH2CH2OH氟哌噻噸Cl 珠氯

10、噻醇NNCH2CH2OHNSCH2CH2CH2RXSCHCH2CH2RXNCOOC2H5H3C哌替啶FCO(CH3)3NR1R2123456R1 OH OHR2ClCF3氟哌啶醇三氟哌多NNNOFCO(CH2)3氟哌利多廣泛用于治療急、慢性精神分裂癥和躁狂癥RCO(CH2)3NR1R2急、慢性FCO(CH2)3NOHCl234561FCO(CH2)3NOHClFCO(CH2)2CHOFCO(CH2)2COOHFCH(CH2)3NOHClOHFCH(CH2)2CHOOHFCH(CH2)2COOHOHFCO(CH3)3NR1R2123456FCH(CH2)3NR2R1FR1 HNNHOR2匹莫齊特

11、Cl五氟利多OHCF3NHNC6H5O 氟司必林一天一次 兩周一次 一周一次H2NO2SCONHCH2OCH3NC2H5NNHNNCH3Cl二苯并氧氮卓類，和氯丙嗪、氟哌啶醇一樣能阻斷紋狀體多巴胺受體，因而臨床應用、療效及不良反應相似，也可導致NONNCH3ClNNOONNNNSCH2CH2CH2NRRRN(CH2)3NRRRN(CH2)3NRRR 丙咪嗪類抗抑郁作用增強N(CH2)3NRCH3R CH3 丙咪嗪Cl H 地昔帕明作用快，副作用小NONHNClNSCH2CH2CH2NRRRN(CH2)3NRRR丙咪嗪SCH2CH2CH2RXCH(CH2)2NRCH3R=CH3 阿米替林 R=H 去甲替林拼合原理CH(CH2)2N(CH3)2.HCl1234567891011a