受体药理学.ppt
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1、非典型抗精神病药物的 受体药理学,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,2,精神分裂症的神经生化假说,多巴胺(DA)假说(经典假说) 5HT假说 谷氨酸假说,多巴胺神经元的解剖定位,定位 DA神经束起源 DA神经束支配 病理生理功能 A16 嗅球 嗅束 嗅觉 A12-14 下丘脑 内侧隆起 通过释放催乳素释放抑制因子 弓状核 结节漏斗束 刺激催乳素的释放 室旁核 通过门循环传导 A 10 室被盖区 伏隔核 / 抗精神病作用 (或 Tsai 区 ) 通过中脑肢体
2、皮质 / 皮质DA束 A 9 黑质 尾状核 锥体外系症状 通过黑质纹状体 DA束 A 4 化学受体调控区 呕吐中枢 抑制呕吐 A 1 脊髓,c,多巴胺通路,下丘脑,中脑-边缘系 阳性症状 阴性症状 中脑-皮层 心境症状 认知症状 黑质-纹状体 EPS 结节-漏斗 催乳素,D2 受体拮抗,J Clin Psych 1998(16) (monograph),2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,6,D2 受体占有率可预测EPS或静坐不能,有 EPS或静坐不能,占有
3、率 78 % 患者没有EPS/静坐不能症状,D2 受体占有率,78 %,Individual Subjects,From: Kapur et al. Am J Psychiatry, 2000,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,7,氟哌啶醇治疗患者的D2受体占有率 与临床疗效、催乳素浓度及EPS症状的关系,30 40 50 60 70 80 90 D2 受体占有率 (%),100 80 60 40 20 0,临床疗效、催乳素浓度及EPS,65 72 78,
4、临床疗效需要 65% 高催乳素血症72% EPS78%的D2受体占有.,Adapted from: Kapur et al, Am J Psychiatry, 2000; 514-520,非典型抗精神病药物的分类,拮抗5-HT2/D2 抗精神病药物(又称第二代) (由氟哌啶醇衍生而来) 利培酮 寿廷多 齐哌西酮 多受体抗精神病药物(又称第三代) (氯氮平 及其相关药物) 氯氮平 再普乐 奎硫平 From: Shen WW, Annales of Clinical Psychiatry 1999; 11: 3: 145-157,Maguire G. Journal of Clinical Psy
5、chiatry. 2002. 63 (Suppl 4): 56-62.,抗精神病药的新分类,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,10,与其它抗精神病药相比, 再普乐和氯氮平具有广谱受体结合特点,再普乐,氯氮平,氟哌啶醇,氯丙嗪,利培酮,奎硫平,齐哌西酮,D1 D2 D4 5HT2A 5HT2C,毒蕈碱 1肾上腺素能 2肾上腺素能 Hist,H1,Data from: Bymaster FP, et al. Unpublished observations.
6、1996. Schotte A, et al. Psychopharmacology(Berl.). 1996;124(1-2):57-73.,再普乐,氯氮平,氟哌啶醇,氯丙嗪,利培酮,奎硫平,齐哌西酮,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,11,N=C,N,CH3,H,N,N,CH3,S,Cl,Clozapine/Olanzapine,2019/8/11 File name/location,Company Confidential Copyright 20
7、00 Eli Lilly and Company,12,N=C,N,OH,O,Clozapine/Quetiapine,N,NS,1,2,3,4,5,6,7,8,9,1,4,5,6,2,3,Cl,H,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,13,N=C,N,OH,O,Quetiapine,N,S,1,2,3,4,5,6,7,8,9,1,4,5,6,2,3,2019/8/11 File name/location,Company Confidential Copy
8、right 2000 Eli Lilly and Company,14,Risperidone,N,O,F,C H2,C H2,N,N,N,=,O,H2 C,*9,*,*7,=*,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,15,N,F,N,C,C,N,O,N,Cl,Sertindole,*=,5,4,*,*,2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and
9、Company,16,Ziprasidone,N,N,Cl,N,S,C,C,N,O,*,*,解释非典型抗精神病药物“非典型” 假说, 5-HT2/D2 比率假说 (Meltzer HY et al. 1989) D4/D2比率假说 (Seeman et al., 1994; Seeman et al., 1997) D2快速解离假说 (Kapur and Seeman, 2001),2019/8/11 File name/location,Company Confidential Copyright 2000 Eli Lilly and Company,18,100- 90- 80- 70-
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