一种估计抗精神病药物体内D2受体占有率的方法。
A method to estimate in vivo D2 receptor occupancy by antipsychotic drugs.
作者信息
Roemer R A, Richelson E, Shagass C, Leventhal L
机构信息
Department of Psychiatry and Behavioral Science, Temple University, School of Medicine, Philadelphia, Pennsylvania, USA.
出版信息
J Psychiatry Neurosci. 1996 Nov;21(5):325-33.
Abstract
A computational method is presented to estimate in vivo receptor occupancies of frequently used antipsychotic medications, which may provide a way to determine their central nervous system (CNS) effects in humans. The method can be used to estimate occupancies of several receptor types based on the daily dose of antipsychotic medication. Estimates of D2 receptor occupancy by haloperidol based on this equation were compared with those yielded by positron emission tomography (PET) measures in humans for the same compounds and dosages: the results of this comparison validated the approach.
摘要
本文提出了一种计算方法，用于估计常用抗精神病药物的体内受体占有率，这可能为确定其对人类中枢神经系统（CNS）的影响提供一种方法。该方法可根据抗精神病药物的每日剂量来估计几种受体类型的占有率。基于此方程计算出的氟哌啶醇对D2受体的占有率，与采用正电子发射断层扫描（PET）测量相同化合物和剂量的人体结果进行了比较：该比较结果验证了该方法。
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本文引用的文献
1
Auditory P300 abnormalities and left posterior superior temporal gyrus volume reduction in schizophrenia.精神分裂症患者的听觉P300异常及左侧颞上回后部体积减小
Arch Gen Psychiatry. 1993 Mar;50(3):190-7. doi: 10.1001/archpsyc.1993.01820150036003.
2
Effects of metabolic perturbation on plasma homovanillic acid in schizophrenia. Relationship to prefrontal cortex volume.代谢紊乱对精神分裂症患者血浆高香草酸的影响。与前额叶皮质体积的关系。
Arch Gen Psychiatry. 1993 Jul;50(7):541-50. doi: 10.1001/archpsyc.1993.01820190043005.
3
Affinity of neuroleptics for D1 receptor of human brain striatum.抗精神病药物对人脑纹状体D1受体的亲和力。
J Psychiatry Neurosci. 1994 Jul;19(4):265-9.
4
Serum concentrations of thioridazine, its major metabolites and serum neuroleptic-like activities in schizophrenics with and without tardive dyskinesia.
Acta Psychiatr Scand. 1982 Oct;66(4):294-305. doi: 10.1111/j.1600-0447.1982.tb00308.x.
5
Correlation of thiothixene serum levels and age.硫利达嗪血清水平与年龄的相关性。
Psychopharmacology (Berl). 1981;74(2):170-2. doi: 10.1007/BF00432687.
6
Fluphenazine pharmacokinetics and therapeutic response.氟奋乃静的药代动力学与治疗反应。
Psychopharmacology (Berl). 1981;73(3):205-10. doi: 10.1007/BF00422403.
7
Haloperidol. Plasma levels and prolactin response as predictors of clinical improvement in schizophrenia: chemical v radioreceptor plasma level assays.氟哌啶醇。血浆水平和催乳素反应作为精神分裂症临床改善的预测指标：化学法与放射受体血浆水平测定法
Arch Gen Psychiatry. 1984 Nov;41(11):1044-9. doi: 10.1001/archpsyc.1983.01790220034006.
8
Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro.抗精神病药物对正常人脑体外神经递质受体的拮抗作用。
Eur J Pharmacol. 1984 Aug 17;103(3-4):197-204. doi: 10.1016/0014-2999(84)90478-3.
9
Radioimmunoassays for phenothiazine drugs and their major metabolites in plasma.
Prog Neuropsychopharmacol Biol Psychiatry. 1983;7(4-6):709-14. doi: 10.1016/0278-5846(83)90050-7.
10
Serum neuroleptic levels in the maintenance treatment of schizophrenia.精神分裂症维持治疗中的血清抗精神病药物水平
Psychopharmacol Bull. 1983;19(1):76-8.
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