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抗精神病药物对人脑受体的亲和力及其在预测不良反应中的应用。

Neuroleptic affinities for human brain receptors and their use in predicting adverse effects.

作者信息

Richelson E

出版信息

J Clin Psychiatry. 1984 Aug;45(8):331-6.

PMID:6146602
Abstract

Affinities of some antipsychotic drugs for 5 human brain receptors (dopamine D-2, muscarinic acetylcholine, histamine H1, alpha 1-adrenergic, and alpha 2-adrenergic receptors) were obtained using radioligand binding techniques. Seventeen drugs were studied at the D-2 receptor; 15 at the remaining receptors. These drugs showed marked differences in affinities at most receptors, and these differences may help explain variations in their propensities to cause certain adverse effects in patients. The clinical efficacy of all neuroleptics appears to be equal. Thus, these differences allow the clinician to choose drugs with low affinity for certain receptors and, thereby, minimize some of the adverse effects of these drugs in patients.

摘要

利用放射性配体结合技术获得了一些抗精神病药物对5种人脑受体(多巴胺D-2、毒蕈碱型乙酰胆碱、组胺H1、α1-肾上腺素能和α2-肾上腺素能受体)的亲和力。对17种药物进行了D-2受体研究;对其余受体研究了15种药物。这些药物在大多数受体上显示出明显的亲和力差异,这些差异可能有助于解释它们在患者中引起某些不良反应倾向的变化。所有抗精神病药物的临床疗效似乎相当。因此,这些差异使临床医生能够选择对某些受体亲和力低的药物,从而将这些药物对患者的一些不良反应降至最低。

相似文献

1
Neuroleptic affinities for human brain receptors and their use in predicting adverse effects.抗精神病药物对人脑受体的亲和力及其在预测不良反应中的应用。
J Clin Psychiatry. 1984 Aug;45(8):331-6.
2
Pharmacology of neuroleptics in use in the United States.美国正在使用的抗精神病药物的药理学。
J Clin Psychiatry. 1985 Aug;46(8 Pt 2):8-14.
3
Interactions of neuroleptic metabolites with dopaminergic, alpha adrenergic and muscarinic cholinergic receptors.抗精神病药物代谢物与多巴胺能、α肾上腺素能和毒蕈碱胆碱能受体的相互作用。
J Pharmacol Exp Ther. 1981 Apr;217(1):81-6.
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[Neuroleptics in geriatrics. Pharmacological criteria for a responsible choice and a correct use].[老年医学中的抗精神病药物。合理选择与正确使用的药理学标准]
Tijdschr Gerontol Geriatr. 1984 Apr;15(2):73-80.
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Neuroleptic binding to human brain receptors: relation to clinical effects.抗精神病药物与人类大脑受体的结合:与临床效果的关系。
Ann N Y Acad Sci. 1988;537:435-42. doi: 10.1111/j.1749-6632.1988.tb42125.x.
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[Profile of the adverse effects of neuroleptic drugs in relation to its receptor binding].
Nord Med. 1987;102(4):120-3.
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Affinity of cyamemazine metabolites for serotonin, histamine and dopamine receptor subtypes.氰美马嗪代谢物对5-羟色胺、组胺和多巴胺受体亚型的亲和力。
Eur J Pharmacol. 2008 Jan 14;578(2-3):142-7. doi: 10.1016/j.ejphar.2007.09.025. Epub 2007 Oct 2.
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Antipsychotic drugs: prediction of side-effect profiles based on neuroreceptor data derived from human brain tissue.抗精神病药物:基于源自人脑组织的神经受体数据预测副作用概况。
Mayo Clin Proc. 1987 May;62(5):369-72. doi: 10.1016/s0025-6196(12)65440-8.
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Amitriptylinoxide: receptor-binding profile compared with other antidepressant drugs.氧化阿米替林:与其他抗抑郁药物相比的受体结合情况
Pharmacopsychiatry. 1985 Sep;18(5):314-9. doi: 10.1055/s-2007-1017388.
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Relative affinities for different classes of neurotransmitter receptors predict neuroleptic efficacy in infantile autism: a hypothesis.不同类型神经递质受体的相对亲和力预测婴儿自闭症的抗精神病药物疗效:一项假说。
Neuropsychobiology. 1986;15(3-4):160-4. doi: 10.1159/000118260.

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