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3H-螺哌啶醇与大鼠纹状体膜中多巴胺受体的结合：洛沙平及其羟基化代谢产物的影响。

3H-Spiroperidol binding to dopamine receptors in rat striatal membranes: influence of loxapine and its hydroxylated metabolites.

作者信息

Coupet J, Rauh C E

出版信息

Eur J Pharmacol. 1979 Apr 15;55(2):215-8. doi: 10.1016/0014-2999(79)90396-0.

DOI:10.1016/0014-2999(79)90396-0
PMID:456420
Abstract

The effects of loxapine and its hydroxylated metabolites 7-hydroxyloxapine and 8-hydroxyloxapine on 3H-spiroperidol binding to rat striatal membranes were investigated. Whereas 7-hydroxyloxapine and loxapine displayed strong affinities for 3H-spiroperidol binding sites, 8-hydroxyloxapine was essentially inactive. The potency of 7-hydroxyloxapine to displace 3H-spiroperidol is 1.5 times and 8 times those of haloperidol and chlorpromazine, respectively. These results suggest that the combined effects of loxapine and 7-hydroxyloxapine on the postsynaptic dopamine receptors in the brain may explain the clinical efficacy of loxapine in the treatment of schizophrenia.

摘要

研究了洛沙平及其羟基化代谢产物7-羟基洛沙平和8-羟基洛沙平对3H-螺哌啶醇与大鼠纹状体膜结合的影响。7-羟基洛沙平和洛沙平对3H-螺哌啶醇结合位点表现出强亲和力，而8-羟基洛沙平基本无活性。7-羟基洛沙平取代3H-螺哌啶醇的效力分别是氟哌啶醇和氯丙嗪的1.5倍和8倍。这些结果表明，洛沙平和7-羟基洛沙平对脑中突触后多巴胺受体的联合作用可能解释了洛沙平治疗精神分裂症的临床疗效。

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1
3H-Spiroperidol binding to dopamine receptors in rat striatal membranes: influence of loxapine and its hydroxylated metabolites.3H-螺哌啶醇与大鼠纹状体膜中多巴胺受体的结合：洛沙平及其羟基化代谢产物的影响。
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Loxapine and clozapine decrease serotonin (S2) but do not elevate dopamine (D2) receptor numbers in the rat brain.洛沙平与氯氮平可降低大鼠脑中5-羟色胺（S2）水平，但不会提高多巴胺（D2）受体数量。
Psychiatry Res. 1984 Aug;12(4):277-85. doi: 10.1016/0165-1781(84)90044-1.

引用本文的文献

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Int J Mol Sci. 2017 Feb 8;18(2):349. doi: 10.3390/ijms18020349.
2
Multiple dose pharmacokinetics of inhaled loxapine in subjects on chronic, stable antipsychotic regimens.接受慢性稳定抗精神病药物治疗方案的受试者吸入洛沙平的多剂量药代动力学
J Clin Pharmacol. 2015 Sep;55(9):985-94. doi: 10.1002/jcph.502. Epub 2015 May 6.
3
Loxapine inhalation powder: a review of its use in the acute treatment of agitation in patients with bipolar disorder or schizophrenia.
洛沙平吸入粉：在双相情感障碍或精神分裂症患者急性治疗激越中的应用评价。
CNS Drugs. 2013 Jun;27(6):479-89. doi: 10.1007/s40263-013-0075-9.
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Psychopharmacology (Berl). 2003 May;167(3):315-23. doi: 10.1007/s00213-003-1418-x. Epub 2003 Mar 28.
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A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes.洛沙平抗精神病活性的神经化学基础：与多巴胺D1、D2、D4及5-羟色胺5-HT2受体亚型的相互作用
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