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奋乃静:催乳素分泌刺激与抗精神病活性之间的关系。

Perlapine: relationship between stimulation of prolactin secretion and antipsychotic activity.

作者信息

Meltzer H Y, Fessler R G, Fang V S

出版信息

Psychopharmacology (Berl). 1977 Oct 20;54(2):183-6. doi: 10.1007/BF00426777.

DOI:10.1007/BF00426777
PMID:412213
Abstract

Perlapine is a dibenzohetereopine compound chemically related to clothiapine, loxapine, and clozapine. Although the latter three compounds are antipsychotic, perlapine has not been reported to be antipsychotic. Nevertheless, all four drugs increase rat plasma prolactin levels. The order of potency is loxapine, perlapine, clothiapine, and clozapine. These results suggest that either perlapine should be reexamined for antipsychotic properties or there are hitherto unsuspected discrepancies between the dopamine receptors relevant to antipsychotic activity in man and those that regulate prolactin secretion in the rat.

摘要

奋乃静是一种二苯并杂环庚烷化合物,在化学结构上与氯噻平、洛沙平和氯氮平相关。尽管后三种化合物具有抗精神病作用,但尚未有报道称奋乃静具有抗精神病作用。然而,这四种药物都会使大鼠血浆催乳素水平升高。其效力顺序为洛沙平、奋乃静、氯噻平、氯氮平。这些结果表明,要么应重新研究奋乃静的抗精神病特性,要么在与人类抗精神病活性相关的多巴胺受体和调节大鼠催乳素分泌的多巴胺受体之间存在迄今未被怀疑的差异。

相似文献

1
Perlapine: relationship between stimulation of prolactin secretion and antipsychotic activity.奋乃静:催乳素分泌刺激与抗精神病活性之间的关系。
Psychopharmacology (Berl). 1977 Oct 20;54(2):183-6. doi: 10.1007/BF00426777.
2
Effect of clozapine on dopamine-induced inhibition of prolactin release from cultured rat pituitary cells.氯氮平对多巴胺诱导的大鼠垂体培养细胞催乳素释放抑制作用的影响。
Pharmacol Res. 1997 Mar;35(3):173-5. doi: 10.1006/phrs.1996.0102.
3
Antipsychotic drugs stimulate prolactin release.抗精神病药物会刺激催乳素释放。
Psychopharmacologia. 1974;40(2):123-7. doi: 10.1007/BF00421361.
4
Perlapine and dopamine metabolism: prediction of antipsychotic efficacy.奋乃静与多巴胺代谢:抗精神病疗效的预测
Eur J Pharmacol. 1977 Jan 7;41(1):65-72. doi: 10.1016/0014-2999(77)90372-7.
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Effects of pirenperone and ketanserin on rat prolactin secretion in vivo and in vitro.匹仑哌隆和酮色林对大鼠体内外催乳素分泌的影响。
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Paradoxical effect of neuroleptic drugs on prolactin secretion by rat pituitary cell cultures.抗精神病药物对大鼠垂体细胞培养物催乳素分泌的矛盾效应。
Life Sci. 1999;65(14):1455-61. doi: 10.1016/s0024-3205(99)00386-0.
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Effects of clozapine and other dibenzo-epines on central dopaminergic and cholinergic systems. Structure-activity relationships.氯氮平及其他二苯并氮杂䓬类药物对中枢多巴胺能和胆碱能系统的作用。构效关系。
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The prolactin response in clinical psychiatry.临床精神病学中的催乳素反应。
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Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release.抗精神病药物SSR181507、阿立哌唑和比氟哌隆在多巴胺D2受体上的部分激动剂特性:G蛋白激活和催乳素释放。
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引用本文的文献

1
Atypical antidopaminergic properties of CI-686: a potential antipsychotic agent.CI-686的非典型抗多巴胺能特性:一种潜在的抗精神病药物。
Psychopharmacology (Berl). 1979;66(1):23-7. doi: 10.1007/BF00431984.

本文引用的文献

1
[Clinical and electroencephalographic effects of methoclopramide in psychiatry].甲氧氯普胺在精神病学中的临床及脑电图效应
Therapie. 1965 Jul-Aug;20(4):975-95.
2
3,4-dihydroxyphenylacetic acid and 4-hydroxy-3-methoxyphenylacetic acid in the mouse striatum: a reflection of intra- and extra-neuronal metabolism of dopamine?小鼠纹状体中的3,4-二羟基苯乙酸和4-羟基-3-甲氧基苯乙酸:多巴胺细胞内和细胞外代谢的反映?
Br J Pharmacol. 1971 Jul;42(3):343-51. doi: 10.1111/j.1476-5381.1971.tb07118.x.
3
Effects of central acting drugs on serum and pituitary prolactin levels in rats.
中枢作用药物对大鼠血清及垂体催乳素水平的影响。
Endocrinology. 1970 Oct;87(4):667-72. doi: 10.1210/endo-87-4-667.
4
Loxapine: a controlled evaluation in chronic schizophrenic patients.洛沙平:对慢性精神分裂症患者的对照评估。
Curr Ther Res Clin Exp. 1970 Sep;12(9):594-7.
5
Inhibition of rat prolactin release by apomorphine in vivo and in vitro.
Endocrinology. 1974 Jul;95(1):123-9. doi: 10.1210/endo-95-1-123.
6
The influence of surgery, time of day, blood volume reduction and anaesthetics on plasma prolactin in ovariectomized rats.手术、一天中的时间、血容量减少及麻醉对去卵巢大鼠血浆催乳素的影响。
J Endocrinol. 1974 Jul;62(1):75-83. doi: 10.1677/joe.0.0620075.
7
6-(4-Methyl-1-piperazinyl)morphanthridine (Perlapine), a new tricyclic compound with sedative and sleep-promoting properties. A pharmacological study.6-(4-甲基-1-哌嗪基)吗啉蒽啶(派拉平),一种具有镇静和助眠特性的新型三环化合物。药理学研究。
Psychopharmacologia. 1973 Feb 20;28(4):325-37. doi: 10.1007/BF00422753.
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Effects of haloperidol on serum and pituitary prolactin, LH and FSH, and hypothalamic PIF and LRF.
Neuroendocrinology. 1974;15(1):10-20. doi: 10.1159/000122288.
9
Hypothalamic control of prolactin secretion.下丘脑对催乳素分泌的控制。
Vitam Horm. 1972;30:165-221. doi: 10.1016/s0083-6729(08)60796-7.
10
Effects of serotonin precursors and melatonin on serum prolactin release in rats.血清素前体和褪黑素对大鼠血清催乳素释放的影响。
Endocrinology. 1973 Jul;93(1):152-5. doi: 10.1210/endo-93-1-152.