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马吲哚性厌食症是由多巴胺能机制的激活介导的。

Mazindol anorexia is mediated by activation of dopaminergic mechanisms.

作者信息

Kruk Z L, Zarrindast M R

出版信息

Br J Pharmacol. 1976 Nov;58(3):367-72.

PMID:990591
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1667599/
Abstract

1 Anorexia in rats following injections of mazindol (0.1-8 mg/kg i.p.) could be antagonized by pretreatment with a dopamine receptor blocker (primozide) but not by pretreatment with an alpha-adrenoceptor blocker (phenoxybenzamine), a beta-adrenoceptor blocker ((-)-propranolol), or a 5-hydroxytryptamine receptor blocker (methergoline). 2 In rats with a unilateral lesion in the substantia nigra made by stereotaxic injection of 6-hydroxydopamine, mazindol caused a dose-dependent turning towards the lesioned side, indicating an indirect mechanism of action. This effect could be antagonized by pretreatment with a dopamine receptor blocker. 3 In rats pretreated with reserpine and alpha-methyl-p-tyrosine, mazindol did not have any motor stimulant action. 4 In vitro studies with synaptosomes prepared from rat brain, indicated that mazindol blocks uptake and causes release of dopamine. 5 It is concluded that the anorectic action of mazindol is mediated by a dopaminergic mechanism.

摘要
  1. 腹腔注射吗吲哚(0.1 - 8毫克/千克)后大鼠出现的厌食症状,可被多巴胺受体阻断剂(丙酰奋乃静)预处理拮抗,但不能被α-肾上腺素能受体阻断剂(酚苄明)、β-肾上腺素能受体阻断剂((-)-普萘洛尔)或5-羟色胺受体阻断剂(麦角新碱)预处理拮抗。2. 在通过立体定位注射6-羟基多巴胺造成单侧黑质损伤的大鼠中,吗吲哚引起剂量依赖性地转向损伤侧,表明其作用机制为间接机制。该效应可被多巴胺受体阻断剂预处理拮抗。3. 在接受利血平和α-甲基对酪氨酸预处理的大鼠中,吗吲哚没有任何运动兴奋作用。4. 用大鼠脑制备的突触体进行的体外研究表明,吗吲哚可阻断多巴胺摄取并导致其释放。5. 得出结论,吗吲哚的厌食作用是由多巴胺能机制介导的。

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1
Mazindol anorexia is mediated by activation of dopaminergic mechanisms.马吲哚性厌食症是由多巴胺能机制的激活介导的。
Br J Pharmacol. 1976 Nov;58(3):367-72.
2
Behavioural effects of a new non-phenylethylamine anorexigenic agent: mazindol.
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The roles of brain noradrenaline and dopamine in the anorectic activity of diethylpropion in rats: a comparison with d-amphetamine.脑去甲肾上腺素和多巴胺在大鼠中对二乙丙胺苯丙酮厌食活性的作用:与右旋苯丙胺的比较。
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引用本文的文献

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Dopamine-like properties of ephedrine in rat brain.麻黄碱在大鼠脑中的多巴胺样特性。
Br J Pharmacol. 1981 Sep;74(1):119-22. doi: 10.1111/j.1476-5381.1981.tb09962.x.
2
Satietin, a blood-borne anorectic glycoprotein, as the putative rate-limiting satiety signal in the negative feed-back of food intake.饱腹感素是一种通过血液传播的厌食性糖蛋白,被认为是食物摄入负反馈中假定的限速饱腹感信号。
Z Ernahrungswiss. 1984 Jun;23(2):85-103. doi: 10.1007/BF02021684.
3
Satietin; a 50,000 dalton glycoprotein in human serum with potent, long-lasting and selective anorectic activity.饱腹感素;一种存在于人体血清中的50000道尔顿糖蛋白,具有强效、持久且选择性的食欲抑制活性。
J Neural Transm. 1984;59(3):163-94. doi: 10.1007/BF01250007.
4
The anorectic action of mazindol.
Ir J Med Sci. 1978 Aug;147 Suppl 1:66-70. doi: 10.1007/BF02947908.
5
Food-intake and locomotor activity: effects of mazindol and spiperone [proceedings].食物摄入量与运动活动:马吲哚和螺哌隆的作用[会议论文集]
Br J Pharmacol. 1978 Jun;63(2):412P-413P.
6
Effects of morphine on uptake and release of dopamine in mouse and rat striatal synaptosomes [proceedings].吗啡对小鼠和大鼠纹状体突触体中多巴胺摄取和释放的影响[会议论文集]
Br J Pharmacol. 1978 Jun;63(2):386P.
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Effect of mazindol on brain dopamine turnover in spiperone-treated rats.
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8
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本文引用的文献

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1-Methyl-8-beta-carbobenzyloxy-aminomethyl-10-alpha-ergoline, a potent and long-lasting 5-hydroxytryptamine antagonist.1-甲基-8-β-苄氧羰基-氨甲基-10-α-麦角灵,一种强效且长效的5-羟色胺拮抗剂。
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Regional differences in H3-norepinephrine and H3-dopamine uptake into rat brain homogenates.大鼠脑匀浆中H3-去甲肾上腺素和H3-多巴胺摄取的区域差异。
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Receptor activity and turnover of dopamine and noradrenaline after neuroleptics.抗精神病药物治疗后多巴胺和去甲肾上腺素的受体活性及更新率
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A comparison of the capacities of isomers of amphetamine, deoxypipradrol and methylphenidate to inhibit the uptake of tritiated catecholamines into rat cerebral cortex slices, synaptosomal preparations of rat cerebral cortex, hypothalamus and striatum and into adrenergic nerves of rabbit aorta.对苯丙胺、脱氧哌甲酯和哌醋甲酯的异构体抑制氚标记儿茶酚胺摄取进入大鼠大脑皮层切片、大鼠大脑皮层、下丘脑和纹状体的突触体标本以及兔主动脉肾上腺素能神经的能力进行比较。
J Pharmacol Exp Ther. 1972 Jun;181(3):407-16.
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Clonidine induced intrahypothalamic stimulation of eating in rats.
Psychopharmacologia. 1972;25(2):162-8. doi: 10.1007/BF00423193.
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Dopamine and 5-hydroxytryptamine inhibit feeding in rats.
Nat New Biol. 1973 Nov 14;246(150):52-3. doi: 10.1038/newbio246052a0.
7
Role of monoamines in the anorexigenic actions of fenfluramine, amphetamine and p-chloromethamphetamine.单胺类物质在芬氟拉明、苯丙胺和对氯甲基苯丙胺的厌食作用中的作用。
Eur J Pharmacol. 1974 Aug;27(3):313-23. doi: 10.1016/0014-2999(74)90006-5.
8
Evidence for dopamine receptor stimulation by apomorphine.阿扑吗啡对多巴胺受体刺激作用的证据。
J Pharm Pharmacol. 1967 Sep;19(9):627-9. doi: 10.1111/j.2042-7158.1967.tb09604.x.
9
Mechanism of action of norepinephrine in eliciting an eating response on injection into the rat hypothalamus.去甲肾上腺素注入大鼠下丘脑引发进食反应的作用机制。
J Pharmacol Exp Ther. 1968 Apr;160(2):336-48.
10
Letter: Reduction of food intake by apomorphine: a pimozide-sensitive effect.信函:阿扑吗啡减少食物摄入量:一种对匹莫齐特敏感的效应。
J Pharm Pharmacol. 1973 Nov;25(11):909-11. doi: 10.1111/j.2042-7158.1973.tb09973.x.