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喹哌嗪的抗伤害感受作用:与中枢5-羟色胺能受体刺激的关系。

Antinociceptive action of quipazine: relation to central serotonergic receptor stimulation.

作者信息

Samanin R, Bernasconi S, Quattrone A

出版信息

Psychopharmacologia. 1976 Mar 16;46(2):219-22. doi: 10.1007/BF00421395.

DOI:10.1007/BF00421395
PMID:181775
Abstract

Quipazine, a serotonin receptor stimulant, inhibited the response of rats to painful stimuli in two methods currently used to measure antinociception in these animals: the hot plate and tail compression test. The antinocicptive action was observed with doses ranging from 5 to 20 mg/kg i.p according to the test situation. The effect was significantly antagonized by a pretreatment with methergoline, a potent serotonin antagonist. An electrolytic lesion placed in the nucleus raphe medianus, which produced a marked decrease of serotonin in the forebrain did not, or only slightly, affected the effect of quipazine, depending on the method used to measure antinociception. It is suggested that quipazine can produce antinociceptive action in rats by interacting with a serotonergic mechanism. The action appears to be due mainly to a direct action on postsynaptic serotonin receptors, although a presynaptic component can also contribute to the effect of quipazine.

摘要

喹哌嗪是一种血清素受体兴奋剂,在目前用于测量这些动物抗伤害感受的两种方法中,即热板法和尾部压迫试验中,它抑制了大鼠对疼痛刺激的反应。根据试验情况,腹腔注射5至20毫克/千克的剂量时可观察到抗伤害感受作用。用强效血清素拮抗剂麦角新碱预处理可显著拮抗该作用。在前脑血清素显著减少的中缝正中核放置电解损伤,根据用于测量抗伤害感受的方法不同,对喹哌嗪的作用没有影响或仅有轻微影响。提示喹哌嗪可通过与血清素能机制相互作用在大鼠中产生抗伤害感受作用。该作用似乎主要是由于对突触后血清素受体的直接作用,尽管突触前成分也可能对喹哌嗪的作用有贡献。

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Antinociceptive action of quipazine: relation to central serotonergic receptor stimulation.喹哌嗪的抗伤害感受作用:与中枢5-羟色胺能受体刺激的关系。
Psychopharmacologia. 1976 Mar 16;46(2):219-22. doi: 10.1007/BF00421395.
2
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Brain Res. 1990 May 7;515(1-2):155-62. doi: 10.1016/0006-8993(90)90590-8.
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Pharmacol Biochem Behav. 1977 Mar;6(3):325-9. doi: 10.1016/0091-3057(77)90032-6.

引用本文的文献

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Br J Clin Pharmacol. 1983 Nov;16(5):471-5. doi: 10.1111/j.1365-2125.1983.tb02202.x.
3
Metergoline elevates or reduces nociceptive thresholds in mice depending on test method and route of administration.

本文引用的文献

1
The effect of lowering the 5-hydroxytryptamine content of the rat spinal cord on analgesia produced by morphine.降低大鼠脊髓5-羟色胺含量对吗啡产生的镇痛作用的影响。
J Physiol. 1974 Jan;236(2):483-98. doi: 10.1113/jphysiol.1974.sp010448.
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EVIDENCE FOR THE EXISTENCE OF MONOAMINE-CONTAINING NEURONS IN THE CENTRAL NERVOUS SYSTEM. I. DEMONSTRATION OF MONOAMINES IN THE CELL BODIES OF BRAIN STEM NEURONS.中枢神经系统中含单胺神经元存在的证据。I. 脑干神经元细胞体中单胺的证实。
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Studies on central nervous system depressants. (III). Influence of some tranquillizing agents on morphine analgesia.
根据测试方法和给药途径的不同,麦角苄酯可提高或降低小鼠的痛觉阈值。
Psychopharmacology (Berl). 1984;82(4):306-9. doi: 10.1007/BF00427675.
4
Antagonistic properties of quipazine at presynaptic serotonin receptors and alpha-adrenoceptors in rat brain cortex slices.喹哌嗪对大鼠大脑皮层切片中突触前5-羟色胺受体和α-肾上腺素能受体的拮抗特性。
Naunyn Schmiedebergs Arch Pharmacol. 1981 Nov;317(3):204-8. doi: 10.1007/BF00503817.
5
Enhanced behavioural, electrocortical and hyperthermic effects of serotonin-like agents after impairment of serotonin transmission in fowl brain.禽类大脑中5-羟色胺传递受损后,类5-羟色胺药物的行为、皮层电活动及体温升高效应增强。
Naunyn Schmiedebergs Arch Pharmacol. 1980 Jul;312(3):229-34. doi: 10.1007/BF00499151.
6
Therapeutic implications of modifying endogenous serotonergic analgesic systems.调节内源性血清素能镇痛系统的治疗意义。
Anesth Prog. 1985 Jan-Feb;32(1):19-22.
7
The role of 5HT1A receptors in the modulation of the acoustic startle reflex in rats.5-羟色胺1A受体在调节大鼠听觉惊吓反射中的作用。
Psychopharmacology (Berl). 1989;97(4):507-13. doi: 10.1007/BF00439556.
8
Alterations of cerebrospinal fluid 5-hydroxyindoleacetic acid, and total blood serotonin content during clozapine treatment.氯氮平治疗期间脑脊液5-羟吲哚乙酸及全血血清素含量的变化
Psychopharmacology (Berl). 1978 Mar 1;56(2):195-8. doi: 10.1007/BF00431849.
9
Evidence for a receptor supersensitivity following impairment of central serotoninergic activity in the rabbit.家兔中枢5-羟色胺能活性受损后受体超敏反应的证据。
Naunyn Schmiedebergs Arch Pharmacol. 1979 Nov;309(2):125-9. doi: 10.1007/BF00501219.
中枢神经系统抑制剂的研究。(III)。某些镇静剂对吗啡镇痛作用的影响。
Arch Int Pharmacodyn Ther. 1963 Jan 1;141:223-32.
4
Synthetic analgesics. II. Dithienylbutenyl- and dithienylbutylamines.合成镇痛药。II. 二噻吩基丁烯基胺和二噻吩基丁胺。
J Pharmacol Exp Ther. 1953 Mar;107(3):385-93.
5
Similarities between the pharmacological actions of quipazine and serotonin.喹哌嗪与血清素药理作用之间的相似性。
Eur J Pharmacol. 1969;6(3):274-80. doi: 10.1016/0014-2999(69)90185-x.
6
Antagonism of the analgesic effect of morphine and other drugs by p-chlorophenylalanine, a serotonin depletor.对氯苯丙氨酸(一种血清素耗竭剂)对吗啡及其他药物镇痛作用的拮抗作用。
Psychopharmacologia. 1968;12(4):278-85. doi: 10.1007/BF00401407.
7
Increased serotonin turnover in the acutely morphine treated rat.急性吗啡处理的大鼠中血清素周转率增加。
Life Sci I. 1971 Sep 1;10(17):977-83. doi: 10.1016/0024-3205(71)90255-4.
8
Quipazine, a new type of antidepressant agent.喹哌嗪,一种新型抗抑郁药。
Psychopharmacologia. 1971;21(1):89-100. doi: 10.1007/BF00404000.
9
Reduced effect of morphine in midbrain raphe lesioned rats.中脑缝际核损伤大鼠中吗啡作用减弱。
Eur J Pharmacol. 1970;10(3):339-43. doi: 10.1016/0014-2999(70)90205-0.
10
Evaluation of the peripheral and central antagonistic activities against 5-hydroxytryptamine of some new agents.某些新型药物对5-羟色胺的外周和中枢拮抗活性评估。
Br J Pharmacol. 1970 May;39(1):223P-224P.