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促甲状腺激素释放激素的一种新类似物Nα-[(S)-4-氧代-2-氮杂环丁烷基]羰基-L-组氨酰-L-脯氨酰胺脱水物(YM-14673)对脊髓横断大鼠脊髓反射电位和屈肌反射的影响。

Effects of a new analog of thyrotropin-releasing hormone, N alpha-[(S)-4-oxo-2-azetidinyl) carbonyl]-L-histidyl-L-prolinamide dehydrate (YM-14673) on spinal reflex potentials and flexor reflexes in spinalized rats.

作者信息

Ono H, Nagano N, Yamada M, Fukuda H

机构信息

Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

出版信息

Neuropharmacology. 1990 Jan;29(1):69-74. doi: 10.1016/0028-3908(90)90085-6.

DOI:10.1016/0028-3908(90)90085-6
PMID:2106102
Abstract

Experiments were performed on spinalized rats, transected at the Cl level. The intravenous administration of TRH and its analog YM-14673 (N alpha-[(S)-4-oxo-2-azetidinyl) carbonyl]-L-histidyl-L-prolinamide dehydrate) produced marked increases in the amplitude of mono- and polysynaptic reflex potentials and those of the withdrawal flexor reflexes. The effects of YM-14673 were stronger and longer-lasting than those of TRH. The stimulant action of TRH and YM-14673 on the flexor reflexes was not antagonized by prazosin, chlorpromazine, haloperidol or cyproheptadine, suggesting no involvement of the release of catecholamines or serotonin in the stimulant effects of TRH and its analog. Therefore, YM-14673 may be beneficial for the treatment of several spinal motor neuron diseases.

摘要

实验在C1水平横断脊髓的大鼠身上进行。静脉注射促甲状腺激素释放激素(TRH)及其类似物YM - 14673(Nα-[(S)-4-氧代-2-氮杂环丁烷基)羰基]-L-组氨酰-L-脯氨酰胺脱水物)可使单突触和多突触反射电位以及屈肌反射电位的幅度显著增加。YM - 14673的作用比TRH更强且更持久。TRH和YM - 14673对屈肌反射的兴奋作用不受哌唑嗪、氯丙嗪、氟哌啶醇或赛庚啶的拮抗,这表明TRH及其类似物的兴奋作用不涉及儿茶酚胺或5-羟色胺的释放。因此,YM - 14673可能对几种脊髓运动神经元疾病的治疗有益。

相似文献

1
Effects of a new analog of thyrotropin-releasing hormone, N alpha-[(S)-4-oxo-2-azetidinyl) carbonyl]-L-histidyl-L-prolinamide dehydrate (YM-14673) on spinal reflex potentials and flexor reflexes in spinalized rats.促甲状腺激素释放激素的一种新类似物Nα-[(S)-4-氧代-2-氮杂环丁烷基]羰基-L-组氨酰-L-脯氨酰胺脱水物(YM-14673)对脊髓横断大鼠脊髓反射电位和屈肌反射的影响。
Neuropharmacology. 1990 Jan;29(1):69-74. doi: 10.1016/0028-3908(90)90085-6.
2
Effects of TA-0910, an orally active TRH analog, on the spinal reflex in spinal rats.口服活性促甲状腺激素释放激素类似物TA-0910对脊髓损伤大鼠脊髓反射的影响。
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Effects of a new TRH analogue, YM-14673, on spontaneous motor activity in rats.新型促甲状腺激素释放激素类似物YM-14673对大鼠自发运动活性的影响。
Arch Int Pharmacodyn Ther. 1989 Sep-Oct;301:100-11.
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Central dopaminergic actions of YM-14673, a new TRH analogue, in rodents.新型促甲状腺激素释放激素类似物YM-14673在啮齿动物中的中枢多巴胺能作用
Eur J Pharmacol. 1990 May 16;180(2-3):319-24. doi: 10.1016/0014-2999(90)90316-x.
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Effects of YM-14673, a new TRH analogue, on responses to morphine in rodents.新型促甲状腺激素释放激素类似物YM-14673对啮齿动物吗啡反应的影响。
Arch Int Pharmacodyn Ther. 1989 Jul-Aug;300:29-36.
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Effects of a new analogue of thyrotropin-releasing hormone on pentobarbital-induced sleeping time in rodents.一种促甲状腺激素释放激素新类似物对啮齿动物戊巴比妥诱导睡眠时间的影响。
Neuropharmacology. 1989 Aug;28(8):863-6. doi: 10.1016/0028-3908(89)90179-2.
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Antagonizing effects of YM-14673, a new TRH derivative, on behavioral and electroencephalographic changes in reserpinized animals.新型促甲状腺激素释放激素衍生物YM-14673对利血平化动物行为和脑电图变化的拮抗作用
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Effects of a new TRH analogue, YM-14673, on disturbance of passive avoidance learning in senescence-accelerated mice.
Pharmacol Biochem Behav. 1990 Mar;35(3):727-9. doi: 10.1016/0091-3057(90)90314-8.
9
Effects of a new TRH analogue, YM-14673 on the central nervous system.
Naunyn Schmiedebergs Arch Pharmacol. 1987 Nov;336(5):561-5. doi: 10.1007/BF00169314.
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Effects of a new TRH analogue, YM-14673 on a passive avoidance test as a possible criterion of improvement in cognitive disturbance in rodents.新型促甲状腺激素释放激素类似物YM-14673对被动回避试验的影响,作为啮齿动物认知障碍改善的可能标准。
Naunyn Schmiedebergs Arch Pharmacol. 1988 Sep;338(3):262-7. doi: 10.1007/BF00173398.

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The synthetic TRH analogue taltirelin exerts modality-specific antinociceptive effects via distinct descending monoaminergic systems.合成促甲状腺激素释放激素类似物他替瑞林通过不同的下行单胺能系统发挥模式特异性的镇痛作用。
Br J Pharmacol. 2007 Feb;150(4):403-14. doi: 10.1038/sj.bjp.0707125. Epub 2007 Jan 15.