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6,7-二甲氧基-4-乙基-β-咔啉-3-羧酸甲酯(DMCM)使小脑环磷酸鸟苷增加。

Increase of cyclic GMP in cerebellum by methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM).

作者信息

Serra M, Concas A, Salis M, Biggio G

出版信息

Brain Res. 1983 Aug 29;273(2):347-51. doi: 10.1016/0006-8993(83)90860-0.

DOI:10.1016/0006-8993(83)90860-0
PMID:6311353
Abstract

The intraperitoneal administration of DMCM (0.5-3 mg/kg) produced a dose-related increase in the content of cyclic GMP in the rat cerebellar cortex. The effect of DMCM on cyclic GMP was abolished by pretreatment with benzodiazepine receptor ligands, diazepam and Ro15-1788 and by the GABA agonist muscimol. The results suggest that DMCM increases cerebellar cyclic GMP content through a direct action on benzodiazepine receptors located in the cerebellar cortex. The interaction between DMCM and the GABAergic system associated with benzodiazepine receptors is discussed. Cerebellar cyclic GMP content can be used as a biochemical index to differentiate agonists and antagonists for benzodiazepine receptors.

摘要

腹腔注射DMCM(0.5 - 3毫克/千克)可使大鼠小脑皮质中环状鸟苷酸(cGMP)的含量呈剂量依赖性增加。苯二氮䓬受体配体地西泮和Ro15 - 1788以及GABA激动剂蝇蕈醇预处理可消除DMCM对cGMP的影响。结果表明,DMCM通过直接作用于位于小脑皮质的苯二氮䓬受体来增加小脑cGMP含量。文中讨论了DMCM与和苯二氮䓬受体相关的GABA能系统之间的相互作用。小脑cGMP含量可用作区分苯二氮䓬受体激动剂和拮抗剂的生化指标。

相似文献

1
Increase of cyclic GMP in cerebellum by methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM).6,7-二甲氧基-4-乙基-β-咔啉-3-羧酸甲酯(DMCM)使小脑环磷酸鸟苷增加。
Brain Res. 1983 Aug 29;273(2):347-51. doi: 10.1016/0006-8993(83)90860-0.
2
Contrasting effects of ethyl beta-carboline-3-carboxylate (beta CCE) and diazepam on cerebellar cyclic GMP content and antagonism of both effects by Ro 15-1788, a specific benzodiazepine receptor blocker.β-咔啉-3-羧酸乙酯(βCCE)和地西泮对小脑环磷酸鸟苷含量的对比作用以及特异性苯二氮䓬受体阻滞剂Ro 15-1788对两者作用的拮抗作用
Eur J Pharmacol. 1983 May 20;90(1):97-102. doi: 10.1016/0014-2999(83)90218-2.
3
Ethyl beta-carboline-3-carboxylate reverses the diazepam effect on cerebellar cyclic GMP.β-咔啉-3-羧酸乙酯可逆转地西泮对小脑环鸟苷酸的作用。
Eur J Pharmacol. 1982 May 21;80(2-3):259-62. doi: 10.1016/0014-2999(82)90065-6.
4
DMCM: a potent convulsive benzodiazepine receptor ligand.DMCM:一种强效的惊厥性苯二氮䓬受体配体。
Eur J Pharmacol. 1983 Oct 14;94(1-2):117-24. doi: 10.1016/0014-2999(83)90448-x.
5
Discriminative stimulus properties of methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM), an inverse agonist at benzodiazepine receptors.6,7-二甲氧基-4-乙基-β-咔啉-3-羧酸甲酯(DMCM)的辨别刺激特性,一种苯二氮䓬受体反向激动剂。
Life Sci. 1985 Jan 7;36(1):15-23. doi: 10.1016/0024-3205(85)90281-4.
6
The benzodiazepine antagonist Ro 15-1788 reverses the effect of methyl-beta-carboline-3-carboxylate but not of harmaline on cerebellar cGMP and motor performance in mice.苯二氮䓬拮抗剂Ro 15 - 1788可逆转甲基-β-咔啉-3-羧酸酯对小鼠小脑环磷酸鸟苷和运动能力的影响,但不能逆转哈马灵的影响。
Eur J Pharmacol. 1985 Feb 26;109(2):241-7. doi: 10.1016/0014-2999(85)90425-x.
7
Behavioral evidence for the role of noradrenaline in the putative anxiogenic actions of the inverse benzodiazepine receptor agonist methyl-4-ethyl-6,7-dimethoxy-beta-carboline-3-carboxylate.去甲肾上腺素在反向苯二氮䓬受体激动剂甲基-4-乙基-6,7-二甲氧基-β-咔啉-3-羧酸酯假定的致焦虑作用中作用的行为学证据
J Pharmacol Exp Ther. 1989 Jul;250(1):358-63.
8
Effects of two convulsant beta-carboline derivatives, DMCM and beta-CCM, on regional neurotransmitter amino acid levels and on in vitro D-[3H]aspartate release in rodents.两种惊厥性β-咔啉衍生物DMCM和β-CCM对啮齿动物局部神经递质氨基酸水平及体外D-[3H]天冬氨酸释放的影响。
J Neurochem. 1985 Aug;45(2):370-81. doi: 10.1111/j.1471-4159.1985.tb03998.x.
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Blockade of the diazepam-induced increase in rat striatal acetylcholine content by the specific benzodiazepine antagonists ethyl-beta-carboline-3-carboxylate and Ro 15-1788.
Brain Res. 1985 Jun 17;336(2):342-5. doi: 10.1016/0006-8993(85)90664-x.
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Interaction of beta-carboline inverse agonists for the benzodiazepine site with another site on GABAA receptors.β-咔啉反向激动剂与苯二氮䓬位点在GABAA受体上的另一位点的相互作用。
Br J Pharmacol. 1995 Mar;114(5):1040-4. doi: 10.1111/j.1476-5381.1995.tb13310.x.

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