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两种不可逆的γ-氨基丁酸转氨酶抑制剂，γ-乙炔基γ-氨基丁酸（4-氨基-5-己炔酸）和γ-乙烯基γ-氨基丁酸（4-氨基-5-己烯酸）对光敏狒狒（豚尾狒狒）癫痫反应的阻断作用

Blockade of epileptic responses in the photosensitive baboon, Papio papio, by two irreversible inhibitors of GABA-transaminase, gamma-acetylenic GABA (4-amino-hex-5-ynoic acid) and gamma-vinyl GABA (4-amino-hex-5-enoic acid).

作者信息

Meldrum B, Horton R

出版信息

Psychopharmacology (Berl). 1978 Sep 15;59(1):47-50. doi: 10.1007/BF00428029.

DOI:10.1007/BF00428029
PMID:100812
Abstract

The anticonvulsant potency and neurological toxicity of two new catalytic inhibitors of GABA-transaminase have been assessed in acute experiments in baboons with a natural syndrome of photic epilepsy. gamma-Acetylenic GABA, 160--200 mg/kg, or gamma-vinyl GABA, 450--950 mg/kg, intravenously, gave complete protection against generalised myoclonus or seizure responses induced by photic stimulation (in baboons without or with priming with subconvulsant doses of allylglycine). The protection became maximal 1--3 h after injection, and continued for 7--24 h. Signs characteristic of the acute toxicity of anticonvulsant drugs (nystagmus and ataxia) were not seen. The potential use of these compounds in human epilepsy deserves investigation.

摘要

在患有自然光性癫痫综合征的狒狒身上进行的急性实验中，评估了两种新型γ-氨基丁酸转氨酶催化抑制剂的抗惊厥效力和神经毒性。静脉注射160 - 200mg/kg的γ-乙炔基氨基丁酸或450 - 950mg/kg的γ-乙烯基氨基丁酸，可完全预防由光刺激诱发的全身性肌阵挛或癫痫反应（在未用或先用亚惊厥剂量烯丙基甘氨酸引发的狒狒中）。注射后1 - 3小时保护作用达到最大，并持续7 - 24小时。未观察到抗惊厥药物急性毒性的特征性体征（眼球震颤和共济失调）。这些化合物在人类癫痫中的潜在用途值得研究。

相似文献

1
Blockade of epileptic responses in the photosensitive baboon, Papio papio, by two irreversible inhibitors of GABA-transaminase, gamma-acetylenic GABA (4-amino-hex-5-ynoic acid) and gamma-vinyl GABA (4-amino-hex-5-enoic acid).两种不可逆的γ-氨基丁酸转氨酶抑制剂，γ-乙炔基γ-氨基丁酸（4-氨基-5-己炔酸）和γ-乙烯基γ-氨基丁酸（4-氨基-5-己烯酸）对光敏狒狒（豚尾狒狒）癫痫反应的阻断作用
Psychopharmacology (Berl). 1978 Sep 15;59(1):47-50. doi: 10.1007/BF00428029.
2
Catalytic inhibitors of GABA-transaminase as anticonvulsants in baboons with photosensitive epilepsy [proceedings].γ-氨基丁酸转氨酶催化抑制剂作为光敏性癫痫狒狒的抗惊厥药物[会议论文集]
Br J Pharmacol. 1978 Jun;63(2):390P.
3
Audiogenic seizure protection by elevated brain GABA concentration in mice: effects of gamma-acetylenic gaba and gamma-vinyl GABA, two irreversible GABA-T inhibitors.小鼠脑内γ-氨基丁酸（GABA）浓度升高对听源性癫痫的保护作用：两种不可逆性GABA转氨酶（GABA-T）抑制剂——γ-乙炔基氨基丁酸和γ-乙烯基氨基丁酸的作用
Eur J Pharmacol. 1977 Oct 15;45(4):319-28. doi: 10.1016/0014-2999(77)90270-9.
4
The effect of 4-amino hex-5-ynoic acid (gamma-acetylenic GABA, gammma-ethynyl GABA) a catalytic inhibitor of GABA transaminase, on brain GABA metabolism in vivo.4-氨基己-5-炔酸（γ-乙炔基γ-氨基丁酸），一种γ-氨基丁酸转氨酶的催化抑制剂，对体内脑γ-氨基丁酸代谢的影响。
J Neurochem. 1977 Apr;28(4):717-23. doi: 10.1111/j.1471-4159.1977.tb10618.x.
5
Effects of the bicyclic GABA agonist, THIP, on myoclonic and seizure responses in mice and baboons with reflex epilepsy.双环GABA激动剂THIP对患有反射性癫痫的小鼠和狒狒肌阵挛及癫痫反应的影响。
Eur J Pharmacol. 1980 Feb 8;61(3):231-7. doi: 10.1016/0014-2999(80)90125-9.
6
Antiseizure activity of gamma-acetylenic gamma-aminobutyric acid: a catalytic irreversible inhibitor of gamma-aminobutyric acid transaminase.γ-乙炔基γ-氨基丁酸的抗癫痫活性：一种γ-氨基丁酸转氨酶的催化不可逆抑制剂。
J Pharmacol Exp Ther. 1977 Jun;201(3):606-12.
7
Attempts to correlate alterations in brain GABA metabolism by GABA-T inhibitors with their anticonvulsant effects.尝试将γ-氨基丁酸转氨酶（GABA-T）抑制剂引起的脑内γ-氨基丁酸（GABA）代谢变化与其抗惊厥作用联系起来。
Adv Exp Med Biol. 1979;123:43-57. doi: 10.1007/978-1-4899-5199-1_3.
8
Seizures induced by allylglycine, 3-mercaptopropionic acid and 4-deoxypyridoxine in mice and photosensitive baboons, and different modes of inhibition of cerebral glutamic acid decarboxylase.烯丙基甘氨酸、3-巯基丙酸和4-脱氧吡哆醇在小鼠和光敏狒狒中诱发的癫痫发作，以及脑谷氨酸脱羧酶的不同抑制模式。
Br J Pharmacol. 1973 Sep;49(1):52-63. doi: 10.1111/j.1476-5381.1973.tb08267.x.
9
Hypersynchronisation and sedation produced by GABA-transaminase inhibitors and picrotoxin: does GABA participate in sleep control?γ-氨基丁酸转氨酶抑制剂和印防己毒素引起的过度同步化与镇静作用：γ-氨基丁酸是否参与睡眠调控？
Waking Sleeping. 1979 Jul;3(3):245-54.
10
Action of progabide in the photosensitive baboon, Papio papio.丙戊酸γ-氨基丁酯在光敏狒狒（豚尾狒狒）中的作用。
Epilepsia. 1982 Oct;23(5):463-70. doi: 10.1111/j.1528-1157.1982.tb05434.x.

引用本文的文献

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Molecular targets for antiepileptic drug development.抗癫痫药物研发的分子靶点
Neurotherapeutics. 2007 Jan;4(1):18-61. doi: 10.1016/j.nurt.2006.11.010.
2
Novel mechanisms of action of three antiepileptic drugs, vigabatrin, tiagabine, and topiramate.三种抗癫痫药物（氨己烯酸、噻加宾和托吡酯）的新型作用机制。
Neurochem Res. 2003 Feb;28(2):333-40. doi: 10.1023/a:1022393604014.
3
Localized 1H NMR measurements of gamma-aminobutyric acid in human brain in vivo.活体人脑中γ-氨基丁酸的局部¹H核磁共振测量

本文引用的文献

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GABA agonists and audiogenic seizures.γ-氨基丁酸激动剂与听源性癫痫发作
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Effects of DI-n-propylacetate, and anticonvulsive compound, on GABA metabolism.二正丙基乙酸酯（一种抗惊厥化合物）对γ-氨基丁酸（GABA）代谢的影响。
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Analysis of the major amino acids of rat brain after in vivo inhibition of GABA transaminase by ethanolamine O-sulphate.用硫酸乙醇胺对大鼠体内γ-氨基丁酸转氨酶进行抑制后大鼠脑主要氨基酸的分析。
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Newer antiepileptic drugs. Towards an improved risk-benefit ratio.新型抗癫痫药物。旨在改善风险效益比。
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Place of newer antiepileptic drugs in the treatment of epilepsy.新型抗癫痫药物在癫痫治疗中的地位。
Drugs. 1993 Dec;46(6):1009-24. doi: 10.2165/00003495-199346060-00006.
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Gamma-vinyl GABA: comparison of neurochemical and anticonvulsant effects in mice.γ-乙烯基γ-氨基丁酸：小鼠神经化学和抗惊厥作用的比较
J Neural Transm. 1988;72(3):213-33. doi: 10.1007/BF01243421.
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The role of the brain stem in generalized epileptic seizures.脑干在全身性癫痫发作中的作用。
Metab Brain Dis. 1987 Jun;2(2):81-112. doi: 10.1007/BF00999720.
8
Effect of vigabatrin (gamma-vinyl GABA) on amino acid levels in CSF of epileptic patients.氨己烯酸（γ-乙烯基-GABA）对癫痫患者脑脊液中氨基酸水平的影响。
J Neurol Neurosurg Psychiatry. 1988 Nov;51(11):1395-400. doi: 10.1136/jnnp.51.11.1395.
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GABAergic mechanisms in the pathogenesis and treatment of epilepsy.癫痫发病机制与治疗中的γ-氨基丁酸能机制
Br J Clin Pharmacol. 1989;27 Suppl 1(Suppl 1):3S-11S. doi: 10.1111/j.1365-2125.1989.tb03454.x.
10
Development of tolerance to the effects of vigabatrin (gamma-vinyl-GABA) on GABA release from rat cerebral cortex, spinal cord and retina.对氨己烯酸（γ-乙烯基-GABA）对大鼠大脑皮层、脊髓和视网膜GABA释放影响的耐受性的发展。
Br J Pharmacol. 1990 Jun;100(2):324-8. doi: 10.1111/j.1476-5381.1990.tb15803.x.
J Neurochem. 1973 Aug;21(2):437-40. doi: 10.1111/j.1471-4159.1973.tb04263.x.
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Effect of sodium n-dipropylacetate on audiogenic seizures and brain -aminobutyric acid level.正丙基乙酸钠对听源性癫痫发作及脑γ-氨基丁酸水平的影响。
Biochem Pharmacol. 1973 Jul 15;22(14):1701-8. doi: 10.1016/0006-2952(73)90383-3.
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Seizures induced by allylglycine, 3-mercaptopropionic acid and 4-deoxypyridoxine in mice and photosensitive baboons, and different modes of inhibition of cerebral glutamic acid decarboxylase.烯丙基甘氨酸、3-巯基丙酸和4-脱氧吡哆醇在小鼠和光敏狒狒中诱发的癫痫发作，以及脑谷氨酸脱羧酶的不同抑制模式。
Br J Pharmacol. 1973 Sep;49(1):52-63. doi: 10.1111/j.1476-5381.1973.tb08267.x.
6
Effects of atropine and eserine on the electroencephalogram, on behaviour and on light-induced epilepsy in the adolescent baboon (Papio papio).阿托品和毒扁豆碱对幼年狒狒（豚尾狒狒）脑电图、行为及光诱发性癫痫的影响。
Electroencephalogr Clin Neurophysiol. 1970 May;28(5):449-58. doi: 10.1016/0013-4694(70)90270-1.
7
Catalytic inhibition of gamma-aminobutyric acid - alpha-ketoglutarate transaminase of bacterial origin by 4-aminohex-5-ynoic acid, a substrate analog.底物类似物4-氨基己-5-炔酸对细菌来源的γ-氨基丁酸-α-酮戊二酸转氨酶的催化抑制作用。
Biochem Biophys Res Commun. 1975 Nov 3;67(1):301-6. doi: 10.1016/0006-291x(75)90316-2.
8
Audiogenic seizure protection by elevated brain GABA concentration in mice: effects of gamma-acetylenic gaba and gamma-vinyl GABA, two irreversible GABA-T inhibitors.小鼠脑内γ-氨基丁酸（GABA）浓度升高对听源性癫痫的保护作用：两种不可逆性GABA转氨酶（GABA-T）抑制剂——γ-乙炔基氨基丁酸和γ-乙烯基氨基丁酸的作用
Eur J Pharmacol. 1977 Oct 15;45(4):319-28. doi: 10.1016/0014-2999(77)90270-9.
9
The effect of 4-amino hex-5-ynoic acid (gamma-acetylenic GABA, gammma-ethynyl GABA) a catalytic inhibitor of GABA transaminase, on brain GABA metabolism in vivo.4-氨基己-5-炔酸（γ-乙炔基γ-氨基丁酸），一种γ-氨基丁酸转氨酶的催化抑制剂，对体内脑γ-氨基丁酸代谢的影响。
J Neurochem. 1977 Apr;28(4):717-23. doi: 10.1111/j.1471-4159.1977.tb10618.x.
10
Antiseizure activity of gamma-acetylenic gamma-aminobutyric acid: a catalytic irreversible inhibitor of gamma-aminobutyric acid transaminase.γ-乙炔基γ-氨基丁酸的抗癫痫活性：一种γ-氨基丁酸转氨酶的催化不可逆抑制剂。
J Pharmacol Exp Ther. 1977 Jun;201(3):606-12.