Pentylenetetrazole
(Synonyms: 戊四唑) 目录号 : GC12357
Pentylenetetrazole是一种γ-氨基丁酸（GABA）A受体的非选择性拮抗剂。
Cas No.:54-95-5
Sample solution is provided at 25 µL, 10mM.
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Pentylenetetrazole is a non-selective antagonist of the γ-aminobutyric acid (GABA) A receptor[1]. The GABAA receptor, a major inhibitory neurotransmitter receptor widely present in the central nervous system, mediates the fast inhibitory effects of GABA by increasing the permeability of the cell membrane to chloride ions, causing hyperpolarization and thus inhibiting neuronal excitability[2]. Pentylenetetrazole is often used to study the mechanism of epileptic seizures, screen antiepileptic drugs, and investigate oxidative stress and neuroinflammatory responses[3][4].
In vivo, Pentylenetetrazole (35mg/kg; i.p.; every other day for 14 times) induced epileptic seizures, increased levels of oxidative stress markers (e.g., malondialdehyde, MDA), decreased the activities of antioxidant enzymes (e.g., glutathione, GSH; superoxide dismutase, SOD; catalase, CAT) , elevated the levels of inflammatory cytokines (e.g., IL-1β, IL-6, TNF-α), and led to neuroinflammatory responses and neuronal damage in mice model[5]. Intraperitoneal injection of Balb-c mice with Pentylenetetrazole (60mg/kg; i.p.; 24h) significantly decreased protein thiols (PSH), cysteine (CSH), and non-protein mixed disulfides (NPSSC), while increasing protein symmetric disulfides (PSSP), non-protein symmetric disulfides (NPSSR), lipid peroxidation, and protein oxidation levels in the mouse hippocampus[6]. Pentylenetetrazole (35mg/kg; i.p.; three times a week) induced kindling in rats, significantly increased the hippocampal concentrations of alanine, arginine, glutamate, aspartate, and taurine, while decreasing GABA levels, leading to an over fourfold increase in the Glu/GABA ratio[7].
References:
[1] Huang RQ, Bell-Horner CL, Dibas MI, Covey DF, Drewe JA, Dillon GH. Pentylenetetrazole-induced inhibition of recombinant gamma-aminobutyric acid type A (GABA(A)) receptors: mechanism and site of action. J Pharmacol Exp Ther. 2001;298(3):986-995.
[2] Lambert JJ, Belelli D, Hill-Venning C, Peters JA. Neurosteroids and GABAA receptor function. Trends Pharmacol Sci. 1995;16(9):295-303.
[3] Shimada T, Yamagata K. Pentylenetetrazole-Induced Kindling Mouse Model. J Vis Exp. 2018;(136):56573.
[4] Monteiro ÁB, Alves AF, Ribeiro Portela AC, et al. Pentylenetetrazole: A review. Neurochem Int. 2024;180:105841.
[5] Younis NS, Almostafa MM, Mohamed ME. Geraniol Ameliorates Pentylenetetrazol-Induced Epilepsy, Neuroinflammation, and Oxidative Stress via Modulating the GABAergic Tract: In vitro and in vivo studies. Drug Des Devel Ther. 2024;18:5655-5672.
[6] Patsoukis N, Zervoudakis G, Panagopoulos NT, Georgiou CD, Angelatou F, Matsokis NA. Thiol redox state (TRS) and oxidative stress in the mouse hippocampus after pentylenetetrazol-induced epileptic seizure. Neurosci Lett. 2004;357(2):83-86.
[7] Szyndler J, Maciejak P, Turzyńska D, et al. Changes in the concentration of amino acids in the hippocampus of pentylenetetrazole-kindled rats. Neurosci Lett. 2008;439(3):245-249.
Pentylenetetrazole是一种γ-氨基丁酸（GABA）A受体的非选择性拮抗剂[1]。GABAA受体是中枢神经系统中广泛存在的主要抑制性神经递质受体，通过增加细胞膜对氯离子的通透性来介导GABA的快速抑制作用，导致细胞膜超极化，从而抑制神经元的兴奋性[2]。Pentylenetetrazole常用于研究癫痫发作的机制、筛选抗癫痫药物以及研究氧化应激和神经炎症反应[3][4]。
在体内实验中，Pentylenetetrazole（35mg/kg; 腹腔注射; 每两天一次，共14次）诱导了小鼠的癫痫发作，增加了氧化应激标志物（如丙二醛，MDA）的水平，降低了抗氧化酶（如谷胱甘肽，GSH；超氧化物歧化酶，SOD；过氧化氢酶，CAT）的活性，提高了炎症因子（如IL-1β、IL-6、TNF-α）的水平，并导致了神经炎症反应和神经元损伤[5]。对Balb-c小鼠进行腹腔注射Pentylenetetrazole（60mg/kg; 24小时）显著降低了蛋白硫醇（PSH）、半胱氨酸（CSH）和非蛋白混合二硫化物（NPSSC）的水平，同时增加了蛋白对称二硫化物（PSSP）、非蛋白对称二硫化物（NPSSR）、脂质过氧化和蛋白质氧化水平[6]。Pentylenetetrazole（35mg/kg; 腹腔注射; 每周三次）在大鼠中诱导了癫痫发作，显著增加了海马区的丙氨酸、精氨酸、谷氨酸、天冬氨酸和牛磺酸的浓度，同时降低了GABA水平，导致谷氨酸与GABA比值（Glu/GABA）增加了四倍以上[7]。
| Animal experiment [1]: | |
Animal models | Male Balb-c mice |
Preparation Method | Male Balb-c mice (3–6 months old) were housed in small groups in a room with controlled light/dark cycle (12/12h) at 22℃. They were separated in two groups and treated as follows: In group I (single convulsive dose), animals received i.p. 60mg/kg Pentylenetetrazole dissolved in 0.9% saline and were decapitated 15min, 30min and 24h after tonic clonic seizure. In group II (controls), animals received i.p. the same volume of saline and were decapitated 30min after administration of saline. The brain was quickly dissected and the hippocampus was removed and washed with ice-cold phosphate-EDTA buffer [10mM phosphate buffer, pH 7.2, containing 1mM EDTA and 1mM of the antioxidant BHA (in final 0.15% ethanol)]. Then, the tissue was homogenized in a glass-glass PotterElvehjem homogenizer and was used for the subsequent assays. |
Dosage form | 60mg/kg; i.p.; 15min, 30min and 24h |
Applications | Pentylenetetrazole significantly decreased protein thiols (PSH), cysteine (CSH), and non-protein mixed disulfides (NPSSC), while increasing protein symmetric disulfides (PSSP), non-protein symmetric disulfides (NPSSR), lipid peroxidation, and protein oxidation levels in the mouse hippocampus. |
References: | |
| Cas No. | 54-95-5 | SDF | |
| 别名 | 戊四唑 | ||
| 化学名 | 6,7,8,9-tetrahydro-5H-tetrazolo[1,5-a]azepine | ||
| Canonical SMILES | N12N=NN=C1CCCCC2 | ||
| 分子式 | C6H10N4 | 分子量 | 138.17 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 3 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 7.2375 mL | 36.1873 mL | 72.3746 mL |
| 5 mM | 1.4475 mL | 7.2375 mL | 14.4749 mL |
| 10 mM | 0.7237 mL | 3.6187 mL | 7.2375 mL |
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动物数量 | 只 |
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