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Ibotenic acid

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Chemical Structure| 2552-55-8 同义名 : DL-Ibotenic acid;NSC 204850;Ibotenate;(RS)-Ibotenic acid
CAS号 : 2552-55-8
货号 : A104575
分子式 : C5H6N2O4
纯度 : 95%
分子量 : 158.112
MDL号 : MFCD00069294
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(25.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(31.62 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Qm) receptor sites. Ibotenic acid (Ibo) is capable of acting at both NMDA and trans-ACPD receptors in the CNS, although only activation of NMDA receptors is involved in Ibo neurotoxicity. Ibotenic acid is toxic to cortical neurons exposes for 5 min with an EC50=77.3±8 μM (n=5) as measured by release of lactate dehydrogenase to the culture media[3]. Ibotenic acid was inhibitors of (S)-glutamic acid decarboxylase (GAD) in mouse brain homogenates, and was shown to undergo decarboxylation during incubation with brain homogenates. The formation of the decarboxylated product, muscimol, which primarily occurred in a synaptosomal fraction, was dependent on the presence of pyridoxal-5-phosphate (PALP) and was inhibited by (S)-glutamic acid, 3-mercaptopropionic acid (3MPA), aminooxyacetic acid (AOAA), and allyglycine, suggesting that ibotenic acid is a substrate for GAD. The overall decomposition rate for ibotenic acid (8.7 nmol min-1 mg-1 of protein), which apparently embraces other reactions in addition to decarboxylation to muscimol, was higher than the rate of decarboxylation of (S)-glutamic acid (3.2 nmol min-1 mg-1 of protein)[4]. Ibotenic acid induced similar neuronal migration impairments in control and alcohol-exposed pups (nodular heterotopia in the white matter and/or deep cortical layers, subpial ectopia, and micro- or polymicrogyria)[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00005925 Epilepsy Phase 1 Terminated - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT00921128 Parkinson's Disease Phase 1 Withdrawn - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.32mL

1.26mL

0.63mL

31.62mL

6.32mL

3.16mL

63.25mL

12.65mL

6.32mL
参考文献

[1]Karthick C, Periyasamy S, Jayachandran KS, Anusuyadevi M. Intrahippocampal Administration of Ibotenic Acid Induced Cholinergic Dysfunction via NR2A/NR2B Expression: Implications of Resveratrol against Alzheimer Disease Pathophysiology. Front Mol Neurosci. 2016 Apr 26;9:28.

[2]Effects of BIS-MEP on Reversing Amyloid Plaque Deposition and Spatial Learning and Memory Impairments in a Mouse Model of β-Amyloid Peptide- and Ibotenic Acid-Induced Alzheimer’s Disease

[3]Zinkand WC, Moore WC, Thompson C, Salama AI, Patel J. Ibotenic acid mediates neurotoxicity and phosphoinositide hydrolysis by independent receptor mechanisms. Mol Chem Neuropathol. 1992 Feb-Apr;16(1-2):1-10

[4]Nielsen EO, Schousboe A, Hansen SH, Krogsgaard-Larsen P. Excitatory amino acids: studies on the biochemical and chemical stability of ibotenic acid and related compounds. J Neurochem. 1985 Sep;45(3):725-31

[5]Adde-Michel C, Hennebert O, Laudenbach V, Marret S, Leroux P. Effect of perinatal alcohol exposure on ibotenic acid-induced excitotoxic cortical lesions in newborn hamsters. Pediatr Res. 2005 Feb;57(2):287-93