(R,S)-AMPA (hydrate)
(Synonyms: αamino3hydroxy5methyl4Isoxazolepropionic Acid) 目录号 : GC46344A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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- Purity: >95.00%
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AMPA is the defining agonist for the AMPA subgroup of ionotropic glutamate receptors, which mediate excitatory neurotransmission.1,2 Because AMPA does not interfere with binding sites for kainic acid or NMDA , it can be used to distinguish AMPA receptor-
1.Scannevin, R.H., and Huganir, R.L.Postsynaptic organization and regulation of excitatory synapsesNature Reviews.Neuroscience1133-141(2000) 2.Gouaux, E.Structure and function of AMPA receptorsJournal of Physiology554(2)249-253(2004)
Cas No. | N/A | SDF | |
别名 | αamino3hydroxy5methyl4Isoxazolepropionic Acid | ||
Canonical SMILES | OC1=NOC(C)=C1CC(N)C(O)=O.O | ||
分子式 | C7H10N2O4.XH2O | 分子量 | 186.2 |
溶解度 | Water: 10 mM | 储存条件 | Store at Room temperature |
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1 mg | 5 mg | 10 mg | |
1 mM | 5.3706 mL | 26.8528 mL | 53.7057 mL |
5 mM | 1.0741 mL | 5.3706 mL | 10.7411 mL |
10 mM | 0.5371 mL | 2.6853 mL | 5.3706 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Perampanel, an antagonist of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors, for the treatment of epilepsy: studies in human epileptic brain and nonepileptic brain and in rodent models
J Pharmacol Exp Ther 2014 Oct;351(1):124-33.PMID:25027316DOI:10.1124/jpet.114.212779.
Perampanel [Fycompa, 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile hydrate 4:3; Eisai Inc., Woodcliff Lake, NJ] is an AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonist used as an adjunctive treatment of partial-onset seizures. We asked whether perampanel has AMPA receptor antagonist activity in both the cerebral cortex and hippocampus associated with antiepileptic efficacy and also in the cerebellum associated with motor side effects in rodent and human brains. We also asked whether epileptic or nonepileptic human cortex is similarly responsive to AMPA receptor antagonism by perampanel. In rodent models, perampanel decreased epileptic-like activity in multiple seizure models. However, doses of perampanel that had anticonvulsant effects were within the same range as those engendering motor side effects. Perampanel inhibited native rat and human AMPA receptors from the hippocampus as well as the cerebellum that were reconstituted into Xenopus oocytes. In addition, with the same technique, we found that perampanel inhibited AMPA receptors from hippocampal tissue that had been removed from a patient who underwent surgical resection for refractory epilepsy. Perampanel inhibited AMPA receptor-mediated ion currents from all the tissues investigated with similar potency (IC50 values ranging from 2.6 to 7.0 μM). Cortical slices from the left temporal lobe derived from the same patient were studied in a 60-microelectrode array. Large field potentials were evoked on at least 45 channels of the array, and 10 μM perampanel decreased their amplitude and firing rate. Perampanel also produced a 33% reduction in the branching parameter, demonstrating the effects of perampanel at the network level. These data suggest that perampanel blocks AMPA receptors globally across the brain to account for both its antiepileptic and side-effect profile in rodents and epileptic patients.