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(R,S)-AMPA (hydrate) Sale

(Synonyms: αamino3hydroxy5methyl4Isoxazolepropionic Acid) 目录号 : GC46344

A neuropeptide with diverse biological activities

(R,S)-AMPA (hydrate) Chemical Structure

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5mg
¥1,400.00
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10mg
¥2,660.00
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25mg
¥5,950.00
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50mg
¥10,500.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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-specific activity that contributes to a neuronal response. (R,S)-AMPA contains an equal mixture of the active (S)-enantiomer and the inactive (R)-enantiomer.

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)

Chemical Properties

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
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Research Update

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.