| Identification | Back Directory | [Name]
2,6-DIFLUORO-4-[2-(PHENYLSULFONYLAMINO)E | [CAS]
141286-78-4 | [Synonyms]
2-[2,6-Difluoro-4-[[2-[(phenylsulfonyl)amino]ethyl]thio]phenoxy]acetamide
2,6-Difluoro-4-[2-(phenylsul-fonyl-amino)-ethyl-thio]-phenoxy-acet-amide (PEPA) | [Molecular Formula]
C16H16F2N2O4S2 | [MDL Number]
MFCD04974493 | [MOL File]
141286-78-4.mol | [Molecular Weight]
402.44 |
| Chemical Properties | Back Directory | [Boiling point ]
617.6±65.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
protect from light | [solubility ]
DMSO: >20mg/mL | [form ]
solid | [pka]
10.44±0.40(Predicted) | [color ]
white | [InChIKey]
GTACSIONMHMRPD-UHFFFAOYSA-N |
| Hazard Information | Back Directory | [Description]
PEPA is a positive allosteric modulator (PAM) of AMPA receptors. It selectively increases glutamate-induced currents in X. laevis oocytes expressing the flop isoforms of the AMPA receptor subunits glutamate receptor 3 (GluR3) and GluR4 over the flip isoforms of these subunits at 200 μM. PEPA (10 mg/kg) decreases the latency to find the platform in the Morris water maze, indicating reversal of memory deficits, in a rat model of memory impairment induced by middle cerebral artery occlusion (MCAO). It decreases freezing time in a contextual fear freezing paradigm in mice when administered at a dose of 30 mg/kg. | [Uses]
PEPA is an allosteric potentiator of AMPA desensitization. | [Biological Activity]
Novel allosteric potentiator of AMPA receptor desensitization. Slows the rate of onset of desensitization and potentiates steady-state equilibrium currents induced by glutamate with subunit (GluR3/4 > GluR1) and splice variant (flop > flip) selectivity. Ameliorates post-ischemic memory impairment in rats following i.v. administration. | [Biochem/physiol Actions]
2,6-Difluoro-4-[2-(phenylsul-fonyl-amino)-ethyl-thio]-phenoxy-acet-amide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor agonist that reduces ischemia-induced performance deficits in rats. | [in vivo]
PEPA (30 mg/kg; i.p.; once) decreases freezing time in a contextual fear freezing paradigm in mice[3]. | Animal Model: | Male C57BL/6J mice (10-12 weeks old) were applied stress (a 2 h restraint, a 20 min forced swim, and ether inhalation)[3] | | Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg | | Administration: | i.p.; once | | Result: | The significant decrease of the freezing response in the extinction sessions was only seen in the 30 mg/kg. |
| [storage]
Store at RT | [References]
[1] Sekiguchi, M., Fleck, M.W., Mayer, M.L., et al. A novel allosteric potentiator of AMPA receptors: 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluoro-phenoxyacetamide. J. Neurosci. 17(15), 5760-5771 (1997).
[2] Sekiguchi, M., Yamada, K., Jin, J., et al. The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment. Neuroreport 12(13), 2947-29950 (2001).
[3] KO ZUSHIDA. Facilitation of extinction learning for contextual fear memory by PEPA: a potentiator of AMPA receptors.[J]. Journal of Neuroscience, 2007, 27 1: 158-166. DOI:10.1523/JNEUROSCI.3842-06.2007. |
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