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IDRA 21

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Chemical Structure| 22503-72-6 同义名 : -
CAS号 : 22503-72-6
货号 : A150690
分子式 : C8H9ClN2O2S
纯度 : 97%
分子量 : 232.687
MDL号 : MFCD00270874
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: 250 mg/mL(1074.4 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
动物实验配方：
生物活性
描述 IDRA 21, a positive allosteric modulator of the glutamate AMPA receptor, produced a concentration-dependent inhibition of glutamate-induced inactivation of membrane currents in recombinant HEK 293 (human embryonic kidney) cells stably transfected with human GluR1/2 flip receptors. Oral administration of IDRA 21 produced a highly significant improvement in the performance of a delayed matching-to-sample (DMTS) task by young adult rhesus monkeys. The pattern of task improvement over the dose range 0.15 - 10 mg/kg was maintained to 48 hr after the single dose administration[1]. IDRA-21 reduces alpha-amino-3-hydroxy-5-methylisoxazolepropionic acid (AMPA) receptors desensitisation in vitro and restores learning and cognitive impairment in vivo. In cerebellar granule cells (CGCs) in culture IDRA-21 reduces NMDAR whole-cell currents. IDRA-21 shortens miniature excitatory postsynaptic currents mediated by NMDARs (NMDA-mEPSCs) in CGCs grown in low potassium with no effect on peak amplitudes[2]. IDRA 21 and cyclothiazide potentiate KA-evoked (kainic acid) current in a dose dependent way, being cyclothiazide more potent but less efficacious than IDRA 21. Conversely IDRA 5 acts as a negative modulator of KA evoked-current[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.30mL

0.86mL

0.43mL

21.49mL

4.30mL

2.15mL

42.98mL

8.60mL

4.30mL
参考文献

[1]Buccafusco JJ, Weiser T, Winter K, Klinder K, Terry AV. The effects of IDRA 21, a positive modulator of the AMPA receptor, on delayed matching performance by young and aged rhesus monkeys. Neuropharmacology. 2004;46(1):10‐22

[2]Losi G, Puia G, Braghiroli D, Baraldi M. IDRA-21, a positive AMPA receptor modulator, inhibits synaptic and extrasynaptic NMDA receptor mediated events in cultured cerebellar granule cells. Neuropharmacology. 2004;46(8):1105‐1113

[3]Puia G, Losi G, Razzini G, Braghiroli D, Di Bella M, Baraldi M. Modulation of kainate--activated currents by diazoxide and cyclothiazide analogues (IDRA) in cerebellar granule neurons. Prog Neuropsychopharmacol Biol Psychiatry. 2000;24(6):1007‐1015

[4]24(6):1007‐1015