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化學性質:
規格 | 1mg 5mg 10mg |
CAS | 199656-46-7 |
別名 |
|
化學名 | 3-(2-chlorophenyl)-2-[2-[6-[(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro-4(3H)-quinazolinone-(2Z)-2-butenedioate |
分子式 | C26H24ClFN4O • C4H4O4 |
分子量 | 579.0 |
溶解度 | Soluble in DMSO |
儲存條件 | Room temperature |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
IC50: 25 nM for AMPA receptor-mediated currents in rat cortical neurons
CP-465022 is an AMPA antagonist.
The inhibition of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor has been hypothesized to lead to neuroprotective efficacy after cerebral ischemia on the basis of the activity in ischemia models of a variety of compounds with varying selectivity for AMPA over other glutamate receptor subtypes.
In vitro: CP-465022 inhibited AMPA receptor-mediated currents in rat cortical neurons and such inhibition was found to be noncompetitive with agonist concentration. CP-465022 was selective for AMPA over kainate and N-methyl-D-aspartate receptors. However, CP-465022 was found to be equipotent for AMPA receptors composed of different AMPA receptor subunit combinations, which indicated that CP-465022 is equivalently potent for inhibition of AMPA receptor-mediated responses in different types of neurons expressing different AMPA receptor subunits [1].
In vivo: Animal study showed that CP-465022 could potently and efficaciously inhibit AMPA receptor-mediated hippocampal synaptic transmission and the induction of seizures. However, at comparable doses, CP-465022 failed to prevent CA1 neuron loss after brief global ischemia or to reduce infarct volume after temporary middle cerebral artery occlusion [2].
Clinical trial: So far, no clinical study has been conducted.
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原創作者:上海莼試生物技術有限公司
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