| Identification | Back Directory | [Name]
CP-465022 (maleate) | [CAS]
199656-46-7 | [Synonyms]
CP-465022 (maleate)
CP-392,110 (maleate)
WLLUWLRVXIHECY-KSUUAYPFSA-N
CP-465022 Maleate, 3-(2-Chlorophenyl)-2-[2-[6- [(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro- 4(3H)-quinazolinone Maleate | [Molecular Formula]
C30H28ClFN4O5 | [MDL Number]
MFCD30533447 | [MOL File]
199656-46-7.mol | [Molecular Weight]
579.019 |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [IC 50]
25 nm for ampa receptor-mediated currents in rat cortical neurons | [References]
[1] lazzaro jt, paternain av, lerma j, chenard bl, ewing fe, huang j, welch wm, ganong ah, menniti fs. functional characterization of cp-465,022, a selective, noncompetitive ampa receptor antagonist. neuropharmacology. 2002 feb;42(2):143-53.
[2] menniti fs, buchan am, chenard bl, critchett dj, ganong ah, guanowsky v, seymour pa, welch wm. cp-465,022, a selective noncompetitive ampa receptor antagonist, blocks ampa receptors but is not neuroprotective in vivo. stroke. 2003 jan;34(1):171-6. |
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