Perzinfotel (EAA-090) is a drug which acts as a potent
NMDA antagonist
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor ( NMDAR). They are commonly used as anesthetics for humans and animals; the state of anesthesia they ind ...
. It has
neuroprotective effects and has been investigated for the treatment of
stroke
Stroke is a medical condition in which poor cerebral circulation, blood flow to a part of the brain causes cell death. There are two main types of stroke: brain ischemia, ischemic, due to lack of blood flow, and intracranial hemorrhage, hemor ...
, but lacks
analgesic
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
effects. Nevertheless, it shows a good safety profile compared to older drugs, although further development of this drug has been discontinued.
Prodrugs were developed since the oral bioavailability of perzinfotel is only around 3-5%.
References
NMDA receptor antagonists
Phosphonic acids
Quinones
Cyclobutenes
Nitrogen heterocycles
Heterocyclic compounds with 2 rings
Enones
Dissociative drugs
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