PD-137889
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PD-137889 (''N''-methylhexahydrofluorenamine) is a chemical compound that is active as an
NMDA receptor 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 animals and humans; the state of anesthesia they induce ...
in the
central nervous system The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all p ...
at roughly 30 times the potency of the "flagship" of its class,
ketamine Ketamine is a dissociative anesthetic used medically for induction and maintenance of anesthesia. It is also used as a recreational drug. It is one of the safest anesthetics, as, in contrast with opiates, ether, and propofol, it suppresses ...
, and substitutes for
phencyclidine Phencyclidine or phenylcyclohexyl piperidine (PCP), also known as angel dust among other names, is a dissociative anesthetic mainly used recreationally for its significant mind-altering effects. PCP may cause hallucinations, distorted percept ...
in animal studies. K''i'' sup>3HCP binding = 27  nM versus ketamine's K''i'' = 860 nM.Polycyclic amine derivatives useful as cerebrovascular agents
United States Patent; Coughenour, et al. Family ID: 22686445 Appl. #07/186,834


See also

* Aptiganel *
Dizocilpine Dizocilpine (INN), also known as MK-801, is a pore blocker of the ''N''-Methyl-D-aspartate (NMDA) receptor, a glutamate receptor, discovered by a team at Merck in 1982. Glutamate is the brain's primary excitatory neurotransmitter. The channel is ...
* Fourphit *
Metaphit Metaphit (1- -(3-Isothiocyanato)phenylyclohexylpiperidine) is a research chemical that acts as an acylator of NMDARAn, sigma and DAT binding sites in the CNS. It is the ''m''-isothiocyanate derivative of phencyclidine (PCP) and binds irreversi ...
*
Selfotel Selfotel (CGS-19755) is a drug which acts as a competitive NMDA antagonist, directly competing with glutamate for binding to the receptor. Initial studies showed it to have anticonvulsant, anxiolytic, analgesic and neuroprotective effects, and ...


References

Arylcyclohexylamines Dissociative drugs General anesthetics NMDA receptor antagonists Sedatives Tricyclic compounds {{Sedative-stub