GYKI 52466 is a 2,3-
benzodiazepine that acts as an ionotropic
glutamate receptor
Receptor may refer to:
* Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...
antagonist, which is a non-competitive
AMPA receptor antagonist (IC
50 values are 10-20, ~ 450 and >> 50 μM for AMPA-, kainate- and NMDA-induced responses respectively), orally-active
anticonvulsant, and
skeletal muscle relaxant. Unlike conventional 1,4-benzodiazepines, GYKI 52466 and related 2,3-benzodiazepines do not act on
GABAA receptors. Like other AMPA receptor antagonists, GYKI 52466 has anticonvulsant and
neuroprotective
Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal los ...
properties.
See also
*
GYKI 52895, another 2,3-benzodiazepine with other than GABAergic function
*
Tifluadom
*
Lufuradom
References
{{Benzodiazepines
AMPA receptor antagonists
Anticonvulsants
Muscle relaxants