LY-404187 is an
AMPA receptor
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic receptor, ionotropic transmembrane receptor for glutamate (iGluR) that mediates fast synapse, synap ...
positive allosteric modulator which was developed by
Eli Lilly and Company
Eli Lilly and Company is an American pharmaceutical company headquartered in Indianapolis, Indiana, with offices in 18 countries. Its products are sold in approximately 125 countries. The company was founded in 1876 by, and named after, Colonel ...
.
It is a member of the
biarylpropylsulfonamide class of AMPA receptor potentiators.
LY-404187 has been demonstrated to enhance cognitive function in animal studies, and has also shown effects suggesting
antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
action as well as having possible application in the treatment of
schizophrenia,
Parkinson's disease and
ADHD
Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inapp ...
. These effects appear to be mediated through multiple mechanisms of action secondary to AMPA receptor potentiation, with a prominent effect seen in research being increased levels of
BDNF in the brain. It may therefore be continued on to human trials, although Eli Lilly has developed a whole family of biarylpropylsulfonamide derivatives and it is unclear at this stage which compound is most likely to be selected for further development.
See also
*
AMPA receptor positive allosteric modulator
AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the receptor (AMPR), a type of ionotropic glutamate receptor which mediates most fast synaptic neurotransmission in the central nervous system.
Medical ...
References
AMPA receptor positive allosteric modulators
Eli Lilly and Company brands
Nitriles
Sulfonamides
Experimental drugs
Isopropyl compounds
Biphenyls
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