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The AMPA receptor bound to a glutamate antagonist showing the amino terminal, ligand binding, and transmembrane domain, PDB 3KG2. The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic transmembrane receptor for glutamate and predominantly Na + ion channel that mediates fast synaptic transmission in the ...
α-Methylphenylalanine (α-MePhe or AMPA) is an artificial amino acid and a phenethylamine and amphetamine derivative. [1] It is the α- methylated analogue of phenylalanine , the precursor of the catecholamine neurotransmitters , and the amino acid analogue of amphetamine (α-methylphenethylamine), a psychostimulant and monoamine releasing agent .
AMPA activates AMPA receptors that are non-selective cationic channels allowing the passage of Na + and K + and therefore have an equilibrium potential near 0 mV. AMPA was first synthesized, along with several other ibotenic acid derivatives, by Krogsgaard-Larsen , Honoré, and others toward differentiating glutamate sensitive receptors from ...
Ampakines or AMPAkines are a subgroup of AMPA receptor positive allosteric modulators with a benzamide or closely related chemical structure. [ 1 ] [ 2 ] They are also known as "CX compounds". [ 1 ] Ampakines take their name from the AMPA receptor (AMPAR), a type of ionotropic glutamate receptor with which the ampakines interact and act as ...
CX-516, one of the earliest and a prototypical AMPAR PAM.It is a low-impact AMPAR PAM. Tulrampator (S-47445, CX-1632), a newer and high-impact AMPAR PAM.. AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the AMPA receptor (AMPR), a type of ionotropic glutamate receptor which mediates most fast synaptic neurotransmission in the central nervous system.
Osavampator is a selective positive allosteric modulator (PAM) of the AMPA receptor. [3] [4] Osavampator and other AMPA PAMs potentiate the effects of agonists at the main site of the AMPA receptor by slowing the rate of desensitization and internalization of the receptor. [5] The terminal half-life of osavampator is 33.1–47.8 hours. [6]
On the other hand, kainate receptors are less understood than AMPA receptors. Although, the function is somewhat similar: the ion channel permeates the flow of sodium and potassium ions, and to a lower extent the Calcium ions. [citation needed] As mentioned, binding of quisqualic acid to these receptors leads to an influx of calcium and sodium ...
CX-614 is an ampakine drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptors. [1]Chronic CX-614 treatments produce rapid increases in the synthesis of the brain-derived neurotrophic factor BDNF which has very important effects on synaptic plasticity [2] and may have applications in the treatment of neurodegenerative diseases such as Alzheimer's disease.