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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 ...
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 ...
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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.
The AMPA receptor bound to a glutamate antagonist showing the amino terminal, ligand binding, and transmembrane domain, PDB 3KG2 Glutamic acid. Glutamate receptors are synaptic and non synaptic receptors located primarily on the membranes of neuronal and glial cells. [1]
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.
Desensitization prevents a receptor from activating, despite the presence of an agonist. This is often caused by repeated or intense exposures to an agonist. Eliminating or reducing this phenomenon increases the receptor's overall activation. AMPA receptors are susceptible to desensitization via a disruption of a ligand-binding domain dimer ...
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