Modeling Noncompetitive Antagonism of a Nicotinic Acetylcholine Receptor
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چکیده
منابع مشابه
Molecular Mechanism of AMPA Receptor Noncompetitive Antagonism
AMPA-type glutamate receptors are specifically inhibited by the noncompetitive antagonists GYKI-53655 and CP-465,022, which act through sites and mechanisms that are not understood. Using receptor mutagenesis, we found that these antagonists bind at the interface between the S1 and S2 glutamate binding core and channel transmembrane domains, specifically interacting with S1-M1 and S2-M4 linkers...
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Tetracaine (N,N-dimethylaminoethyl-4-butylaminobenzoate) and related N,N-dialkylaminoethyl substituted benzoic acid esters have been used to characterize the high-affinity binding site for aromatic amine noncompetitive antagonists in the Torpedo nicotinic acetylcholine receptor (nAChR). [H]Tetracaine binds at equilibrium to a single site with a Keq value of 0.5 mM in the absence of agonist or p...
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Nicotinic acetylcholine receptors (nAChR) are diverse members of the neurotransmitter-gated ion channel superfamily and play critical roles in chemical signaling throughout the nervous system. The present study establishes the acute functional effects of bupropion, phencyclidine, and ibogaine on two human nAChR subtypes. Function of muscle-type nAChR (alpha1 beta gamma delta) in TE671/RD cells ...
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ژورنال
عنوان ژورنال: Biophysical Journal
سال: 2004
ISSN: 0006-3495
DOI: 10.1529/biophysj.103.037457