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The present study examines the interaction of the neurotransmitter 5-hydroxytryptamine (5-HT) with muscle-type nicotinic acetylcholine receptors. 5-HT inhibits the initial rate of [125I]alpha-bungarotoxin binding to Torpedo acetylcholine receptor membranes (IC(50)=8.5+/-0.32 mM) and [3H]5-HT can be photoincorporated into acetylcholine receptor subunits, with labeling of the alpha-subunit inhibitable by both agonists and competitive antagonists. Within the agonist-binding domain, [3H]5-HT photoincorporates into alphaTyr(190), alphaCys(192) and alphaCys(193). Functional studies using the human clonal cell line TE671/RD, show that 5-HT is a weak inhibitor (IC(50)=1.55+/-0.25 mM) of acetylcholine receptor activity. In this regard, agonist-response profiles in the absence and presence of 5-HT indicate a noncompetitive mode of inhibition. In addition, 5-HT displaces high affinity [3H]thienylcyclohexylpiperidine binding to the desensitized Torpedo acetylcholine receptor channel (IC(50)=1.61+/-0.07 mM). Collectively, these results indicate that 5-HT interacts weakly with the agonist recognition site and inhibits receptor function noncompetitively by binding to the acetylcholine receptor channel.
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
April 1993,
Journal of neuroscience research,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
November 1986,
The Journal of physiology,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
January 2003,
Journal of proteome research,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
October 1998,
The Journal of pharmacology and experimental therapeutics,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
August 1987,
European journal of pharmacology,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
July 1997,
Anesthesia and analgesia,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
September 2005,
Anesthesia and analgesia,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
March 1990,
Biochemical and biophysical research communications,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
March 2005,
The European journal of neuroscience,
M P Blanton, and
E A McCardy, and
J D Fryer, and
M Liu, and
R J Lukas
August 1993,
Molecular pharmacology,
