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Molecular Pharmacology

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Research ArticleArticle

Aminotriarylmethane Dyes Are High-Affinity Noncompetitive Antagonists of the Nicotinic Acetylcholine Receptor

Monica M. Lurtz and Steen E. Pedersen
Molecular Pharmacology January 1999, 55 (1) 159-167; DOI: https://doi.org/10.1124/mol.55.1.159
Monica M. Lurtz
Department of Molecular Physiology and Biophysics, Baylor College of Medicine, Houston, Texas
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Steen E. Pedersen
Department of Molecular Physiology and Biophysics, Baylor College of Medicine, Houston, Texas
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Abstract

A series of aminotriarylmethane dyes were examined for binding to the nicotinic acetylcholine receptor (AChR) from Torpedo californica. Several compounds were found to bind to the noncompetitive antagonist site of the AChR as demonstrated by inhibition of [3H]phencyclidine binding; apparentK D values ranged from 50 nM to >100 μM. One dye with high affinity, crystal violet, revealed a greater than 200-fold fluorescence enhancement upon binding the AChR. Using fluorescence to measure binding, we determined that one crystal violet bound per receptor with a dissociation constant of 100 nM; in the presence of the agonist carbamylcholine this value decreased to 10 nM. The K D for [3H]acetylcholine binding likewise was decreased in the presence of crystal violet. These results are consistent with preferential binding of crystal violet to the desensitized conformation of the AChR. Crystal violet binding blocked agonist-induced 22Na ion efflux from AChR-rich vesicles. It is concluded that crystal violet and other dyes of similar structure bind to the high-affinity noncompetitive antagonist site of the AChR associated with the channel lumen. Because of their optical properties, crystal violet and several of the other homologous dyes are likely to be useful ligands for further characterization of the AChR channel. Structure-activity comparison of the various dyes suggests the importance of nonquaternary nitrogens in binding the pore. Additional steric bulk on amines or at meta positions increase or have neutral effect on affinity, suggesting that steric considerations alone do not limit high affinity for the binding site.

Footnotes

    • Received July 6, 1998.
    • Accepted September 22, 1998.
  • Send reprint requests to: Dr. Steen E. Pedersen, Department of Molecular Physiology and Biophysics, Baylor College of Medicine, One Baylor Plaza, Houston, TX 77030. E-mail:pedersen{at}bcm.tmc.edu

  • ↵1 Current address: Department of Veterinary Pathobiology, University of Minnesota Medical School, St. Paul, MN 55455.

  • Public Health Service Grants NS28879 and NS35212 supported this research. S.E.P. was supported by Research Career Development Award NS01618. M.M.L. was supported by Training Grant HL07676.

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 55 (1)
Molecular Pharmacology
Vol. 55, Issue 1
1 Jan 1999
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Research ArticleArticle

Aminotriarylmethane Dyes Are High-Affinity Noncompetitive Antagonists of the Nicotinic Acetylcholine Receptor

Monica M. Lurtz and Steen E. Pedersen
Molecular Pharmacology January 1, 1999, 55 (1) 159-167; DOI: https://doi.org/10.1124/mol.55.1.159

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Research ArticleArticle

Aminotriarylmethane Dyes Are High-Affinity Noncompetitive Antagonists of the Nicotinic Acetylcholine Receptor

Monica M. Lurtz and Steen E. Pedersen
Molecular Pharmacology January 1, 1999, 55 (1) 159-167; DOI: https://doi.org/10.1124/mol.55.1.159
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