Interactions of Acetylcholine Receptors with Organic Mercury Compounds

  • M. E. Eldefrawi
  • N. A. Mansour
  • A. T. Eldefrawi
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 84)


Micromolar concentrations of methylmercury and several organic mercury fungicides were found to block binding of [3H]acetylcholine (ACh) to the ACh-receptor of the electric organ of the electric ray, Torpedo ocellata. The same compounds had little or no effect on the catalytic activity of ACh-esterase of the same tissue. [14C]Methyl-mercury bound to the purified ACh-receptor with high affinity (Kd= 7μM) and there were 6.5 ± 0.5 binding sites for each ACh-binding site. Binding of methylmercury was highly cooperative with a Hill coefficient of 2.6. This binding was irreversible by redialysis in methylmercury — free medium, however, the bound [14C]methylmercury was easily displaced from the receptor protein with μM concentrations of BAL or penicillamine. Methylmercury also blocked binding of [3H] nicotine and [3H]pilocarpine to the nicotinic and muscarinic ACh-receptors of the rat brain, respectively. The data suggest that the ACh-receptor may be a target for methylmercury and other organic mercury compounds.


Acetylcholine Receptor Equilibrium Dialysis Electric Organ Double Reciprocal Plot Synaptosomal Fraction 
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Copyright information

© Plenum Press, New York 1977

Authors and Affiliations

  • M. E. Eldefrawi
    • 1
  • N. A. Mansour
    • 1
  • A. T. Eldefrawi
    • 1
  1. 1.Dept. of Pharmacology & Experimental TherapeuticsUniv. of Maryland School of MedicineBaltimoreUSA

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