Physiol. Res. 55: 585-589, 2006


Different Sensitivity of Miniature Endplate Currents of the Rat Extensor Digitorum Longus, Soleus and Diaphragm Muscles to a Novel Acetylcholinesterase Inhibitor C-547

K. A. PETROV1, I. V. KOVYAZINA2, V. V. ZOBOV1, E. A. BUKHARAEVA2,3,
E. E. NIKOLSKY2,3, F. VYSKOČIL4,5


1Kazan Institute of Organic and Physical Chemistry, Russian Academy of Sciences, 2Kazan Institute of Biochemistry and Biophysics, Russian Academy of Sciences, 3Kazan State Medical University, Kazan, Russia, 4Department of Animal Physiology and Developmental Biology, Faculty of Sciences, Charles University and 5 Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic

Received date March 13, 2006
Accepted date April 18, 2006
On-line available June 22, 2006



Summary
A novel derivative of 6-methyluracil, C-547, increased the amplitude and prolonged the duration of miniature endplate currents (MEPCs) which is typical for acetylcholinesterase inhibition. In the soleus and extensor digitorum longus significant potentiation was detected at nanomolar concentrations. In contrast, in the diaphragm muscle, the increase in the amplitudes of the MEPCs and the decay time constant  appeared only when the concentration of C-547 was elevated to 1x10-7 M. Possible consequences for the exploitation of this drug, which can selectively inhibit AChE in particular synapses, are discussed.


Key words
Miniature endplate current • Acetylcholinesterase • Anticholinesterase


© 2006 by the Institute of Physiology, Czech Academy of Sciences