Effects of velnacrine, tacrine and physostigmine on tetanic twitch responses at the rat neuromuscular junction.
The effects of velnacrine (1-hydroxytacrine), tacrine and physostigmine on indirectly elicited twitch at low and high stimulation frequencies were analyzed in the rat phrenic hemidiaphragm preparation. At 0.2 Hz, velnacrine and physostigmine behaved in a similar manner, the latter showing a higher potentiating effect. This potentiation was observed at 3-100 microM velnacrine, whereas a slight depression appeared at higher concentrations. When tetanic responses were studied, the drug concentrations needed to depress tetanic tension and tetanic fade were quite different in the case of velnacrine (depression of tetanic tension from 1 microM and tetanic fade from 170 microM), whereas physostigmine and tacrine were able to affect these parameters at very similar concentrations. The results suggest that some effects of velnacrine could differ from those of tacrine in spite of the chemical similarity.
Bosch
F
F
Departament de Farmacologia i Psiquiatria, Facultat Medicina, Universitat Autònoma de Barcelona, Bellaterra, Spain.
Morales
M
M
Badia
A
A
Baños
J E
JE
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D003964:Diaphragm / Q000502:physiology; D004558:Electric Stimulation; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009469:Neuromuscular Junction / Q000187:drug effects* / Q000502:physiology; D010791:Phrenic Nerve / Q000502:physiology; D010830:Physostigmine / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013619:Tacrine / Q000031:analogs & derivatives* / Q000494:pharmacology
D002800:Cholinesterase Inhibitors; D013619:Tacrine; D010830:Physostigmine; C056424:velnacrine