F. Marino et al., INHIBITION OF ENDOGENOUS ACETYLCHOLINE-RELEASE BY BLOCKADE OF VOLTAGE-DEPENDENT CALCIUM CHANNELS IN ENTERIC NEURONS OF THE GUINEA-PIG COLON, Journal of Pharmacy and Pharmacology, 45(5), 1993, pp. 449-452
The effects on acetylcholine release from the guinea-pig colon of the
N-type calcium channel blocker omega-conotoxin GVIA (omega-conotoxin),
the L-type calcium channel blocker nifedipine and the putative blocke
r of T-type channels, flunarizine, have been investigated. Endogenous
basal acetylcholine release and electrically (1 Hz, 1 ms, 456 mA)-evok
ed overflow in the presence of cholinesterase inhibitor were studied.
omega-Conotoxin (1-10 nM) and nifedipine (0.03-3 muM) dose-dependently
inhibited basal and electrically-evoked acetylcholine release. Maxima
l inhibition of basal or electrically-evoked acetylcholine release was
about 40% for nifedipine and about 75% for omega-conotoxin. The poten
cy of nifedipine was inversely related to the external calcium concent
ration: its EC50 value in low-calcium medium (0.5 mM) was as low as 12
nm. Flunarizine inhibited acetylcholine release only at concentration
s higher than 0.2 muM. Our results are consistent with an involvement
of N- and L-type calcium channels in the control of the endogenous ace
tylcholine release from the guinea-pig colon.