TY - JOUR
T1 - Trapping of an open-channel blocker at the frog neuromuscular acetylcholine channel
AU - Neely, A.
AU - Lingle, C. J.
PY - 1986
Y1 - 1986
N2 - At the ganglionic nicotinic acetylcholine channel (Gurney, A. M., and H. P. Rang, 1984, Br. J. Pharmacol., 82:623–642) and on some cholinergic neuromuscular synapses of Crustacea (Lingle, C., 1983a, J. Physiol. (Lond.), 339:395–417; Lingle, C., 1983b, J. Physiol. (Lond.), 339:419–437), some agents that block cholinergic currents by an open-channel block mechanism appear to become trapped within the channel when it subsequently closes. It is unknown whether trapping of some open-channel blockers might also occur at the neuromuscular nicotinic acetylcholine channel. Here we show that the long-lived cholinergic blocking action of chlorisondamine, a ganglionic nicotinic blocker, can in part be most simply explained by an open-channel block mechanism followed by a subsequent trapping of the blocking molecule within the closed ion channel. Unique structural characteristics of the chlorisondamine molecule place several provocative constraints on the mechanism by which trapping may be occurring.
AB - At the ganglionic nicotinic acetylcholine channel (Gurney, A. M., and H. P. Rang, 1984, Br. J. Pharmacol., 82:623–642) and on some cholinergic neuromuscular synapses of Crustacea (Lingle, C., 1983a, J. Physiol. (Lond.), 339:395–417; Lingle, C., 1983b, J. Physiol. (Lond.), 339:419–437), some agents that block cholinergic currents by an open-channel block mechanism appear to become trapped within the channel when it subsequently closes. It is unknown whether trapping of some open-channel blockers might also occur at the neuromuscular nicotinic acetylcholine channel. Here we show that the long-lived cholinergic blocking action of chlorisondamine, a ganglionic nicotinic blocker, can in part be most simply explained by an open-channel block mechanism followed by a subsequent trapping of the blocking molecule within the closed ion channel. Unique structural characteristics of the chlorisondamine molecule place several provocative constraints on the mechanism by which trapping may be occurring.
UR - http://www.scopus.com/inward/record.url?scp=0023002078&partnerID=8YFLogxK
U2 - 10.1016/S0006-3495(86)83538-X
DO - 10.1016/S0006-3495(86)83538-X
M3 - Article
C2 - 3491634
AN - SCOPUS:0023002078
SN - 0006-3495
VL - 50
SP - 981
EP - 986
JO - Biophysical Journal
JF - Biophysical Journal
IS - 5
ER -