Buckingham_1993_J.Exp.Biol_182_255

Reference

Title : Actions of vesamicol on an alpha-bungarotoxin-sensitive neuronal nicotinic acetylcholine receptor - Buckingham_1993_J.Exp.Biol_182_255
Author(s) : Buckingham SD , Lummis SC , Balk ML , Schroeder M , Sattelle DB
Ref : J Exp Biol , 182 :255 , 1993
Abstract :

Electrophysiology and binding studies were used to determine the actions of vesamicol [2-(4-phenylpiperidino)cyclohexanol (AH5183)] on an alpha-bungarotoxin-sensitive, neuronal nicotinic acetylcholine receptor in the nervous system of the cockroach, Periplaneta americana. Electrophysiological studies on an identified motor neurone revealed a reversible blocking action of (+/-)-vesamicol on the response to ionophoretically applied acetylcholine with an IC50 value of 8.0 x 10(-6) mol1(-1). The block was weakly voltage-dependent over the membrane potential range of -50 mV to -90 mV, and appeared to be non-competitive. No difference in potency was observed between the resolved stereoisomers. (+/-)-Vesamicol was found to suppress specific binding of 125I-labelled alpha-bungarotoxin to cockroach nervous tissue with an IC50 value of 5.1 x 10(-3) mol1(-1) and an estimated Hill coefficient of 0.73. Differences in the Hill coefficients were found when the resolved stereoisomers were tested separately. These data provide the first demonstration of a blocking action by vesamicol of a neuronal nicotinic acetylcholine receptor.

PubMedSearch : Buckingham_1993_J.Exp.Biol_182_255
PubMedID: 8228781

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Citations formats

Buckingham SD, Lummis SC, Balk ML, Schroeder M, Sattelle DB (1993)
Actions of vesamicol on an alpha-bungarotoxin-sensitive neuronal nicotinic acetylcholine receptor
J Exp Biol 182 :255

Buckingham SD, Lummis SC, Balk ML, Schroeder M, Sattelle DB (1993)
J Exp Biol 182 :255