Pharmacological Actions of Some Cyclic Analogues of Choline

Overview

Journal Br J Pharmacol

Publisher Wiley

Specialty Pharmacology

Date 1984 Apr 1

PMID 6326923

Citations 1

Authors

B A Hemsworth

S M Shreeve

G B Veitch

Affiliations

Soon will be listed here.

Abstract

Two cyclic choline analogues (3-hydroxy-N,N- dimethylpiperidinium and 2-hydroxymethyl-N,N- dimethylpiperidinium ) and two cyclic homocholine analogues (4-hydroxy-N,N- dimethylpiperidinium and 3-hydroxymethyl-N,N- dimethylpiperidinium ) have been studied with regard to their actions at the cholinergic synapse. All the analogues had some direct depolarizing activity on the frog rectus abdominis muscle but they were less potent in this respect than acetylcholine. Compared to physostigmine, the analogues were weak inhibitors of cholinesterase enzymes. All the analogues were found to have a presynaptic blocking action on the rat phrenic nerve-hemidiaphragm preparation, which was reversed by choline. In addition, they all inhibited the high affinity transport of choline into synaptosomes but only the cyclic choline analogues were found to be acetylated by soluble choline acetyltransferase in vitro. We conclude that the hydroxypiperidinium analogues caused the presynaptic block seen at the neuromuscular junction by inhibiting acetylcholine synthesis.

Citing Articles

3-Hydroxy-N,N-dimethylpiperidinium: a precursor of a false cholinergic transmitter.

Hemsworth B, Shreeve S, Veitch G Br J Pharmacol. 1984; 82(2):477-84.

PMID: 6145473 PMC: 1987026. DOI: 10.1111/j.1476-5381.1984.tb10783.x.

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