Pharmacological actions of some cyclic analogues of choline

1 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 sy...

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Bibliographic Details
Published in:British journal of pharmacology 1984-04, Vol.81 (4), p.685-692
Main Authors: Hemsworth, B.A., Shreeve, S.M., Veitch, G.B.A.
Format: Article
Language:English
Subjects:
Abdominal Muscles - physiology
Acetylcholine - pharmacology
Animals
Biological Transport, Active
Brain - metabolism
Chemical Phenomena
Chemistry
Choline - metabolism
Choline - pharmacology
Cholinesterase Inhibitors - pharmacology
Electric Stimulation
In Vitro Techniques
Muscle Contraction - drug effects
Phrenic Nerve - physiology
Piperidines - metabolism
Piperidines - pharmacology
Ranidae
Rats
Synaptic Transmission
Synaptosomes - metabolism
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Summary:1 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. 2 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. 3 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. 4 We conclude that the hydroxypiperidinium analogues caused the presynaptic block seen at the neuromuscular junction by inhibiting acetylcholine synthesis.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1984.tb16135.x