Journal article
Stereoisomers of quaternary and tertiary 4-methyl piperidine analogs of hemicholinium-3
The Journal of pharmacology and experimental therapeutics, Vol.247(2), pp.640-644
11/1988
DOI: 10.1016/S0022-3565(25)13413-7
PMID: 3183960
Abstract
Previous studies have shown that quaternary and tertiary 4-methyl piperidine derivatives of hemicholinium-3 (A-5 and A-4, respectively) are potent inhibitors of choline uptake. The d-, l-, and mesostereoisomers of A-5 and A-4 were separated and the potency and reversibility were compared. Isomeric forms of each compound were found to be approximately equipotent inhibitors in the following preparations: inhibition of rabbit neuromuscular transmission using the sciatic nerve-gastrocnemius muscle preparation, reductions in acetylcholine content in rat caudate tissue slices and inhibition of choline uptake in neuroblastoma cells, line NB41A3. Because these results show no difference in potency or reversibility for the stereoisomers of A-5 or A-4, these studies indicate that hydroxyl substitutions in these agents do not play a role in their biologic activity. Perhaps only 2-point attachment is required for inhibition of choline transport by hemicholinium-like compounds.
Details
- Title: Subtitle
- Stereoisomers of quaternary and tertiary 4-methyl piperidine analogs of hemicholinium-3
- Creators
- K Y Sheff - Department of Pharmacology, College of Medicine, University of Iowa, Iowa CityC E TedfordJ R FlynnM A YorekJ G CannonJ P Long
- Resource Type
- Journal article
- Publication Details
- The Journal of pharmacology and experimental therapeutics, Vol.247(2), pp.640-644
- DOI
- 10.1016/S0022-3565(25)13413-7
- PMID
- 3183960
- ISSN
- 0022-3565
- eISSN
- 1521-0103
- Language
- English
- Date published
- 11/1988
- Academic Unit
- Fraternal Order of Eagles Diabetes Research Center; Endocrinology and Metabolism; Internal Medicine
- Record Identifier
- 9984094610302771
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