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3-Hydroxy-N,N-dimethylpiperidinium: a precursor of a false cholinergic transmitter
- Source :
- British Journal of Pharmacology. 82:477-484
- Publication Year :
- 1984
- Publisher :
- Wiley, 1984.
-
Abstract
- A cyclic choline analogue, 3-hydroxy-N,N-dimethylpiperidinium, has been shown to be transported into a crude preparation of synaptosomes by high and low affinity transport mechanisms. Under conditions favouring the high affinity system the synaptosomes metabolized approximately 50% of the accumulated analogue to 3-acetoxy-N,N-dimethylpiperidinium, which was detected by paper electrophoresis. The phrenic nerve endplate region of a mouse hemidiaphragm accumulated 3-hydroxy-N,N-dimethylpiperidinium on nervous stimulation. This tissue metabolized approximately 60% of the accumulated analogue to the acetylated derivative which was released on nervous stimulation into the bathing medium. Compared to acetylcholine, 3-acetoxy-N,N-dimethylpiperidinium was shown to be 57 times less potent an agonist at the nicotinic receptors of the frog rectus abdominis muscle and 162 times less potent an agonist at the muscarinic receptors of the guinea-pig ileum. It is concluded that 3-hydroxy-N,N-dimethylpiperidinium is a precursor of a false cholinergic transmitter.
- Subjects :
- Agonist
medicine.medical_specialty
medicine.drug_class
Guinea Pigs
Nerve Tissue Proteins
Stimulation
In Vitro Techniques
Mice
Parasympathetic nervous system
chemistry.chemical_compound
Piperidines
Parasympathetic Nervous System
Internal medicine
Muscarinic acetylcholine receptor
medicine
Animals
Cholinesterases
Electrophoresis, Paper
Pharmacology
Neurotransmitter Agents
Chemistry
Brain
Muscle, Smooth
Acetylcholinesterase
Rats
Phrenic Nerve
medicine.anatomical_structure
Endocrinology
Cholinergic
Anura
medicine.symptom
Acetylcholine
Muscle Contraction
Synaptosomes
Research Article
medicine.drug
Muscle contraction
Subjects
Details
- ISSN :
- 00071188
- Volume :
- 82
- Database :
- OpenAIRE
- Journal :
- British Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....c8590d52d0164bf8c5ab0b7052da70ca