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          Institute: MPI für medizinische Forschung     Collection: Abteilung Zellphysiologie     Display Documents

ID: 22729.0, MPI für medizinische Forschung / Abteilung Zellphysiologie
Pharmacology of the nicotinic acetylcholine receptor from fetal rat muscle expressed in Xenopus Oocytes
Translation of Title:Pharmacology of the nicotinic acetylcholine receptor from fetal rat muscle expressed in Xenopus Oocytes
Authors:Cooper, Julia C.; Gutbrod, Oliver; Witzemann, Veit; Methfessel, Christoph
Date of Publication (YYYY-MM-DD):1996-08-15
Title of Journal:European Journal of Pharmacology
Journal Abbrev.:European Journal of Pharmacology
Issue / Number:3
Start Page:287
End Page:298
Review Status:Peer-review
Audience:Experts Only
Intended Educational Use:No
Abstract / Description:The fetal rat muscle nicotinic acetylcholine receptor was expressed in Xenopus oocytes. Using the voltage-clamp technique, the response to a range of agonists was measured, listed in order of (decreasing) activity efficacy: anatoxin greater-than or equal to epibatidine > acetylcholine > DMPP (1,1-dimethyl-4-phenylpiperazinium) >> cytisine > pyrantel > nicotine > coniine > tubocurare > lobeline. The agonist responses were compared with the steric and electrostatic properties of the molecules, using molecular modelling. Single-channel currents were measured in outside-out patches for acetylcholine, nicotine, cytisine, anatoxin and epibatidine. The conductance of the single channels was independent of the type of agonist. The mean open times were characteristic of the agonist applied. Tubocurare, better known for its antagonist properties, was also a partial agonist. Single-channel currents were also observed for tubocurare, and for methyllycaconitine in patches with a very high density of the muscle nicotinic acetylcholine receptor, and these were blocked by small alpha, Greek-bungarotoxin. The agonist properties of physostigmine, galanthamine and their methyl derivatives were also investigated. The conductance of the channels observed in outside-out patches was similar to that obtained for the classical agonists. The single-channel currents observed for physostigmine, galanthamine and their methyl derivatives were blocked by small alpha, Greek-bungarotoxin, methyllycaconitine and mecamylamine, in contrast to previously reported studies on neuronal and adult muscle nicotinic acetylcholine receptors.
Free Keywords:Nicotinic acetylcholine receptor; Muscle, fetal, rat; Patch-clamp; Voltage-clamp; Molecular modelling; Nicotinic agonist; Non-competitive agonist;muscle; in vitro study; ligand binding; nicotinic receptor; nicotinic agent
External Publication Status:published
Document Type:Article
Communicated by:Wulf Kaiser
Affiliations:MPI für medizinische Forschung/Abteilung Zellphysiologie/
Identifiers:URI:http://www.sciencedirect.com/science?_ob=ArticleUR... [Abstract]
URI:http://www.sciencedirect.com/science?_ob=MImg&_ima... [Fulltext PDF]
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