Home LiteratureArticle Details
PMID: 6478036 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S. Research Support, U.S. Gov't, P.H.S.

Agonists block currents through acetylcholine receptor channels.

Biophysical journal ·Vol. 46 ·No. 2 ·1984-08-00 ·Pages 277-83

Sine SM, Steinbach JH

Abstract

We have examined the effects of high concentrations of cholinergic agonists on currents through single acetylcholine receptor (AChR) channels on clonal BC3H1 cells. We find that raised concentrations of acetylcholine (ACh; above 300 microM) or carbamylcholine (Carb; above 1,000 microM) produce a voltage- and concentration-dependent reduction in the mean single-channel current. Raised concentrations of suberyldicholine (Sub; above 3 microM) produce a voltage- and concentration-dependent increase in the number of brief duration low-conductance interruptions of open-channel currents. These observations can be quantitatively described by a model in which agonist molecules enter and transiently occlude the ion-channel of the AChR.

MeSH Terms
Acetylcholine/pharmacology Animals Carbachol/pharmacology Cell Line Choline/analogs & derivatives,pharmacology Clone Cells Electric Conductivity/drug effects Membrane Potentials/drug effects Mice Receptors, Cholinergic/drug effects,physiology
Chemicals
Receptors, Cholinergic subecholine Carbachol Choline Acetylcholine
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Sine S M
Steinbach J H
References (17)
17 references, click to expand
  1. Decamethonium in depolarized muscle and the effects of tubocurarine.
    J Physiol. 1970 Sep;210(2):345-61 PMID: 5501266
  2. Activation of a nicotinic acetylcholine receptor.
    Biophys J. 1984 Jan;45(1):175-85 PMID: 6324901
  3. Characterization of a unique muscle cell line.
    J Cell Biol. 1974 May;61(2):398-413 PMID: 4363958
  4. Sodium ions as blocking agents and charge carriers in the potassium channel of the squid giant axon.
    J Gen Physiol. 1977 Dec;70(6):707-24 PMID: 591920
  5. Local anaesthetics transiently block currents through single acetylcholine-receptor channels.
    J Physiol. 1978 Apr;277:153-76 PMID: 306437
  6. Interactions between intrinsic membrane protein and electric field. An approach to studying nerve excitability.
    Biophys J. 1978 May;22(2):295-306 PMID: 656546
  7. Decamethonium both opens and blocks endplate channels.
    Proc Natl Acad Sci U S A. 1978 Jun;75(6):2994-8 PMID: 307251
  8. Potassium channels as multi-ion single-file pores.
    J Gen Physiol. 1978 Oct;72(4):409-42 PMID: 722275
  9. Functional consequences of agonist-mediated state transitions in the cholinergic receptor. Studies in cultured muscle cells.
    J Biol Chem. 1979 May 10;254(9):3315-25 PMID: 429353
  10. Single acetylcholine-activated channels show burst-kinetics in presence of desensitizing concentrations of agonist.
    Nature. 1980 Jul 3;286(5768):71-3 PMID: 6248795
  11. The relationship between agonist occupation and the permeability response of the cholinergic receptor revealed by bound cobra alpha-toxin.
    J Biol Chem. 1980 Nov 10;255(21):10144-56 PMID: 7430118
  12. Relationship between reversible antagonist occupancy and the functional capacity of the acetylcholine receptor.
    J Biol Chem. 1981 Jul 10;256(13):6692-9 PMID: 7240238
  13. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches.
    Pflugers Arch. 1981 Aug;391(2):85-100 PMID: 6270629
  14. Block of endplate channels by permeant cations in frog skeletal muscle.
    J Gen Physiol. 1981 Dec;78(6):593-615 PMID: 6278050
  15. Curare can open and block ionic channels associated with cholinergic receptors.
    Nature. 1982 Jul 15;298(5871):272-5 PMID: 6283380
  16. Bis-quaternary ammonium blockers as structural probes of the sarcoplasmic reticulum K+ channel.
    J Gen Physiol. 1982 May;79(5):869-91 PMID: 6284862
  17. Ionic blockage of sodium channels in nerve.
    J Gen Physiol. 1973 Jun;61(6):687-708 PMID: 4541078
Article Info
Journal
Biophysical journal
Abbr.
Biophys J
ISSN
0006-3495
Published
1984-08-00
Pages
277-83
Language
English
Region
United States
NLM ID
0370626
PMCID
PMC1435044
Subset
IM
Grants
NINDS NIH HHS · NS-13719 · United States
Analysis Services
Analysis Services

Contact

No. 2 Wenbo Road, Zhangqiu District, Jinan, Shandong

Qilu Normal University · Genelibs Bioinformatics Lab

750 Shunhua Rd, Jinan

2F, Bldg F, University Science Park

Tel: 0531-88819269

WeChat Official Account

Follow our WeChat subscription account for real-time updates and the latest in medical and biological research.


Business Email

E-mail: product@genelibs.com