Abstract
The effects of catechol on various ionic channels of isolated primary afferent neurones of the bull-frog were examined by a single-suction-electrode clamp system, which combined internal perfusion and current or voltage clamp using an electronic switching circuit. Catechol was found to inhibit rather specifically the fast K+ current as does 4-aminopyridine (4-AP). Ca2+, Na+ and slow K+ currents were not affected. Although both 4-AP and catechol were inhibitors of the fast K+ channels, their sites of action were quite different. Catechol was effective when applied on the external surface of the cell membrane whereas 4-AP acted preferably internally. We assumed that a single fast K+ channel has two distinct sites for blockers: the catechol site is exposed to the external medium or situated at the outer orifice of the pore, and the 4-AP site is located within the same channel but is more easily accessible from inside the nerve cell than outside. The 4-AP and catechol sites were not, however, completely separate and independent of each other since a synergistic interaction was observed between catechol and 4-AP.
MeSH Terms
4-Aminopyridine
Action Potentials/drug effects
Aminopyridines/pharmacology
Animals
Calcium/physiology
Catechols/pharmacology
Depression, Chemical
Drug Interactions
In Vitro Techniques
Ion Channels/drug effects
Neurons, Afferent/physiology
Potassium/physiology
Rana catesbeiana
Sodium/physiology
Time Factors
Chemicals
Aminopyridines
Catechols
Ion Channels
Sodium
4-Aminopyridine
catechol
Potassium
Calcium
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Ito I
Maeno T
References (27)
27 references, click to expand
-
Convulsant action of polyphenols.
Nature. 1968 Jan 6;217(5123):84-5
PMID: 4384231
-
The action of phenolic substances on motor nerve endings.
J Pharmacol Exp Ther. 1963 Apr;140:41-5
PMID: 13940676
-
Inward and delayed outward membrane currents in isolated neural somata under voltage clamp.
J Physiol. 1971 Feb;213(1):1-19
PMID: 5575338
-
Voltage clamp studies of a transient outward membrane current in gastropod neural somata.
J Physiol. 1971 Feb;213(1):21-30
PMID: 5575340
-
Two fast transient current components during voltage clamp on snail neurons.
J Gen Physiol. 1971 Jul;58(1):36-53
PMID: 5564761
-
The facilitatory effects of catechol and phenol at the neuromuscular junction of the cat.
Neuropharmacology. 1971 Mar;10(21):153-9
PMID: 4328632
-
An analysis of the convulsant activity of substituted benzenes in the mouse.
Toxicol Appl Pharmacol. 1972 Feb;21(2):214-9
PMID: 4401923
-
Injections of calcium ions into spinal motoneurones.
J Physiol. 1972 Sep;225(2):363-90
PMID: 5074394
-
Catechol, a facilitatory drug that demonstrates only a prejunctional site of action.
J Pharmacol Exp Ther. 1973 Jan;184(1):129-35
PMID: 4686002
-
Potassium activation in Helix aspersa neurones under voltage clamp: a component mediated by calcium influx.
J Physiol. 1975 Jul;249(2):211-39
PMID: 1177091
-
Voltage clamping with a single microelectrode.
J Neurobiol. 1975 Jul;6(4):411-22
PMID: 1181381
-
3,4-diaminopyridine. A potent new potassium channel blocker.
Biophys J. 1978 Jun;22(3):507-12
PMID: 667299
-
Inhibition of voltage-dependent potassium conductance by convulsant phenols in the medical giant axon of the crayfish.
Comp Biochem Physiol C. 1980;65C(1):17-24
PMID: 6102009
-
Effects of 4-aminopyridine on potassium currents in a molluscan neuron.
J Gen Physiol. 1981 Jul;78(1):63-86
PMID: 6114129
-
Actions of verapamil, diltiazem and other divalent cations on the calcium-current of Helix neurones.
Br J Pharmacol. 1981 Sep;74(1):87-95
PMID: 7272605
-
Evidence for the existence of three types of potassium channels in the frog Ranvier node membrane.
J Physiol. 1981 Sep;318:297-316
PMID: 6275068
-
Ionic currents in the somatic membrane of rat dorsal root ganglion neurons-III. Potassium currents.
Neuroscience. 1981;6(12):2439-44
PMID: 6275296
-
Kinetic analysis of the action of chemical modulators on neuromuscular transmission.
Jpn J Physiol. 1981;31(5):639-56
PMID: 6120254
-
Pharmacological actions of aminopyridines and related compounds.
Rev Pure Appl Pharmacol Sci. 1981 Oct-Dec;2(4):317-71
PMID: 6278543
-
Intracellular Ca2+ activates a fast voltage-sensitive K+ current in vertebrate sympathetic neurones.
Nature. 1982 Apr 22;296(5859):746-9
PMID: 6280066
-
Cellular neurophysiological effects of phenol derivatives.
Comp Biochem Physiol C. 1982;73(2):231-41
PMID: 6129093
-
Site of action and active form of aminopyridines in squid axon membranes.
J Pharmacol Exp Ther. 1983 Jul;226(1):174-9
PMID: 6306223
-
Voltage-dependent activation of potassium current in Helix neurones by endogenous cellular calcium.
J Physiol. 1983 Jan;334:309-24
PMID: 6408248
-
Catechol and noradrenaline facilitate the neuromuscular transmission via different mechanisms.
Jpn J Physiol. 1983;33(3):497-502
PMID: 6138452
-
Internal perfusion studies demonstrating GABA-induced chloride responses in frog primary afferent neurons.
Am J Physiol. 1984 Mar;246(3 Pt 1):C259-65
PMID: 6608275
-
Separation of ionic currents in the somatic membrane of frog sensory neurons.
J Membr Biol. 1984;78(1):19-28
PMID: 6323715
-
The action of phenol on neuromuscular transmission in the red muscle of fish.
Jpn J Physiol. 1969 Dec;19(6):762-74
PMID: 5309117