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  • 1
    ISSN: 1439-1104
    Keywords: philanthotoxins ; patch clamp ; locust muscle ; ionotropic glutamate receptor ; intracellular injection
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The effects of intracellularly-applied philanthotoxin-343 (PhTX-343) on single channel currents gated by quisqualate-sensitive glutamate receptors (qGluR) of locust leg muscle have been studied. PhTX-343 initially increased qGluR channel open probability, mainly by virtue of an increase in mean channel open time, but this was followed by a decrease in channel open probability, sometimes to zero, because of a decline in the frequency of channel openings and a decline in mean channel open time. These results suggest that antagonism of qGluR by PhTX-343 can arise, in part, through binding of the toxin to a site or sites on the intracellular domain of this receptor.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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  • 2
    ISSN: 1439-1104
    Keywords: glutamate receptors ; locust muscle ; photolabile philanthotoxins ; voltage clamp ; patch clamp
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The effects of philanthotoxin-343 (PhTX-343; tyrosyl-butanoyl-spermine) and photolabile analogues of this synthetic toxin on locust (Schistocerca gregaria) skeletal muscle have been investigated using whole muscle preparations (twitch contractions), single muscle fibres (excitatory postsynaptic currents (EPSCs)) and muscle membrane patches containing single quisqualate-sensitive glutamate receptors (qGluR). Analogues containing an azido group attached to either the butanoyl side-chain of PhTX-343 or as a substitute for the hydroxyl moiety of the tyrosyl residue were about 6 fold more potent antagonists than PhTX-343; those with an azido group located at the distal end of the toxin molecule were generally 2–3 fold less potent than PhTX-343. When these compounds were tested in subdued light, they were reversible antagonists of the muscle twitch, EPSC and qGluR. When a muscle was irradiated with U.V. during application of photolabile toxin combined with either neural stimulation of the muscle orl-glutamate application, antagonism of the twitch, EPSC and qGluR was complete and irreversible.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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