Nitromethylene actions on in situ and expressed insect nicotinic acetylcholine receptors.
Single channel recordings from dissociated housefly (Musca domestica) neurons show that a novel type of nitromethylene insecticide, 2(nitro-methylene)tetrahydro-1,3-thiazine (NMTHT) gates a channel, the conductance and open time histogram of which resemble those obtained when acetylcholine is the agonist. Injection into Xenopus oocytes of a locust (Schistocerca gregaria) alpha-subunit mRNA results in the expression of functional nicotinic receptors sensitive to NMTHT. Control oocytes injected with distilled water are insensitive to the same concentration of this compound. Thus NMTHT exhibits agonist actions at both in situ and expressed insect nicotinic receptors, and one site of action of this compound is on an insect nicotinic receptor alpha-subunit.
Leech
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AFRC Laboratory of Molecular Signalling, Department of Zoology, University of Cambridge, UK.
Jewess
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Marshall
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Sattelle
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DB
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D002038:Bungarotoxins / Q000494:pharmacology; D004175:Diptera; D004553:Electric Conductivity; D066298:In Vitro Techniques; D007306:Insecticides / Q000494:pharmacology*; D015640:Ion Channel Gating / Q000187:drug effects; D007473:Ion Channels / Q000187:drug effects*; D008564:Membrane Potentials / Q000187:drug effects; D009538:Nicotine / Q000494:pharmacology; D009865:Oocytes; D010526:Periplaneta; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000235:genetics; D011994:Recombinant Proteins; D013843:Thiazines / Q000494:pharmacology*; D014982:Xenopus laevis
D002038:Bungarotoxins; D007306:Insecticides; D007473:Ion Channels; D011978:Receptors, Nicotinic; D011994:Recombinant Proteins; D013843:Thiazines; D009538:Nicotine; C000613150:nithiazine; D000109:Acetylcholine