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Invert Neurosci ; 9(2): 85-9, 2009 Nov.
Article in English | MEDLINE | ID: mdl-19847463

ABSTRACT

The actions of benzodiazepines were studied on the responses to GABA of the fast coxal depressor (D(f)) motor neurone of the cockroach, Periplaneta americana. Ro5-4864, diazepam and clonazepam were investigated. Responses to GABA receptors were enhanced by both Ro5-4864 and diazepam, whereas clonazepam, a potent-positive allosteric modulator of human GABA(A) receptors, was ineffective on the native insect GABA receptors of the D(f) motor neurone. Thus, clear pharmacological differences exist between insect and mammalian native GABA-gated chloride channels with respect to the actions of benzodiazepines. The results enhance our understanding of invertebrate GABA-gated chloride channels which have recently proved important in (a) comparative studies aimed at identifying human allosteric drug-binding sites and (b) understanding the actions of compounds used to control ectoparasites and insect crop pests.


Subject(s)
Benzodiazepines/pharmacology , Chloride Channels/metabolism , GABA Modulators/pharmacology , Insect Proteins/metabolism , Motor Neurons/drug effects , gamma-Aminobutyric Acid/metabolism , Animals , Benzodiazepines/administration & dosage , Benzodiazepinones/administration & dosage , Benzodiazepinones/pharmacology , Clonazepam/administration & dosage , Clonazepam/pharmacology , Diazepam/administration & dosage , Diazepam/pharmacology , Dose-Response Relationship, Drug , Evoked Potentials/drug effects , GABA Modulators/administration & dosage , Glutamic Acid/metabolism , In Vitro Techniques , Male , Membrane Potentials/drug effects , Microelectrodes , Motor Neurons/metabolism , Periplaneta
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