| Title | Allosteric modulation by benzodiazepines of GABA-gated chloride channels of an identified insect motor neurone. | | Author(s) | Buckingham SD, Higashino Y, Sattelle DB | | Institution | MRC Functional Genomics Unit, Department of Physiology Anatomy and Genetics, University of Oxford, South Parks Road, Oxford, OX1 3QX, UK, steven.buckingham@dpag.ox.ac.uk. | | Source | Invert Neurosci 2009 Oct 22. | | 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19847463 |
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