Summary
Neuronal primary cultures of Periplaneta americana and Locusta migratoria have been used to study the biophysical and pharmacological properties of the insect GABA receptor using single channel techniques. The insect GABA receptor mediated an increase in chloride conductance, which was blocked by picrotoxin but was insensitive to bicuculline. The vertebrate GABAA agonists isoguvacine, muscimol and ZAPA were potent agonists of the insect GABA receptor but the sulphonic acids 3-amino propane acid and 4-piperizine, which are also agonists of the GABAA receptor, were inactive or only weakly active at the insect GABA receptor.
The gating of the insect GABA receptor was found to involve at least two open and two closed states and the detection of a 35 pS main conductance state and at least three other conductance states associated with the receptor revealed that the insect GABA receptor is of comparable kinetics and conformational complexity to the vertebrate GABAA receptor.
The existence of modulatory sites for benzodiazepines and barbiturates in the insect GABA receptor was confirmed though benzodiazepine-insensitive neurones were also found. Noise and single channel analysis revealed that the mechanism underlying barbiturate enhancement of GABA responses was due to an increase in the mean channel open time.
Pharmacological and single channel studies confirmed that several groups of insecticides interfere with the insect GABA receptor. The mechanism underlying these interactions involves alteration of channel kinetics and reduction of channel conductance.
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© 1993 Birkhäuser Verlag Basel/Switzerland
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Taylor, A., Bermudez, I., Beadle, D.J. (1993). Pharmacology of the GABA receptor of insect central neurones in culture: A patch-clamp study. In: Pichon, Y. (eds) Comparative Molecular Neurobiology. EXS, vol 63. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7265-2_7
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DOI: https://doi.org/10.1007/978-3-0348-7265-2_7
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