Abstract
A model of the cation-selective channel gated by the quisqualatesensitive glutamate receptor (G1uR) of locust muscle is described. This model is based, in part, upon the vertebrate, nicotinic acetylcholine receptor channel with which the G1uR channel has many properties in common. The GluR channel is c. 140Å in length and an integral part of the proposed tetrameric glutamate receptor protein. It has an outer vestibule, 30Å in diameter at its extracellular face, which narrows at the channel gate to a c. 45Å long ion-selectivity filter terminating on the cytoplasmic face of the G1uR. The channel is lined by fixed -ve charges to which permeating cations bind and has a hydrophobic pocket just external to the selectivity filter. Chlorisondamine, an organic cation with a maximum dimension of 9.8Å, passes through the channel at high membrane potentials. This fixes the minimum dimension of the selectivity filter at c. 10Å. The argiotoxins and philanthotoxin should permeate the channel, but perhaps only at high membrane potentials, but the high affinity of these flexible, polycationic molecules for the fixed charges on the channel wall makes them potent open channel blockers. If these toxins compete with divalent cations for the fixed charges on membrane proteins, then competition between Joro spider toxin for Ca2+-bindings sites on the crustacean muscle GluR could cause closed channel block since Ca2+ is a requirement for channel gating in this system, but not for the locust GluR. Interactions with acidic groups of membrane phospholipids may lead to changes in membrane flexibility which could account for some of the effects of these toxins on GluR.
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Usherwood, P.N.R., Blagbrough, I.S. (1989). Antagonism of Insect Muscle Glutamate Receptors — with Particular Reference to Arthropod Toxins. In: Narahashi, T., Chambers, J.E. (eds) Insecticide Action. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-1324-3_2
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DOI: https://doi.org/10.1007/978-1-4684-1324-3_2
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