Channel blocking drugs as tools to study glutamate receptors in insect muscles and molluscan neurons
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The action of three dicationic drugs, derivatives of adamantane (IEM-1460 and IEM-1754) and phencyclidine (IEM-1925), on glutamate receptors (GluRs) at the insect neuromuscular junction (Calliphora vicina larva) and on neurons of the freshwater gastropodian molluscPlanorbarius corneus has been studied using the voltage clamp technique. In the presence of concanavalin A complex glutamate-induced currents recorded from molluscan neurons reflected mainly the opening of cationic channels as a result of decreased desensitisation and inhibition of a chloride component. Under these conditions all drugs studied inhibited the stationary component of glutamate-gated cationic currents in a dose-dependent manner (IC50s were 0.1 μM, 1.0 μM and 19.2 μM for the action of IEM-1925, IEM-1460 and IEM-1754 respectively). The same rank order of potency: IEM-1925 > IEM-1460 > IEM-1754 was observed in both the insect and mollusc. The results of these experiments are compared with those obtained earlier on vertebrate GluRs. Open-channel blocking drugs may help to identify and classify GluRs of invertebrates, and could be used as tools to elucidate the involvement of GluRs in the transmission at certain synapses.
Antonov, S. M., Dudel, J., Franke, C. and Hatt, H. (1989) Argiopine blocks glutamate-activated single-channel currents on crayfish muscle by two mechanisms.J. Physiol. (Lond.),419, 569–587.
Antonov, S. M., Johnson, J. W., Lukomskaya, N. Y., Potapjeva, N. N., Gmiro, V. E. and Magazanik, L. G. (1995) Novel adamantane derivatives act as blockers of open ligand-gated channels and as anticonvulsants.Mol. Pharmacol.,47, 558–567.PubMed
Bahls, F. H., Emery, D. G. and Haydon, P. G. (1995) Glutamatemediated synaptic transmission between neuron B4 and salivary cells ofHelisoma trivolvis.Invertebrate Neurosci.,1, 123–131.CrossRef
Blaschke, M., Keller, B. U., Rivosecchi, R., Hollmann, M., Heinemann, S. and Konnerth, A. (1993) A single amino acid determines the subunit-specific spider toxin block of α-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor channels.Proc. Natl. Acad. Sci. USA,90, 6528–6532.PubMedCrossRef
Bolshakov, V. Y., Gapon, S. A. and Magazanik, L. G. (1991) Different types of glutamate receptors in isolated and identified neurones of the molluscPlanorbarius corneus.J. Physiol. (Lond.),439, 15–35.
Bolshakov, V. Y., Gapon, S. A. and Magazanik, L. G. (1992) Transduction mechanism for glutamate-induced potassium current in neurones of the molluscPlanorbarius corneus.J. Physiol. (Lond.),455, 33–50.
Bolshakov, V. Y., Gapon, S. A., Katchman, A. N. and Magazanik, L. G. (1993) Activation of a common potassium channel in molluscan neurones by glutamate, dopamine and muscarinic agonist.J. Physiol. (Lond.) 468, 11–33.
Brackley, P. T. H., Bell, D. R., Choi, S. K., Nakanishi, K. and Usherwood, P. N. R. (1993) Selective antagonism of native and cloned kainate and NMDA receptors by polymine-containing toxins.J. Pharmacol. Exp. Ther.,266, 1573–1580.PubMed
Chang, H., Ciani, S. and Kidokoro, Y. (1994) Ion permeation properties of the glutamate receptor channel in cultured embryonicDrosophila myotubes.J. Physiol. (Lond.),476.1, 1–16.
Cleland, T. A. (1996) Inhibitory glutamate receptor channels.Molec. Neurobiol.,13, 97–136.
Cull-Candy, S. G. (1976) Two types of extrajunctional L-glutamate receptors in locust muscle fibres.J. Physiol. (Lond.),255, 449–464.
Dierkes, P. W., Hochstrate, P. and Schlue, W. R. (1996) Distribution and functional properties of glutamate receptors in the leech central nervous system.J. Neurophysiol.,75, 3212–2322.
Gapon, S. A. (1983) The effect of putative transmitters on identified neurones of the gastropod molluscPlanorbarius comeus.Z. Evol. Biokh. I. Fiziol.,19, 38–45 (in Russian).
Gapon S. A. and Samoilova M. V. (1982) The dercease of membrane conductance of isolated neurones under the action of putative transmitters in the molluscPlanorbarius corneus.Z. Evol. Biokh. I. Fiziol.,18, 535–538 (in Russian).
Hume, R. I., Dingledine, R. and Heinemann, S. F. (1991). Identification of a site in glutamate receptor subunits that controls calcium permeability.Science,253, 1028–1031.PubMed
Iino, M., Koike, M., Isa, T. and Ozawa, S. (1996) Voltage-dependent blockade of Ca2+-permeable AMPA receptors by Joro spider toxin in cultured rat hippocampal neurones.J. Physiol. (Lond.),424, 151–165.
Jan, L. Y. and Jan Y. N. (1976) L-Glutamate as an excitatory transmitter at theDrosophila larval neuromuscular junction.J. Physiol. (Lond.),262, 215–236.
Katz, P. S. and Levitan, I. B. (1993) Quisqualate and ACPD are agonists for a glutamate-activated current in identifiedAplysia neurons.J. Neurophysiol.,69, 143–150.PubMed
Magazanik, L. G. (1996) Spider neurotoxins as tools for the investigation of glutamate receptors.Toxin Rev.,15, 59–76.
Magazanik, L. G., Antonov, S. M., Fedorova, I. M., Volkova, T. M. and Grishin, E. V. (1986) Argiopin-a naturally occurring blocker of glutamate-sensitive synaptic channels.Biol. Membrany,3, 1204–1219 (in Russian).
Magazanik, L. G., Antonov, S. M. and Gmiro, V. E. (1984) Kinetics and pharmacological blockade of glutamate-activated postsynaptic ion channels.Biol. Membrany 1, 130–140 (in Russian).
Magazanik, L. G., Antonov, S. M., Lukomskaya, N. Y., Potapjeva, N. N., Gmiro, V. E. and Johnson, J. W. (1994) Admantane derivative induced block of acetylcholine, glutamate and NMDA activated open channels.Fiziol. Z.,80, 99–112 (in Russian).
Magazanik, L. G., Buldakova, S. A., Samoilova, M. V., Gmiro, V. E., Mellor, I. and Usherwood, P. N. R. (1997a) Block of open channels of recombinant AMPA receptors and native AMPA/kainate receptors by admantane derivatives.J. Physiol. (Lond.),505.3, 655–663.CrossRef
Magazanik, L. G., Buldakova, S. A., Samoilova, M. V., Mellor, I. and Usherwood, P. N. (1997b) Non-competitive antagonism of cloned and native AMPA/kainate receptors by adamantane derivatives.J. Physiol. (Lond.),501, 17P.
Samoilova, M. V., Frolova, E. V. and Magazanik, L. G. (1997) Glutamate receptors controlling cationic channels in the neurons of gastropod molluscPlanorbarius corneus.Z. Evol. Biokh. I. Fiziol.,33, 331–346 (in Russian).
Sudan, H. L., Kerry, C. J., Mellor, I. R., Choi, S.-K., Huang, D., Nakanishi, K. and Usherwood, P. N. R. (1995) The action of philanthotoxin-343 and photolabile analogues on locust (Schistocerca gregaria) muscle.Invertebrate Neurosci.,1, 139–172.
Stühmer, T., Amar, M., Harvey, R. J., Van Minnen, J. and Darlison, M. G. (1996) Structure and pharmacological properties of a molluscan glutamate-gated cation channel and its likely role in feeding behaviour.J. Neurosci.,16, 2869–2880.PubMed
Tsubokawa, H., Oguro, K., Masuzawa, T., Nakaima, T. and Kawai, N. (1995) Effects of a spider toxin and its analogue on glutamate-activated currents in the hippocampal CAI neuron after ischemia.J. Neurophysiol.,74, 218–225.PubMed
Usherwood, P. N. R. and Blagbrough, I. S. (1991) Spider toxins affecting glutamate receptors: polyamines in therapeutic neurochemistry.Pharmacol. Therap.,52, 245–268.CrossRef
Washburn, M. S., Numberger, M., Zhang, S. and Dingledine, R. (1997) Differential dependence on GluR2 expression of three characteristic features of AMPA receptors.J. Neurosci.,17, 9393–9406.PubMed
Yarowsky P. J. and Carpenter D. O. (1976) Asparate: distinct receptors on Aplysia neurons.Science,192, 807–809.PubMed
- Channel blocking drugs as tools to study glutamate receptors in insect muscles and molluscan neurons
Volume 3, Issue 2-3 , pp 117-126
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- glutamate receptors
- open-channel block
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- Author Affiliations
- 1. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia
- 2. Institute of Experimental Medicine, Russian Medical Academy of Sciences, St. Petersburg, Russia