Channel blocking drugs as tools to study glutamate receptors in insect muscles and molluscan neurons
Purchase on Springer.com
$39.95 / €34.95 / £29.95*
Rent the article at a discountRent now
* Final gross prices may vary according to local VAT.
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.
- Arvanov, V. L., Tsai, M. C., Walker, R. J. and Ayrapetyan, S. N. (1993) Interaction of concanavalin-A and wheat germ agglutinin withHelix acetylcholine receptors.Brain Res.,615, 252–258. CrossRef
- Arvanov, V. L., Chou, H. C., Chen, Y. H., Chen, R. C., Chang, Y. C. and Tsai, M. C. (1995) Effects of concanavalin A on desensitisation kinetics of GABA responses inAchatina fulica neurons.Cell Biol. Toxicol.,11, 113–118. CrossRef
- 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. CrossRef
- 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.
- Brundell, P., Goodnow, R., Jr., Kerry, C. J., Nakanishi, K., Sudan, H. L. and Usherwood, P. N. (1991) Quisqualate-sensitive glutamate receptors of the locustSchistocerca gregaria are antagonised by intracellularly applied philanthotoxin and spermine.Neurosci. Lett.,131, 196–200. CrossRef
- Burnashev, N., Monyer, H., Seeburg, P. H. and Sakmann, B. (1992) Divalent ion permeability of AMPA receptor channels is dominated by the edited form of a single subunit.Neuron,8, 189–198. CrossRef
- 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.
- Clark, R. B., Donaldson, P. L., Gration, K. A. F., Lambert, J. J., Piek, T., Ramsey, R., Spanjer, W. and Usherwood, P. N. R. (1982) Block of locust muscle glutamate receptor by delta-philanthotoxin occurs after receptor activation.Brain Res.,241, 105–114. CrossRef
- 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.
- Darlison, M. G. (1992) Invertebrate GABA and glutamate receptors: molecular biology reveals predictable structures but some unusual pharmacologies.Trends Neurosci.,15, 469–474. CrossRef
- 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).
- Ger, B. A., Katchman, A. N. and Zeimal, E. V. (1979) Biphasic acetylcholine responses of molluscan neurones: their dependence on acetylcholine concentration.Brain Res.,167, 426–430. CrossRef
- Herlitze, S., Raditsch, M., Ruppersberg, J. P., Jahn, W., Monyer, H., Schoepfer, R. and Witzemann, V. (1993) Argiotoxin detects molecular differences in AMPA receptor channels.Neuron,10, 1131–1140. CrossRef
- Hollmann, M. and Heinemann, S. F. (1994) Cloned glutamate receptors.Annu. Rev. Neurosci.,17, 31–108. CrossRef
- 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.
- 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.
- Ikemoto, Y., and Akaike, N. (1988) The glutamate-induced chloride current in Aplysia neurones lacks pharmacological properties seen for excitatory responses to glutamate.Eur. J. Pharmacol.,150, 313–318. CrossRef
- 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.
- Kehoe, J. S. (1978) Transformation by concanavalin A of the response of molluscan neurones to L-glutamate.Nature,274, 866–869. CrossRef
- Kerry, C. J., Ramsey, R. L., Sansom, M. S. P. and Usherwood, P. N. R. (1988) Single channel studies of non-competitive antagonism of a quisqualate-sensitive glutamate receptor by argiotoxin-636-a fraction isolated from orb-web spider venom.Brain Res.,459, 312–327. CrossRef
- Lea, T. J. and Usherwood, P. N. R. (1973) The site of action of ibotenic acid and the identification of two populations of glutamate receptors on insect muscle fibres.Comp. Gen. Pharmacol.,4, 333–350. CrossRef
- Lingle, C. and Marder, E. (1981) A glutamate-activated chloride conductance on a crustacean muscle.Brain Res.,212, 481–488. CrossRef
- 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.
- Mathers, D. A. and Usherwood, P. N. R. (1976) Concanavalin A blocks desensitisation of glutamate receptors on insect muscle fibres.Nature,259, 409–411. CrossRef
- 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.
- 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.
- 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.
- Yarowsky P. J. and Carpenter D. O. (1976) Asparate: distinct receptors on Aplysia neurons.Science,192, 807–809.
- Channel blocking drugs as tools to study glutamate receptors in insect muscles and molluscan neurons
Volume 3, Issue 2-3 , pp 117-126
- Cover Date
- Print ISSN
- Online ISSN
- Additional Links
- glutamate receptors
- open-channel block
- Industry Sectors
- 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