Channel blocking drugs as tools to study glutamate receptors in insect muscles and molluscan neurons

@article{Samoilova2006ChannelBD,
  title={Channel blocking drugs as tools to study glutamate receptors in insect muscles and molluscan neurons},
  author={Marina V. Samoilova and E. V. Frolova and N. N. Potapjeva and Irina M. Fedorova and Valery E. Gmiro and Lev G Magazanik},
  journal={Invertebrate Neuroscience},
  year={2006},
  volume={3},
  pages={117-126}
}
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… 

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  • Chemistry, Medicine
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  • 2006
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References

SHOWING 1-10 OF 50 REFERENCES
Novel adamantane derivatives act as blockers of open ligand-gated channels and as anticonvulsants.
TLDR
Four novel adamantane derivatives appear to act on nicotinic ACh and NMDA receptors via similar mechanisms, although the voltage dependence of block suggested that the drugs bind at a more superficial site in the ACh-activated channel.
Quisqualate and ACPD are agonists for a glutamate-activated current in identified Aplysia neurons.
TLDR
The results indicate that the glutamate receptor mediating the outward potassium response does not conform in its pharmacological profile to any of the known vertebrate glutamate receptor types.
Activation of a common potassium channel in molluscan neurones by glutamate, dopamine and muscarinic agonist.
TLDR
Strong evidence was obtained against the involvement of any known secondary messenger systems (formation of nucleotides, phosphoinositide turnover and subsequent activation of protein kinase C, formation of nitric oxide, metabolism of arachidonic acid) in the transduction mechanism of F‐2268‐, dopamine‐ and glutamate‐induced responses.
Structure and Pharmacological Properties of a Molluscan Glutamate-Gated Cation Channel and its Likely Role in Feeding Behavior
TLDR
The pharmacological properties and deduced location of Lym-eGluR2 are entirely consistent with it being (a component of) the receptor that mediates the excitatory effects of glutamate released from neurons within the feeding central pattern generator.
Different types of glutamate receptors in isolated and identified neurones of the mollusc Planorbarius corneus.
TLDR
The data indicate that in the molluscan neurones studied there are at least three pharmacologically distinct glutamate receptors: (1) a receptor of quisqualate‐ibotenate type which directly controls chloride channel; (2) quisQualate and (3) kainate receptors which control in calcium‐independent manner the common potassium channel by activation of GTP‐binding protein.
Transduction mechanism for glutamate‐induced potassium current in neurones of the mollusc Planorbarius corneus.
TLDR
The failure to demonstrate the involvement of any known secondary messenger systems in glutamate response transduction favours two assumptions: (1) the receptor‐G protein complex controls the potassium channel directly; or (2) some still unknown transduction system is used.
Quisqualate-sensitive glutamate receptors of the locust Schistocerca gregaria are antagonised by intracellularly applied philanthotoxin and spermine
TLDR
It is proposed that spermine and the two toxins bind to the closed and open channel conformations of QUIS-R at a site near the intracellular opening of the channel gated by this receptor.
Spider toxins affecting glutamate receptors: polyamines in therapeutic neurochemistry.
TLDR
The sites and modes of action of these polyamine amide toxins are reviewed with particular reference to their structure-activity relationships and Electrophysiological studies, including those employing Xenopus oocytes, are reviewed and future prospects for the use of polyamines amides in therapy are discussed.
Block of locust muscle glutamate receptors by δ-philathotoxin occurs after receptor activations
TLDR
It is proposed that the toxin blocks open channels gated by both junctional and extrajunctional glutamate receptors on locust muscle and that δ-PTX enters a compartment of the muscle through the glutamate open channels and that it can also block the open channels from this site.
Distribution and functional properties of glutamate receptors in the leech central nervous system.
TLDR
It is concluded that in leech segmental ganglia the majority of the neurons and the neuropile glial cells, but probably not the mechanosensory neurons, possess glutamate receptors of the AMPA-kainate type.
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