Radioligand binding studies reveal agmatine is a more selective antagonist for a polyamine-site on the NMDA receptor than arcaine or ifenprodil

@article{Gibson2002RadioligandBS,
  title={Radioligand binding studies reveal agmatine is a more selective antagonist for a polyamine-site on the NMDA receptor than arcaine or ifenprodil},
  author={D. Alex Gibson and Barton R. Harris and Dennis Trent Rogers and John M. Littleton},
  journal={Brain Research},
  year={2002},
  volume={952},
  pages={71-77}
}
Neurosteroids Induce Allosteric Effects on the NMDA Receptor : Nanomolar Concentrations of Neurosteroids Exert Non-Genomic Effects on the NMDA Receptor Complex
TLDR
The interaction with the NR2B-selective antagonist ifenprodil indicates that this NMDA receptor subunit may be involved in neurosteroid-induced NG108-15 cell detachment.
Agmatine transport into spinal nerve terminals is modulated by polyamine analogs
TLDR
Results suggest that agmatine transport into spinal synaptosomes may be governed by a polyamine transport mechanism.
Agmatine Induces Antihyperalgesic Effects in Diabetic Rats and a Superadditive Interaction with R(–)-3-(2-Carboxypiperazine-4-yl)-propyl-1-phosphonic Acid, a N-Methyl-d-aspartate-Receptor Antagonist
TLDR
The present findings reveal that spinal agmatine produces antiallodynic and antihyperalgesic effects in diabetic neuropathic pain involving, at least for its antihyperAlgesic effect, the imidazoline receptors.
Agmatine: Biological role and therapeutic potentials in morphine analgesia and dependence
TLDR
The development of agmatinase inhibitors will offer a useful method to increase endogenous agmatine in the brain as a possible therapeutic approach to potentiate morphine analgesia and reduce dependence/ withdrawal.
Agmatine requires GluN2B-containing NMDA receptors to inhibit the development of neuropathic pain
TLDR
It is demonstrated that agmatine requires the GluN2B subunit of theNMDA receptor for inhibitory pharmacological actions in pre-clinical models of NMDA receptor-dependent hypersensitivity.
Borne Identity: Leading Endogenous Suspects at Imidazoline Binding Sites
TLDR
The current review collates and reports what is known about these substances and their functional significance at I-BS and concludes that the existence of these sites raises the question as to whether an endogenous modulator exists.
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Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with polyamines.
TLDR
Data indicate that ifenprodil may bind to the NMDA receptor in a state-dependent fashion and preferentially stabilize an inactivated form of the channel.
An allosteric interaction between the NMDA receptor polyamine and ifenprodil sites in rat cultured cortical neurones
TLDR
The interaction of spermine with both ifenprodil and the related NR2B selective antagonist Ro 8–4304 at the NMDA receptor in rat cultured cortical neurones in the presence of saturating concentrations of glycine was studied, supporting the suggestion that Mg2+ might be the physiological ligand acting at the sPermine site mediating glycine‐independent stimulation.
Arcaine uncovers dual interactions of polyamines with the N-methyl-D-aspartate receptor.
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TLDR
The findings suggest that polyamines do not activate or promote the activation of the NMDA receptor, but instead enhance [3H]MK801 binding by allosterically increasing ligand affinity.
Agmatine selectively blocks the N-methyl-D-aspartate subclass of glutamate receptor channels in rat hippocampal neurons.
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TLDR
The results indicate that in hippocampal neurons agmatine selectively modulates the NMDA subclass of glutamate receptor channels mediated by the interaction between the guanidine group and the channel pore, which support other data that ag matine may function as an endogenous neurotransmitter/neuromodulator in brain.
Inhibition of 5-HT3 receptor function by imidazolines in mouse neuroblastoma cells: potential involvement of σ2 binding sites
TLDR
The data suggest that imidazolines and σ-ligands, which as a rule possess low affinity for the 5-HT recognition site of the5-HT3 receptor, may be assumed to exert their inhibitory effect on cation influx through the 5.HT3 receptors channels, at least in part.
Agmatine acts as an antagonist of neuronal nicotinic receptors
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TLDR
The data suggest that agmatine acts both as a cation and as a weak channel blocker at neuronal nicotinic receptors at high concentrations, which is consistent with a non‐competitive effect of Agmatine.
Arcaine blocks N-methyl-D-aspartate receptor responses by an open channel mechanism: whole-cell and single-channel recording studies in cultured hippocampal neurons.
TLDR
Results indicate that arcaine inhibits NMDA-induced [3H]dizocilpine binding by blocking the open NMDA receptor channel, an action that is independent of the polyamine site.
Ifenprodil blocks N-methyl-D-aspartate receptors by a two-component mechanism.
TLDR
Results indicate that high affinity ifenprodil binding is extracellular and does not require agonist binding or channel opening, and intracellular factors may influence ifen Prodil efficacy.
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