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Effect of agmatine on heteromeric N-methyl-D-aspartate receptor channels.
Neurosci Res. 2005 Aug; 52(4):387-92.NR

Abstract

Endogenous polyamines like spermine are known to have four distinct effects on recombinant N-methyl-d-aspartate (NMDA) receptor channels: voltage-dependent inhibition, glycine-dependent stimulation, glycine-independent stimulation and decreased affinity to the agonist (l-glutamate). These effects are highly dependent on the constituting epsilon subunits (epsilon1-epsilon4) of the recombinant NMDA receptor channels. Agmatine reportedly inhibits native NMDA receptor channels in cultured hippocampal neurons. In the present investigation, the effects of agmatine on the epsilon/zeta heteromeric NMDA receptor channels expressed in Xenopus laevis oocytes were examined using the two-electrode voltage clamp method. Agmatine inhibited the four epsilon/zeta (epsilon1/zeta1, epsilon2/zeta1, epsilon3/zeta1 and epsilon4/zeta1) channels with similar sensitivity (an IC50 value of about 300microM at -70mV). This effect was dependent on the membrane potential and was more pronounced at hyperpolarized membrane potentials (voltage-dependent inhibition). Agmatine did not exhibit other stimulatory (glycine-dependent and -independent effects) or inhibitory (decreased affinity to l-glutamate) effects. These properties are similar to the pharmacological profile of well-characterized NMDA receptor channel blockers like phencyclidine and ketamine. Thus, regarding the effects on the NMDA receptor channels, agmatine is not like other endogenous polyamines rather it acts as a channel blocker.

Authors+Show Affiliations

Division of Anesthesiology, Niigata University Graduate School of Medical and Dental Sciences, Niigata 951-8510, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

15982768

Citation

Askalany, Ahmed R., et al. "Effect of Agmatine On Heteromeric N-methyl-D-aspartate Receptor Channels." Neuroscience Research, vol. 52, no. 4, 2005, pp. 387-92.
Askalany AR, Yamakura T, Petrenko AB, et al. Effect of agmatine on heteromeric N-methyl-D-aspartate receptor channels. Neurosci Res. 2005;52(4):387-92.
Askalany, A. R., Yamakura, T., Petrenko, A. B., Kohno, T., Sakimura, K., & Baba, H. (2005). Effect of agmatine on heteromeric N-methyl-D-aspartate receptor channels. Neuroscience Research, 52(4), 387-92.
Askalany AR, et al. Effect of Agmatine On Heteromeric N-methyl-D-aspartate Receptor Channels. Neurosci Res. 2005;52(4):387-92. PubMed PMID: 15982768.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of agmatine on heteromeric N-methyl-D-aspartate receptor channels. AU - Askalany,Ahmed R, AU - Yamakura,Tomohiro, AU - Petrenko,Andrey B, AU - Kohno,Tatsuro, AU - Sakimura,Kenji, AU - Baba,Hiroshi, PY - 2005/01/06/received PY - 2005/04/23/revised PY - 2005/05/10/accepted PY - 2005/6/29/pubmed PY - 2005/10/1/medline PY - 2005/6/29/entrez SP - 387 EP - 92 JF - Neuroscience research JO - Neurosci Res VL - 52 IS - 4 N2 - Endogenous polyamines like spermine are known to have four distinct effects on recombinant N-methyl-d-aspartate (NMDA) receptor channels: voltage-dependent inhibition, glycine-dependent stimulation, glycine-independent stimulation and decreased affinity to the agonist (l-glutamate). These effects are highly dependent on the constituting epsilon subunits (epsilon1-epsilon4) of the recombinant NMDA receptor channels. Agmatine reportedly inhibits native NMDA receptor channels in cultured hippocampal neurons. In the present investigation, the effects of agmatine on the epsilon/zeta heteromeric NMDA receptor channels expressed in Xenopus laevis oocytes were examined using the two-electrode voltage clamp method. Agmatine inhibited the four epsilon/zeta (epsilon1/zeta1, epsilon2/zeta1, epsilon3/zeta1 and epsilon4/zeta1) channels with similar sensitivity (an IC50 value of about 300microM at -70mV). This effect was dependent on the membrane potential and was more pronounced at hyperpolarized membrane potentials (voltage-dependent inhibition). Agmatine did not exhibit other stimulatory (glycine-dependent and -independent effects) or inhibitory (decreased affinity to l-glutamate) effects. These properties are similar to the pharmacological profile of well-characterized NMDA receptor channel blockers like phencyclidine and ketamine. Thus, regarding the effects on the NMDA receptor channels, agmatine is not like other endogenous polyamines rather it acts as a channel blocker. SN - 0168-0102 UR - https://www.unboundmedicine.com/medline/citation/15982768/Effect_of_agmatine_on_heteromeric_N_methyl_D_aspartate_receptor_channels_ DB - PRIME DP - Unbound Medicine ER -