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The effects of alanine-substituted conantokin-G and ifenprodil on the human spermine-activated N-methyl-D-aspartate receptor.
Neuroscience. 2005; 130(2):457-64.N

Abstract

We evaluated the effects of Ala-7-conantokin-G (Con-G(A7)) and ifenprodil on the modulation by spermine of [(3)H]MK801 binding to human cortical membranes. Human cortical tissue was obtained at autopsy and stored at -80 degrees C until assay. Both Con-G(A7) and ifenprodil inhibited [(3)H]MK801 binding, but spermine affected these inhibitions differently. Con-G(A7) IC(50) changed little with spermine concentration, indicative of a non-competitive interaction, whereas the rightward shift in ifenprodil IC(50) with increasing spermine concentration suggested partial competition. When the two agents were tested against the biphasic activation of [(3)H]MK801 binding by spermine, they again differed in their effects. In the activation phase Con-G(A7) was a non-competitive inhibitor of spermine activation, and may even enhance the spermine EC(50), while the ifenprodil data indicated a partially competitive interaction. Both agents were non-competitive in the inhibitory phase. Overall, the data suggest that Con-G(A7) and ifenprodil interact differently with the polyamine modulation of the glutamate-N-methyl-D-aspartate receptor.

Authors+Show Affiliations

School of Molecular and Microbial Sciences, University of Queensland, Brisbane 4072, Australia.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15664702

Citation

Tsai, V W-W, et al. "The Effects of Alanine-substituted conantokin-G and Ifenprodil On the Human Spermine-activated N-methyl-D-aspartate Receptor." Neuroscience, vol. 130, no. 2, 2005, pp. 457-64.
Tsai VW, Dodd PR, Lewis RJ. The effects of alanine-substituted conantokin-G and ifenprodil on the human spermine-activated N-methyl-D-aspartate receptor. Neuroscience. 2005;130(2):457-64.
Tsai, V. W., Dodd, P. R., & Lewis, R. J. (2005). The effects of alanine-substituted conantokin-G and ifenprodil on the human spermine-activated N-methyl-D-aspartate receptor. Neuroscience, 130(2), 457-64.
Tsai VW, Dodd PR, Lewis RJ. The Effects of Alanine-substituted conantokin-G and Ifenprodil On the Human Spermine-activated N-methyl-D-aspartate Receptor. Neuroscience. 2005;130(2):457-64. PubMed PMID: 15664702.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The effects of alanine-substituted conantokin-G and ifenprodil on the human spermine-activated N-methyl-D-aspartate receptor. AU - Tsai,V W-W, AU - Dodd,P R, AU - Lewis,R J, PY - 2004/09/20/accepted PY - 2005/1/25/pubmed PY - 2005/4/26/medline PY - 2005/1/25/entrez SP - 457 EP - 64 JF - Neuroscience JO - Neuroscience VL - 130 IS - 2 N2 - We evaluated the effects of Ala-7-conantokin-G (Con-G(A7)) and ifenprodil on the modulation by spermine of [(3)H]MK801 binding to human cortical membranes. Human cortical tissue was obtained at autopsy and stored at -80 degrees C until assay. Both Con-G(A7) and ifenprodil inhibited [(3)H]MK801 binding, but spermine affected these inhibitions differently. Con-G(A7) IC(50) changed little with spermine concentration, indicative of a non-competitive interaction, whereas the rightward shift in ifenprodil IC(50) with increasing spermine concentration suggested partial competition. When the two agents were tested against the biphasic activation of [(3)H]MK801 binding by spermine, they again differed in their effects. In the activation phase Con-G(A7) was a non-competitive inhibitor of spermine activation, and may even enhance the spermine EC(50), while the ifenprodil data indicated a partially competitive interaction. Both agents were non-competitive in the inhibitory phase. Overall, the data suggest that Con-G(A7) and ifenprodil interact differently with the polyamine modulation of the glutamate-N-methyl-D-aspartate receptor. SN - 0306-4522 UR - https://www.unboundmedicine.com/medline/citation/15664702/The_effects_of_alanine_substituted_conantokin_G_and_ifenprodil_on_the_human_spermine_activated_N_methyl_D_aspartate_receptor_ DB - PRIME DP - Unbound Medicine ER -