Kaitocephalin antagonism of glutamate receptors expressed in xenopus oocytes

Agenor Limon-Ruiz, Jorge M. Reyes-Ruiz, Rishi G. Vaswani, A. Richard Chamberlin, Ricardo Miledi

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

Kaitocephalin is the first discovered natural toxin with protective properties against excitotoxic death of cultured neurons induced by N-methyl-d-aspartate (NMDA) or -amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA)/kainic acid (kainate, KA) receptors. Nevertheless, the effects of kaitocephalin on the function of these receptors were unknown. In this work, we report some pharmacological properties of synthetic (-)-kaitocephalin on rat brain glutamate receptors expressed in Xenopus laevis oocytes and on the homomeric AMPA-type GluR3 and KA-type GluR6 receptors. Kaitocephalin was found to be a more potent antagonist of NMDA receptors (IC50 = 75 ± 9 nM) than of AMPA receptors from cerebral cortex (IC50 = 242 ± 37 nM) and from homomeric GluR3 subunits (IC50 = 502 ± 55 nM). Moreover, kaitocephalin is a weak antagonist of the KA-type receptor GluR6 (IC50 100 M) and of metabotropic (IC50 > 100 M) glutamate receptors expressed by rat brain mRNA.

Original languageEnglish (US)
Pages (from-to)175-181
Number of pages7
JournalACS Chemical Neuroscience
Volume1
Issue number3
DOIs
StatePublished - Mar 17 2010
Externally publishedYes

Fingerprint

Glutamate Receptors
Xenopus
Inhibitory Concentration 50
Oocytes
Kainic Acid Receptors
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Rats
Brain
Isoxazoles
AMPA Receptors
Kainic Acid
Xenopus laevis
Aspartic Acid
Cerebral Cortex
Neurons
kaitocephalin
Pharmacology
Messenger RNA
Gluk2 kainate receptor

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

Cite this

Kaitocephalin antagonism of glutamate receptors expressed in xenopus oocytes. / Limon-Ruiz, Agenor; Reyes-Ruiz, Jorge M.; Vaswani, Rishi G.; Chamberlin, A. Richard; Miledi, Ricardo.

In: ACS Chemical Neuroscience, Vol. 1, No. 3, 17.03.2010, p. 175-181.

Research output: Contribution to journalArticle

Limon-Ruiz, A, Reyes-Ruiz, JM, Vaswani, RG, Chamberlin, AR & Miledi, R 2010, 'Kaitocephalin antagonism of glutamate receptors expressed in xenopus oocytes', ACS Chemical Neuroscience, vol. 1, no. 3, pp. 175-181. https://doi.org/10.1021/cn900037c
Limon-Ruiz, Agenor ; Reyes-Ruiz, Jorge M. ; Vaswani, Rishi G. ; Chamberlin, A. Richard ; Miledi, Ricardo. / Kaitocephalin antagonism of glutamate receptors expressed in xenopus oocytes. In: ACS Chemical Neuroscience. 2010 ; Vol. 1, No. 3. pp. 175-181.
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