Conantokin-R
Biological Activity
Potent, non-competitive NMDA receptor antagonist (IC50 = 93 nM) that has been suggested to have GluN2 (formally NR2) subunit selectivity. Inhibits inward currents evoked by NMDA in central nervous system neurons (IC50 = 350 nM) and exhibits broad anticonvulsant and antiparkinsonian activity in vivo at doses devoid of behavioral toxicity.Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data
(Modifications: X = Gla, Disulfide bridge between 21 - 25)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Structure-function relationships of the NMDA-receptor antagonist peptide, conantokin-R.
Blandl et al.
FEBS Lett., 2000;470:139 -
The amino acid residue at sequence position 5 in the conantokin peptides partially governs subunit-selective antagonism of recombinant N-MthD.-aspartate receptors.
Klein et al.
J.Biol.Chem., 2001;276:26860 -
In vitro and in vivo characterization of conantokin-R, a selective NMDA receptor antagonist isolated from the venom of the fish-hunting snail Conus radiatus.
White et al.
J.Pharmacol.Expr.Ther., 2000;292:425
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