Conantokin G

Biological Activity

GluN2B (formally NR2B) selective, competitive antagonist of the NMDA receptor. Blocks NMDA-evoked current in mouse cortical neurons (IC₅₀ = 480 nM); also inhibits NMDA-evoked responses in oocytes expressing GluN2B (formally NR2B), but not GluN2A (formally NR2A), subunits (IC₅₀ ~300 nM). Exhibits neuroprotective properties in vivo and in vitro.

Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.

Background References

1. Conantokin G is an NR2B-selective competitive antagonist of N-methyl-D-aspartate receptors.
   Donevan and McCabe
   Mol.Pharmacol., 2000;58:614
2. Selective antagonism of nigral neuropeptide responses to methamphetamine by conantokin G, a naturally occurring conopeptide.
   Bush et al.
   Eur.J.Pharmacol., 2000;387:55
3. Neuroprotective efficacy and therapeutic window of the high-affinity N-methyl-D-aspartate antagonist conantokin-G: in vitro (primary cerebellar neurons) and in vivo (rat model of transient focal brain ischemia) studies.
   Williams et al.
   J.Pharmacol.Exp.Ther., 2000;294:378

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