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Submit ReviewConantokin-R
Description: Potent non-competitive NMDA antagonist
Biological Activity for Conantokin-R
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.
Licensing Information
Sold under license from University of Utah
Technical Data for Conantokin-R
| M. Wt | 3098.4 |
| Formula | C127H201N35O49S3 |
| Sequence |
GEXXVAKMAAXLARXNIAKGCKVNCYP (Modifications: X = Gla, Disulfide bridge between 21 - 25) |
| Storage | Store at -20°C |
| CAS Number | 202925-60-8 |
| PubChem ID | 90488802 |
| InChI Key | MJQQZSPLVNQFRB-HHXUSTKESA-N |
| Smiles | [H]NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C(O)=O)C(O)=O)C(=O)N[C@@H](CC(C(O)=O)C(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C(O)=O)C(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C(O)=O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC1=O)C(C)C)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N1CCC[C@H]1C(O)=O |
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.
Product Datasheets for Conantokin-R
References for Conantokin-R
References are publications that support the biological activity of the product.
Blandl et al (2000) Structure-function relationships of the NMDA-receptor antagonist peptide, conantokin-R. FEBS Lett. 470 139 PMID: 10734223
Klein et al (2001) The amino acid residue at sequence position 5 in the conantokin peptides partially governs subunit-selective antagonism of recombinant N-MthD.-aspartate receptors. J.Biol.Chem. 276 26860 PMID: 11335724
White et al (2000) 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. J.Pharmacol.Expr.Ther. 292 425
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Keywords: Conantokin-R, Conantokin-R supplier, Potent, non-competitive, NMDA, receptor, antagonists, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, venoms, GluN2, 3125, Tocris Bioscience
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