Document Detail


Conantokin-G: a novel peptide antagonist to the N-methyl-D-aspartic acid (NMDA) receptor.
MedLine Citation:
PMID:  2177176     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Conantokin-G is a 17 amino acid peptide isolated from the venom of the fish-eating snail Conus geographus which produces hyperactivity when injected into the brains of adult mice. We show that this peptide is a selective N-methyl-D-aspartate (NMDA) antagonist based on its ability to block NMDA-induced elevation of cGMP in rat cerebellar slices in vitro (IC50 = 171 nM), but not kainic acid-induced elevations. This inhibition could not be overcome by increasing the NMDA concentration, indicating non-competitive inhibition. Conantokin-G displayed no affinity for binding sites for thienylcyclohexylpiperidine, various glutamate subclasses or those for several other neurotransmitters/neuromodulators. This peptide, however, enhanced [3H]glycine binding to rat forebrain membranes but not to spinal cord membranes. The activity profile of the peptide in various assays indicates that it is a novel type of non-competitive NMDA antagonist.
Authors:
E E Mena; M F Gullak; M J Pagnozzi; K E Richter; J Rivier; L J Cruz; B M Olivera
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Neuroscience letters     Volume:  118     ISSN:  0304-3940     ISO Abbreviation:  Neurosci. Lett.     Publication Date:  1990 Oct 
Date Detail:
Created Date:  1991-02-28     Completed Date:  1991-02-28     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  7600130     Medline TA:  Neurosci Lett     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  241-4     Citation Subset:  IM    
Affiliation:
Department of Neuroscience, Pfizer Inc., Groton, CT 06340.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Sequence
Animals
Conotoxins*
Cyclic GMP / metabolism
Glutamates / metabolism
Glycine / metabolism
Kainic Acid / pharmacology
Molecular Sequence Data
N-Methylaspartate / antagonists & inhibitors
Peptides, Cyclic / pharmacology*
Phencyclidine / analogs & derivatives,  metabolism
Rats
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
Tritium / diagnostic use
Grant Support
ID/Acronym/Agency:
GM22737/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Conotoxins; 0/Glutamates; 0/Peptides, Cyclic; 0/Receptors, N-Methyl-D-Aspartate; 10028-17-8/Tritium; 21500-98-1/1-(1-(2-thienyl)cyclohexyl)piperidine; 487-79-6/Kainic Acid; 56-40-6/Glycine; 6384-92-5/N-Methylaspartate; 7665-99-8/Cyclic GMP; 77-10-1/Phencyclidine; 93438-65-4/conotoxin GV

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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