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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Reynolds, I. J. |
| Description | Author Affiliation: Reynolds IJ ( Department of Pharmacology, University of Pittsburgh, PA 15261.) |
| Abstract | 1. The mechanism of action of the arylalkylamine spider toxin, argiotoxin636, on the N-methyl-D-aspartate (NMDA) receptor was investigated by use of [3H]-dizocilpine binding to well-washed membranes obtained from rat brain. 2. Argiotoxin636 decreased [3H]-dizocilpine binding with an apparent potency of about 3 microM. The inhibition of [3H]-dizocilpine by argiotoxin636 was insensitive to the concentration of glutamate, glycine and spermidine in the assay. 3. Argiotoxin636 alone had no effect on the dissociation of [3H]-dizocilpine. However, argiotoxin636 reversed the actions of Mg2+ on the dissociation of [3H]-dizocilpine by decreasing the apparent potency of Mg2+. Argiotoxin636 also reversed the action of Ca2+ on the dissociation of [3H]-dizocilpine. 4. These results suggest that argiotoxin636 exerts a novel inhibitory effect on the NMDA receptor complex by binding to one of the Mg2+ sites located within the NMDA-operated ion channel. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 2 |
| Volume Number | 103 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 1991-06-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Magnesium Metabolism Phenylacetates Polyamines Receptors, N-Methyl-D-Aspartate Animals Binding, Competitive Drug Effects Brain Chemistry Dizocilpine Maleate In Vitro Techniques Indoleacetic Acids Ligands Pharmacology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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