| Phosphonate analogues of acidic amino acids: inhibition of excitatory amino acid transmitter binding to cerebellar membranes and of the stimulation of cerebellar cyclic GMP levels. | |
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MedLine Citation:
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PMID: 6124299 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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An examination was made of the ability of phosphonate analogues of acidic amino acids to interact with excitatory amino acid receptors, employing binding assays for [3H]glutamate and [3H]aspartate and by investigating the inhibitory effects of these compounds on the stimulation of cerebellar cyclic GMP levels. In both systems the phosphonates exhibited inhibitory activity, although the cGMP system corresponded better with electrophysiological data. The higher homologues (e.g. 2-amino-5-phosphonovalerate) showed high selectivity for NMDA-type receptors and this effect was stereospecific, with the (-)-isomers being at least 4-7 times more active than the (+)-forms. |
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Authors:
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P J Roberts; G A Foster; N A Sharif; J F Collins |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Brain research Volume: 238 ISSN: 0006-8993 ISO Abbreviation: Brain Res. Publication Date: 1982 Apr |
Date Detail:
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Created Date: 1982-09-10 Completed Date: 1982-09-10 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0045503 Medline TA: Brain Res Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 475-9 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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2-Amino-5-phosphonovalerate Alanine / analogs & derivatives*, pharmacology Amino Acids / metabolism Aminobutyric Acids / pharmacology* Animals Cerebellum / drug effects*, metabolism Cyclic GMP / metabolism* Rats Receptors, Amino Acid Receptors, Cell Surface / drug effects Receptors, Neurotransmitter / drug effects* Stereoisomerism Valine / analogs & derivatives*, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Amino Acids; 0/Aminobutyric Acids; 0/Receptors, Amino Acid; 0/Receptors, Cell Surface; 0/Receptors, Neurotransmitter; 56-41-7/Alanine; 5652-28-8/2-amino-3-phosphonopropionic acid; 6323-99-5/2-amino-4-phosphonobutyric acid; 7004-03-7/Valine; 7665-99-8/Cyclic GMP; 76726-92-6/2-Amino-5-phosphonovalerate |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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