| The pharmacological selectivity of three NMDA antagonists. | |
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MedLine Citation:
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PMID: 2894999 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Three N-methyl-D-aspartate (NMDA) antagonists (+/-)2-amino-5-phosphonopentanoate (AP5), 3-((+/-)-2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP) and ((+/-)-5-methyl-10,11-dihydro-5H-dibenzo(a.d.)cyclohepten-5,10- imin e maleate) (MK-801) have been tested for selectivity against depolarization of motoneurones induced by carbachol, 5-hydroxytryptamine, noradrenaline and substance P in isolated immature rat spinal cord preparations. AP5 (400 microM) and CPP (50 microM) gave mean dose-ratios, for antagonism against NMDA, of 103 +/- 14.9 S.E.M. (eight preparations) and 34.1 +/- 1.9 S.E.M. (14 preparations). MK-801 (1 and 10 microM) was the most potent of the three antagonists yielding dose ratios greater than 100 after 120 min treatment. MK-801 potentiated responses induced by 5-hydroxytryptamine and noradrenaline given dose-ratios of 0.22 +/- 0.16 S.E.M. and 0.20 +/- 0.06 S.E.M., respectively (four preparations). The three antagonists produced no significant antagonism of the non-amino acid agonists (four preparations for each agonist) when dose-ratios against NMDA were at least 40. The observations support the use of these antagonists as tools to identify sites of excitatory amino acid-mediated transmission. |
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Authors:
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A M Childs; R H Evans; J C Watkins |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: European journal of pharmacology Volume: 145 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 1988 Jan |
Date Detail:
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Created Date: 1988-04-22 Completed Date: 1988-04-22 Revised Date: 2009-09-29 |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 81-6 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, The Medical School, Bristol, U.K. |
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 Animals Anticonvulsants / pharmacology* Aspartic Acid / analogs & derivatives*, antagonists & inhibitors Dibenzocycloheptenes / pharmacology* Dizocilpine Maleate Hexamethonium Compounds / pharmacology Motor Neurons / drug effects N-Methylaspartate Norepinephrine / pharmacology Piperazines / pharmacology* Rats Serotonin / pharmacology Synaptic Transmission / drug effects Valine / analogs & derivatives*, pharmacology |
| Grant Support | |
ID/Acronym/Agency:
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//Wellcome Trust |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Dibenzocycloheptenes; 0/Hexamethonium Compounds; 0/Piperazines; 100828-16-8/3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid; 50-67-9/Serotonin; 51-41-2/Norepinephrine; 56-84-8/Aspartic Acid; 6384-92-5/N-Methylaspartate; 7004-03-7/Valine; 76726-92-6/2-Amino-5-phosphonovalerate; 77086-22-7/Dizocilpine Maleate |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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