Document Detail


The pharmacological selectivity of three NMDA antagonists.
MedLine Citation:
PMID:  2894999     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
A M Childs; R H Evans; J C Watkins
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmacology     Volume:  145     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1988 Jan 
Date Detail:
Created Date:  1988-04-22     Completed Date:  1988-04-22     Revised Date:  2009-09-29    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  81-6     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, The Medical School, Bristol, U.K.
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MeSH Terms
Descriptor/Qualifier:
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:
//Wellcome Trust
Chemical
Reg. No./Substance:
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

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