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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2000-6-29
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pubmed:abstractText |
Previous work in our laboratories investigating compounds with structural similarity to ifenprodil (5) and 6 (CP101,606) resulted in compound 7 as a potent and selective antagonist of the NR1/2B subtype of the NMDA receptors. Replacement of the phenol group of 7 with a benzimidazalone group tethered by a three-carbon chain to 4-benzylpiperidine resulted in a slightly less active, but selective, compound. Lengthening the carbon tether resulted in a decrease in NR1/2B potency. Replacement of the phenol ring with a hydantoin resulted in weak antagonists. Compound 11a was one of the most potent NR1/2B antagonists from this study. Compound 11a also potentiated the effects of L-DOPA in a rat model of Parkinson's disease (the 6-hydroxydopamine-lesioned rat), dosed at 30 mg/kg orally.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Benzimidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Excitatory Amino Acid Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Hydantoins,
http://linkedlifedata.com/resource/pubmed/chemical/Neuroprotective Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Oxidopamine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, N-Methyl-D-Aspartate,
http://linkedlifedata.com/resource/pubmed/chemical/Sympatholytics,
http://linkedlifedata.com/resource/pubmed/chemical/ifenprodil
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
4
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1892-7
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:10794706-Animals,
pubmed-meshheading:10794706-Benzimidazoles,
pubmed-meshheading:10794706-Electrophysiology,
pubmed-meshheading:10794706-Excitatory Amino Acid Antagonists,
pubmed-meshheading:10794706-Hydantoins,
pubmed-meshheading:10794706-Hydrogen Bonding,
pubmed-meshheading:10794706-Male,
pubmed-meshheading:10794706-Neuroprotective Agents,
pubmed-meshheading:10794706-Oocytes,
pubmed-meshheading:10794706-Oxidopamine,
pubmed-meshheading:10794706-Parkinson Disease, Secondary,
pubmed-meshheading:10794706-Piperidines,
pubmed-meshheading:10794706-RNA, Messenger,
pubmed-meshheading:10794706-Rats,
pubmed-meshheading:10794706-Rats, Sprague-Dawley,
pubmed-meshheading:10794706-Receptors, N-Methyl-D-Aspartate,
pubmed-meshheading:10794706-Sympatholytics,
pubmed-meshheading:10794706-Xenopus
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pubmed:year |
2000
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pubmed:articleTitle |
Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.
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pubmed:affiliation |
CoCensys, Inc., 213 Technology Drive, Irvine, California 92618, USA.
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pubmed:publicationType |
Journal Article
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