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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2008-3-20
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pubmed:abstractText |
A series of potent indol-3-yl-tetramethylcyclopropyl ketones have been prepared as CB 2 cannabinoid receptor ligands. Two unsubstituted indoles ( 5, 32) were the starting points for an investigation of the effect of indole ring substitutions on CB 2 and CB 1 binding affinities and activity in a CB 2 in vitro functional assay. Indole ring substitutions had varying effects on CB 2 and CB 1 binding, but were generally detrimental to agonist activity. Substitution on the indole ring did lead to improved CB 2/CB 1 binding selectivity in some cases (i.e., 7- 9, 15- 20). All indoles with the morpholino-ethyl side chain ( 32- 43) exhibited weaker binding affinity and less agonist activity relative to that of their tetrahydropyranyl-methyl analogs ( 5- 31). Several agonists were active in the complete Freund's adjuvant model of chronic inflammatory thermal hyperalgesia ( 32, 15).
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:ChandranPrasantP,
pubmed-author:DartMichael JMJ,
pubmed-author:DazaAnthony VAV,
pubmed-author:El-KouhenOdile FOF,
pubmed-author:FrostJennifer MJM,
pubmed-author:GarrisonTiffany RTR,
pubmed-author:GraysonGeorge KGK,
pubmed-author:HsiehGin CGC,
pubmed-author:LiLanlanL,
pubmed-author:MeyerMichael DMD,
pubmed-author:MillerLoan NLN,
pubmed-author:PaiMadhaviM,
pubmed-author:TietjeKarin RKR,
pubmed-author:YaoBetty BBB,
pubmed-author:ZhuChang ZCZ
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pubmed:issnType |
Print
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pubmed:day |
27
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1904-12
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pubmed:meshHeading |
pubmed-meshheading:18311894-Animals,
pubmed-meshheading:18311894-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:18311894-Binding, Competitive,
pubmed-meshheading:18311894-Cell Line,
pubmed-meshheading:18311894-Disease Models, Animal,
pubmed-meshheading:18311894-Drug Evaluation, Preclinical,
pubmed-meshheading:18311894-Humans,
pubmed-meshheading:18311894-Hyperalgesia,
pubmed-meshheading:18311894-Indoles,
pubmed-meshheading:18311894-Ketones,
pubmed-meshheading:18311894-Ligands,
pubmed-meshheading:18311894-Molecular Conformation,
pubmed-meshheading:18311894-Rats,
pubmed-meshheading:18311894-Receptor, Cannabinoid, CB1,
pubmed-meshheading:18311894-Receptor, Cannabinoid, CB2,
pubmed-meshheading:18311894-Stereoisomerism,
pubmed-meshheading:18311894-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.
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pubmed:affiliation |
Neurological Diseases Research, Global Pharmaceutical Research & Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. jennifer.frost@abbott.com
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pubmed:publicationType |
Journal Article
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