|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0002771,
umls-concept:C0031959,
umls-concept:C0036557,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243071,
umls-concept:C0243192,
umls-concept:C0597357,
umls-concept:C0631330,
umls-concept:C0871161,
umls-concept:C1417756,
umls-concept:C1883254
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
2007-1-17
|
|
pubmed:abstractText |
A series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues have been discovered as novel NOP receptor agonists. Structure-activity relationships have been explored via N-3 substitution of the benzimidazol-2-one with a range of functionality. The N-methyl acetamide derivative (+)-7f was found to be a high-affinity, potent NOP agonist with greater than 100-fold selectivity over the MOP receptor. Furthermore (+)-7f was shown to be both antinociceptive and sedative when administered iv to rodents.
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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
0968-0896
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
15
|
|
pubmed:volume |
15
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1828-47
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|
pubmed:meshHeading |
|
|
pubmed:year |
2007
|
|
pubmed:articleTitle |
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
|
|
pubmed:affiliation |
Department of Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, UK. r.palin@organon.co.uk
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|
pubmed:publicationType |
Journal Article
|
