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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
24
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pubmed:dateCreated |
1998-1-12
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pubmed:abstractText |
Superpotent and highly delta-opioid receptor selective cyclic peptides of the general formula H-Tyr-c[D-Pen-Gly-Phe(p-X)-Pen]-Phe-OH (where X = hydrogen or halogen) have been synthesized. In the binding assays the most selective and most potent compound is the p-bromophenyl-alanine-4 analogue (IC50 value = 0.19 nM, selectivity ratio = 21,000 for delta vs mu). In the GPI and MVD bioassays the most selective and most potent analogue is the p-fluoro-substituted analogue Tyr-[D-Pen-Gly-Phe(p-F)-Pen]-Phe-OH. In the MVD assay it has an exceptionally low IC50 value of 0.016 nM and a delta vs mu selectivity ratio of 45,000.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
40
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3957-62
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:9397176-Amino Acid Sequence,
pubmed-meshheading:9397176-Analgesics,
pubmed-meshheading:9397176-Animals,
pubmed-meshheading:9397176-Enkephalins,
pubmed-meshheading:9397176-Guinea Pigs,
pubmed-meshheading:9397176-Kinetics,
pubmed-meshheading:9397176-Male,
pubmed-meshheading:9397176-Peptides, Cyclic,
pubmed-meshheading:9397176-Radioligand Assay,
pubmed-meshheading:9397176-Rats,
pubmed-meshheading:9397176-Rats, Sprague-Dawley,
pubmed-meshheading:9397176-Receptors, Opioid, delta,
pubmed-meshheading:9397176-Substrate Specificity
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pubmed:year |
1997
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pubmed:articleTitle |
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
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pubmed:affiliation |
Department of Chemistry, University of Arizona, Tucson 85721, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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