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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
1997-6-27
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pubmed:abstractText |
A series consisting of spiroindanyl (5-7), benzospiroindanyl (8-10), and spiroperinaphthyl (11) derivatives of naltrexone and oxymorphone were synthesized in order to investigate the role of an orthogonal-oriented "address" for delta opioid receptors. All of the ligands exhibited a preference for delta receptors in vitro. The 7-benzospiroindanyl derivative 8 (BSINTX) was the most selective delta opioid receptor antagonist in vitro. In mice BSINTX antagonized the delta 1-selective agonist, [D-Pen2,D-Pen5]enkephalin without significantly affecting the antinociceptive potency of delta 2, mu, and kappa agonists. The results of this study are consistent with an orthogonally-oriented address favoring delta 1 activity.
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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/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, D-Penicillamine (2,5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalins,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Naltrexone,
http://linkedlifedata.com/resource/pubmed/chemical/Oxymorphone,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/Spiro Compounds
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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 |
23
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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 |
1720-5
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9171881-Analgesia,
pubmed-meshheading:9171881-Analgesics,
pubmed-meshheading:9171881-Animals,
pubmed-meshheading:9171881-Brain,
pubmed-meshheading:9171881-Cell Membrane,
pubmed-meshheading:9171881-Enkephalin, D-Penicillamine (2,5)-,
pubmed-meshheading:9171881-Enkephalins,
pubmed-meshheading:9171881-Guinea Pigs,
pubmed-meshheading:9171881-Ileum,
pubmed-meshheading:9171881-Ligands,
pubmed-meshheading:9171881-Male,
pubmed-meshheading:9171881-Mice,
pubmed-meshheading:9171881-Mice, Inbred ICR,
pubmed-meshheading:9171881-Molecular Structure,
pubmed-meshheading:9171881-Muscle, Smooth,
pubmed-meshheading:9171881-Naltrexone,
pubmed-meshheading:9171881-Oxymorphone,
pubmed-meshheading:9171881-Receptors, Opioid, delta,
pubmed-meshheading:9171881-Spiro Compounds,
pubmed-meshheading:9171881-Vas Deferens
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pubmed:year |
1997
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pubmed:articleTitle |
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.
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pubmed:affiliation |
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis 55455, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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