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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
11
|
| pubmed:dateCreated |
1994-7-7
|
| pubmed:abstractText |
To investigate delta-opioid receptor topography near the 3-position of [D-Pen2,D-Pen5]enkephalin (DPDPE), a series of small-group 3-position analogs of DPDPE have been synthesized and assayed for binding potencies and in vitro biological activities. L-Amino acid substitutions at this position are highly favored over D-amino acid substitutions, with the smallest, [L-Ala3]DPDPE (DPADPE), being the most favored in the series investigated. [L-Ala3]DPDPE is nearly as delta-potent and more delta-selective in both rat brain binding (18 nM vs [3H] [p-ClPhe4]DPDPE and mu/delta = 610) and peripheral bioassays (12 nM in the MVD and GPI/MVD = 4500) when compared to DPDPE (8.5 nM, mu/delta = 73 and 4.1 nM, GPI/MVD = 1800, respectively). Whereas DPDPE is a potent analgesic when given icv, [L-Ala3]DPDPE is only a weak analgesic. However, [L-Ala3]DPDPE has been found to antagonize DPDPE, but not Deltorphin II, in a moderately potent (pA2 = 5.7) and selective fashion in vivo. Thus, [L-Ala3]DPDPE is a fairly potent agonist at peripheral delta receptors and is a moderately potent (mixed) antagonist of delta 1 receptors in the brain. It appears that [L-Ala3]DPDPE does not interact in any significant manner with delta 2 or mu receptors in the brain.
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| 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/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
May
|
| pubmed:issn |
0022-2623
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
27
|
| pubmed:volume |
37
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
N
|
| pubmed:pagination |
1572-7
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:8201592-Amino Acid Sequence,
pubmed-meshheading:8201592-Analgesia,
pubmed-meshheading:8201592-Analgesics,
pubmed-meshheading:8201592-Animals,
pubmed-meshheading:8201592-Brain,
pubmed-meshheading:8201592-Cell Membrane,
pubmed-meshheading:8201592-Enkephalin, D-Penicillamine (2,5)-,
pubmed-meshheading:8201592-Enkephalins,
pubmed-meshheading:8201592-Guinea Pigs,
pubmed-meshheading:8201592-Male,
pubmed-meshheading:8201592-Mice,
pubmed-meshheading:8201592-Mice, Inbred ICR,
pubmed-meshheading:8201592-Molecular Sequence Data,
pubmed-meshheading:8201592-Rats,
pubmed-meshheading:8201592-Rats, Sprague-Dawley,
pubmed-meshheading:8201592-Receptors, Opioid, delta,
pubmed-meshheading:8201592-Receptors, Opioid, mu,
pubmed-meshheading:8201592-Stereoisomerism,
pubmed-meshheading:8201592-Structure-Activity Relationship
|
| pubmed:year |
1994
|
| pubmed:articleTitle |
[L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.
|
| pubmed:affiliation |
Department of Chemistry, University of Arizona, Tucson 85721.
|
| pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.
|