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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2005-8-18
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pubmed:abstractText |
H-Dmt-d-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA) binds with high affinity and selectivity to the mu opioid receptor and is a potent and long-acting analgesic. Substitution of d-Arg in position 2 with Tic and masking of the lysine amine side chain by Z protection and of the C-terminal carboxylic function instead of the amide function transform a potent and selective mu agonist into a potent and selective delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. Such a delta antagonist could be used as a pharmacological tool.
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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 |
Aug
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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 |
25
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5608-11
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16107162-Animals,
pubmed-meshheading:16107162-Binding, Competitive,
pubmed-meshheading:16107162-Guinea Pigs,
pubmed-meshheading:16107162-Ileum,
pubmed-meshheading:16107162-Male,
pubmed-meshheading:16107162-Mice,
pubmed-meshheading:16107162-Muscle, Smooth,
pubmed-meshheading:16107162-Muscle Contraction,
pubmed-meshheading:16107162-Oligopeptides,
pubmed-meshheading:16107162-Rats,
pubmed-meshheading:16107162-Receptors, Opioid, delta,
pubmed-meshheading:16107162-Receptors, Opioid, mu,
pubmed-meshheading:16107162-Synaptosomes,
pubmed-meshheading:16107162-Vas Deferens
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pubmed:year |
2005
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pubmed:articleTitle |
From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.
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pubmed:affiliation |
Department of Toxicology, University of Cagliari, I-09124, Cagliari, Italy. gbalboni@unica.it
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pubmed:publicationType |
Journal Article,
In Vitro
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