Linked Life Data

14612191

Source:http://linkedlifedata.com/resource/pubmed/id/14612191

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
2003-11-12
pubmed:abstractText
H-Dmt-D-Arg-Phe-Lys-NH2 (Dmt=2',6'-dimethyltyrosine) ([Dmt1] DALDA) is a highly potent and selective micro opioid peptide agonist capable of producing an antinociceptive effect after systemic administration. Fluorescent analogues of [Dmt1] DALDA containing either beta-dansyl-L-alpha,beta-diaminopropionic acid [Dap(dns)] or beta-anthraniloyl-L-alpha,beta-diaminopropionic acid [Dap(atn)] in place of Lys4 were synthesized. Both analogues retained subnanomolar mu opioid receptor binding affinity, very high mu opioid agonist activity in the guinea pig ileum assay and extraordinarily high antinociceptive activity in the mouse tail-flick test (intrathecal administration). The maxima of the fluorescence emission spectra recorded in Tris-HCl buffer (pH 6.6) indicated a completely aqueous environment of the fluorophore in both peptides. The high fluorescence quantum yield (phi=0.358) of the [Dap(atn)4] analogue was particularly remarkable. These fluorescent [Dmt1] DALDA analogues represent valuable pharmacological tools for various applications, including studies on the binding to receptors and other biopolymers, cellular uptake and intracellular distribution, and tissue distribution.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0196-9781
pubmed:author
pubmed:issnType
Print
pubmed:volume
24
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1195-200
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2003
pubmed:articleTitle
Highly potent fluorescent analogues of the opioid peptide [Dmt1] DALDA.
pubmed:affiliation
Laboratory of Chemical Biology and Peptide Research, Clinical Research Institute of Montreal, 110 Pine Avenue West, Montreal, Quebec, Canada H2W 1R7.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.