Page last updated: 2024-12-07

tyrosyl-seryl(o-tert-butyl)-glycyl-phenylalanyl-leucyl-threonine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

tyrosyl-seryl(O-tert-butyl)-glycyl-phenylalanyl-leucyl-threonine: has good selectivity & high affinity for delta opioid receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID130662
CHEMBL ID298972
MeSH IDM0154756

Synonyms (17)

Synonym
(ser(2)(o-t-butyl)-leu(5))enkephalyl-thr(6)
leu(5) enkephalin, ser(2)(o-tert-butyl)-thr(6)
tyrosyl-seryl(o-tert-butyl)-glycyl-phenylalanyl-leucyl-threonine
l-threonine, n-(n-(n-(n-(o-(1,1-dimethylethyl)-n-l-tyrosyl-d-seryl)glycyl)-l-phenylalanyl)-l-leucyl)-
tyr-ser(o-tert-bu)-gly-phe-leu-thr
111035-56-4
dstbulet
CHEMBL298972 ,
bdbm50019053
2-{2-[2-(2-{2-[2-amino-3-(4-hydroxy-phenyl)-propionylamino]-3-tert-butoxy-propionylamino}-acetylamino)-3-phenyl-propionylamino]-4-methyl-pentanoylamino}-3-hydroxy-butyric acid
(2s,3r)-2-[[(2s)-2-[[(2s)-2-[[2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-[(2-methylpropan-2-yl)oxy]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoic acid
gtpl3873
DTXSID40149447
110786-67-9
tyr-d-ser(otbu)-gly-phe-leu-thr
tyr-d-ser(o-t-bu)-gly-phe-leu-thr
Q27077122

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" A dose-response curve was also made for the mu-opioid receptor agonist, morphine."( Spinal antinociception by Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr, a selective delta-opioid receptor agonist.
Dickenson, AH; Kalso, EA; McQuay, HJ; Sullivan, AF, 1992
)
0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00610.00000.60689.2330AID149938
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.37400.00000.38458.6000AID151897
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID149938Inhibition of [3H]DTLET binding torat brain membrane Opioid receptor delta 11988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
AID76226Inhibitory potency evaluated against electrically evoked contractions of guinea pig ileum1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
AID231531Ratio of binding affinity towards Mu receptor to that of Delta receptor1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
AID229264Ratio of IC50 for MVD to GPI1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
AID151897Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 11988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
AID132839Inhibitory potency evaluated against electrically evoked contractions of mouse vas deferens1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
AID1346361Human delta receptor (Opioid receptors)1988The Journal of biological chemistry, Mar-25, Volume: 263, Issue:9
[3H][D-Ser2(O-tert-butyl),Leu5]enkephalyl-Thr6 and [D-Ser2(O-tert-butyl),Leu5]enkephalyl-Thr6(O-tert-butyl). Two new enkephalin analogs with both a good selectivity and a high affinity toward delta-opioid binding sites.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (29.17)18.7374
1990's17 (70.83)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.42

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.42 (24.57)
Research Supply Index3.26 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]