Compounds > deltorphin ii, ile(5,6)-
Page last updated: 2024-12-08

deltorphin ii, ile(5,6)-

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

Description

deltorphin II, Ile(5,6)-: a highly selective delta agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID197381
CHEMBL ID433720
MeSH IDM0233558

Synonyms (9)

Synonym
tyr-d-ala-phe-gly-ile-ile-gly-nh2
(ile(5,6))deltorphin ii
deltorphin ii, ile(5,6)-
CHEMBL433720 ,
bdbm50057010
(s)-4-((s)-2-{(r)-2-[(s)-2-amino-3-(4-hydroxy-phenyl)-propionylamino]-propionylamino}-3-phenyl-propionylamino)-4-{(1s,2s)-1-[(1s,2s)-1-(carbamoylmethyl-carbamoyl)-2-methyl-butylcarbamoyl]-2-methyl-butylcarbamoyl}-butyric acid
(4s)-4-[[(2s)-2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]-5-[[(2s,3s)-1-[[(2s,3s)-1-[(2-amino-2-oxoethyl)amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic aci
138166-93-5
DTXSID00160512
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00140.00000.60689.2330AID149808; AID149945; AID149946; AID149947
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki3.18800.00000.38458.6000AID151910
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki10.00000.00000.18683.9500AID148600
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID138362The inhibitory concentration activity was measured on electrically induced contraction of the mouse vas deferens (MVD)1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID149947The binding affinity was measured using [3H]naltrindole against Opioid receptor delta 1 of rat brain1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID233884Selectivity ratio was measured as ratio of binding affinity of Mu opioid receptor to the binding affinity of delta opioid receptor ([3H]- DIDII.1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID79051The inhibitory concentration activity was measured on guinea pig ileum (GPI)1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID149808Inhibition against binding of radioligand [Ile5,6-3H]-deltorphin to membrane from baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor delta 12000Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
AID148600The binding affinity was measured using [3H]- U-69593 against Opioid receptor kappa 1 of rat brain1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID151910The binding affinity was measured using [3H]- DAGO against Opioid receptor mu 1 of rat brain1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID149946The binding affinity was measured using [3H]-DIDII against Opioid receptor delta 1 of rat brain1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
AID149945The binding affinity was measured using [3H]- TIPPsi against Opioid receptor delta 11997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (60.00)18.2507
2000's2 (40.00)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: 12.40

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 Index12.40 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.40)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
enkephalin, d-penicillamine (2,5)-
Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.. DPDPE : A heterodetic cyclic peptide that is a cyclic enkephalin analogue, having D-penicillaminyl residues located at positions 2 and 5, which form the heterocycle via a disulfide bond.		210heterodetic cyclic peptidedelta-opioid receptor agonist
enkephalin, ser(2), leu(5), thr(6)-
enkephalin, Ser(2), Leu(5), Thr(6)-: specific probe for the delta-opiate receptor subtype in brain membranes		210oligopeptide
enkephalin, leucine
Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.. Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties.		210pentapeptide;
peptide zwitterion		analgesic;
delta-opioid receptor agonist;
human metabolite;
mu-opioid receptor agonist;
neurotransmitter;
rat metabolite
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		210morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
enkephalin, ala(2)-mephe(4)-gly(5)-
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.		210
nociceptin
[no description available]		210organic molecular entity;
polypeptide		human metabolite;
rat metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9910