Compounds > ufp-502
Page last updated: 2024-11-12

ufp-502

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

Cross-References

ID SourceID
PubMed CID10345770
CHEMBL ID109390
MeSH IDM0516153

Synonyms (5)

Synonym
CHEMBL109390 ,
ufp-502
bdbm50179191
(s)-n-((1h-benzo[d]imidazol-2-yl)methyl)-2-((s)-2-amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
h-dmt-tic-nh-ch2-bid
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.00010.00010.729810.0000AID497196
Delta-type opioid receptorMus musculus (house mouse)Ki0.00000.00000.53939.4000AID362403
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00000.00000.60689.2330AID362403; AID497193
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00050.00000.38458.6000AID362404; AID497194
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.03550.00020.660310.0000AID322691
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID497194Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
AID73682In vitro inhibitory activity against electrically evoked contractions of guinea pig ileum (GPI)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID256774Functional bioactivity against mu opioid receptor in guinea-pig ileum2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID322691Agonist activity at mu opioid receptor assessed as inhibition of electrically-stimulated Hartley guinea pig contraction2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
AID362404Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
AID497196Agonist activity at delta opioid receptor in mouse vas deference2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
AID256773Functional bioactivity against delta opioid receptor in mouse vas deferens2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID256771Displacement of [3H]DAMGO from rat mu opioid receptor in brain P2 synaptosomes2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID151746Inhibition of [3H]DAGO binding to Opioid receptor mu 1 of rat brain P2 synaptosomes2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID362403Displacement of [3H]deltorphin2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
AID139792Delta or Mu antagonist activity tested in mouse vas deferens (MVD) along with N,N-dimethyl-Dmt-Tic-OH2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID497347Agonist activity at mu opioid receptor in Hartley guinea pig small intestine2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
AID125450In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID322688Selectivity ratio of Sprague-Dawley rat mu opioid receptor to Sprague-Dawley rat delta opioid receptor2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
AID362420Selectivity ratio of Ki for mu opioid receptor in Sprague-Dawley rat brain to Ki for delta opioid receptor in Sprague-Dawley rat brain2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
AID362405Agonist activity at mu opioid receptor in Hartley guinea pig ileum myenteric plexus longitudinal muscle assessed as inhibition of electrically-stimulated muscle contraction2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
AID105933Negative logarithm of the molar concentration required to produce 50% of the maximum effect in mu receptor from mouse vas deferens (MVD)2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID151611Binding affinity for rat brain P2 synaptosome Opioid receptor mu 12002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID149792Inhibition of [3H]DPDPE binding to Opioid receptor delta 1 of rat brain P2 synaptosomes2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
AID73190Negative logarithm of the molar concentration of an agonist to produce 50% of the maximum effect in guinea pig ileum (mu receptor) determined by Salvadori et al.2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID149672Binding affinity at Opioid receptor delta 1 using rat brain receptor (P2 synaptosome) assay2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID322686Binding affinity to mu opioid receptor in Sprague-Dawley rat brain membrane2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
AID322687Binding affinity to delta opioid receptor in Sprague-Dawley rat brain membrane2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
AID362406Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
AID256770Displacement of [3H]deltorphin II from rat delta opioid receptor in brain P2 synaptosomes2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID497348Ratio of Ki for Sprague-Dawley rat mu opioid receptor to Ki for Sprague-Dawley rat delta opioid receptor2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
AID139793Delta or Mu antagonist activity tested in mouse vas deferens (MVD) along with, naloxone2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.
AID322689Agonist activity at delta opioid receptor assessed as inhibition of electrically-stimulated mouse vas deferens contraction2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
AID497193Displacement of [3H]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.
AID256772Selectivity for rat mu opioid receptor over delta opioid receptor2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
AID234756Relative binding to mu and delta opioid receptors (ratio of Ki)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (83.33)29.6817
2010's1 (16.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
dermorphin
dermorphin: opiate-like peptide present in amphibian skin		2.7130oligopeptide
deltorphin i, ala(2)-
deltorphin I, Ala(2)-: isolated from skin extracts of frogs belonging to the genus Phyllomedusa; has affinity to opioid receptors		2.4220peptide
h-dmt-tic-gly-nh-bzl
H-Dmt-Tic-Gly-NH-Bzl: bifunctional opioid ligand;structure in first source		2.4320
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.		02.0110