Page last updated: 2024-11-11

binaltorphimine

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

Description

binaltorphimine: kappa opiate receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5484197
CHEMBL ID610001
SCHEMBL ID1240173
MeSH IDM0147408

Synonyms (15)

Synonym
binaltorphimine
CHEMBL610001
bni ligand
unii-94l0jas27s
105618-27-7
4,8:11,15-dimethano-20h-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-20-methyl-, (8r-(4bs*,8alpha,8abeta,10aalpha,11beta,14as*,19aalpha,20bbeta))-
94l0jas27s ,
SCHEMBL1240173
Q15634055
DTXSID90909634
7,12-bis(cyclopropylmethyl)-20-methyl-5,6,7,8,9,10,11,12,13,14,20,20b-dodecahydro-19ah-4,8:11,15-dimethanobis[1]benzofuro[2,3-a:3',2'-i]dipyrido[4,3-b:3',4'-h]carbazole-1,8a,10a,18-tetrol
4,8:11,15-dimethano-20h-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol, 7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-20-methyl-, (8r-(4bs*,8.alpha.,8a.beta.,10a.alpha.,11.beta.,14as*,19a.alpha.,2
nih-10588
(4bs,8r,8as,10as,11r,14as,19ar,20br)-7,12-bis(cyclopropylmethyl)-5,6,7,8,9,10,11,12,13,14,19a,20b-dodecahydro-20-methyl-4,8:11,15-dimethano-20h-bisbenzofuro(2,3-a:3',2'-i)dipyrido(4,3-b:3',4'-h)carbazole-1,8a,10a,18-tetrol
(1s,2s,7s,8s,12r,20r,24r,32r)-11,33-bis(cyclopropylmethyl)-22-methyl-19,25-dioxa-11,22,33-triazaundecacyclo[24.9.1.18,14.01,24.02,32.04,23.05,21.07,12.08,20.030,36.018,37]heptatriaconta-4(23),5(21),14(37),15,17,26,28,30(36)-octaene-2,7,17,27-tetrol
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.00560.00000.03891.1570AID148841; AID149465
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.01100.00000.01590.0430AID149465
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID148841Antagonistic activity for Opioid receptor kappa 1 of guinea pig ileal longitudinal muscle at 100 nM1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID147907Binding affinity against Opioid receptor mu 1 was measured in the guinea pig brain membranes using [3H]DAMGO as radioligand1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
AID149774Binding affinity against Opioid receptor delta 1 was measured in the guinea pig brain membranes using [3H]DADLE in the presence of 1 uM unlabeled DAMGO as radioligand1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
AID230649Ki ratio measured as the ke values of mu receptor/kappa receptor from guinea pig brain membranes.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
AID229497Ratio of IC50 DADLE and antagonist binding to delta opioid receptor1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID233096Ratio of antagonistic activity for mu and kappa receptors1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID149465Antagonistic activity for Opioid receptor mu 1 in guinea pig ileal longitudinal muscle at 100 nM1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID148134Binding affinity against Opioid receptor kappa 1 was measured in the guinea pig brain membranes using [3H]EK in the presence of 1 uM unlabeled DAMGO as radioligand1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
AID149244Antagonistic activity for Opioid receptor delta 1 in mouse vas deferens at 20 nM1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID233094Ratio of antagonistic activity for delta and kappa receptors1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID229499Ratio of IC50 ethylketazocine and antagonist binding to opioid receptor1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
AID230648Ki ratio measured as the ke values of Opioid receptor delta 1/Opioid receptor kappa 1 from guinea pig brain membranes.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.
AID229500Ratio of IC50 morphine and antagonist binding to opioid receptor1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (9.30)18.7374
1990's22 (51.16)18.2507
2000's7 (16.28)29.6817
2010's7 (16.28)24.3611
2020's3 (6.98)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.77

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index32.77 (24.57)
Research Supply Index3.83 (2.92)
Research Growth Index5.13 (4.65)
Search Engine Demand Index39.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.77)

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%
Other45 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]