Page last updated: 2024-11-04

n(8)-bromoacetyl-n(1)-3'-(4-indolyloxy)-2'-hydroxypropyl-1,8-diamino-4-menthane

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

Description

N(8)-bromoacetyl-N(1)-3'-(4-indolyloxy)-2'-hydroxypropyl-1,8-diamino-4-menthane: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1239
CHEMBL ID157881
MeSH IDM0160433

Synonyms (21)

Synonym
EU-0100977
LOPAC0_000977
n8-bromoacetyl-n1-3'-(4-indolyloxy)-2'-hydroxy-propyl-[z]-1,8-diamino-p-methane
( inverted question mark)-pindobind
P-119
(+/-)-pindobind
CHEMBL157881 ,
106469-51-6
2-bromo-n-[2-[4-[[2-hydroxy-3-(1h-indol-4-yloxy)propyl]amino]-4-methylcyclohexyl]propan-2-yl]acetamide
CCG-205057
n(8)-bromoacetyl-n(1)-3'-(4-indolyloxy)-2'-hydroxypropyl-1,8-diamino-4-menthane
acetamide, 2-bromo-n-(1-(4-((2-hydroxy-3-(1h-indol-4-yloxy)propyl)amino)-4-methylcyclohexyl)-1-methylethyl)-
n8-bim
SR-01000075283-1
sr-01000075283
acetamide,2-bromo-n-[1-[4-[[2-hydroxy-3-(1h-indol-4-yloxy)propyl]amino]-4-methylcyclohexyl]-1-methylethyl]-
bdbm50226717
2-bromo-n-{2-[4-({2-hydroxy-3-[(1h-indol-4-yl)oxy]propyl}amino)-4-methylcyclohexyl]propan-2-yl}ethanimidic acid
DTXSID20910011
n-(2-(4-((3-((1h-indol-4-yl)oxy)-2-hydroxypropyl)amino)-4-methylcyclohexyl)propan-2-yl)-2-bromoacetamide
(+/-)pindobind

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"1 microM), followed by washout, produced concentration-dependent rightward shifts of the dose-response curve to cumulative additions of (-)-isoprenaline and oxymethylene-isoprenaline and reductions in the maximal response."( Persistent beta-adrenoceptor blockade with alkylating pindolol (BIM) in guinea-pig left atria and trachea.
Molenaar, P; Pitha, J; Russell, F; Summers, R, 1988
)
0.27
[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)
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki0.00090.00050.35461.6000AID41632; AID41633
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki0.00090.00000.667310.0000AID41632; AID41633
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki0.00090.00050.33671.6000AID41632; AID41633
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Kd0.00190.00140.06510.3910AID41615; AID41619
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Kd0.00190.00140.06010.3910AID41615; AID41619
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Kd0.00190.00140.06510.3910AID41615; AID41619
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID41632Binding affinity against beta adrenergic receptor from rat heart tissues was determined1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41775Percent potency for irreversible blockade of the [3H]dihydroalprenolol binding to beta adrenergic receptor of rat heart reticulocyte pretreated with alkylating beta blockers at concentration of 1 x 10e-7 M1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41633Binding affinity against beta adrenergic receptor from rat lung tissues was determined1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41470Concentration of binding sites of protein for [3H]dihydroalprenolol binding to o beta adrenergic receptor of rat lung reticulocytes was determined in the presence of (-)-isoproterenol (1*10e-5 M)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID41877Percent potency for irreversible blockade of the [3H]dihydroalprenolol binding to beta adrenergic receptor of rat lung reticulocyte pretreated with alkylating beta-blockers1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41619Binding affinity against the [3H]dihydroalprenolol binding to membrane preparation from rat lung reticulocyte pretreated with alkylating beta-blockers1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41879Percent potency for irreversible blockade of the [3H]dihydroalprenolol binding to o beta adrenergic receptor of rat heart reticulocyte1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41469Concentration of binding sites of protein for [3H]dihydroalprenolol binding to membrane preparations from rat heart reticulocyte in the presence of (-)-isoproterenol (1*10e-5 M)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41464Concentration of binding sites of protein for [3H]dihydroalprenolol binding to beta adrenergic receptor of rat lung reticulocyte1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41459Concentration of binding sites of protein for [3H]dihydroalprenolol binding to beta adrenergic receptor of rat heart reticulocyte1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID41615Binding affinity against the [3H]dihydroalprenolol binding to beta adrenergic receptor of rat heart reticulocytes1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (50.00)18.7374
1990's2 (25.00)18.2507
2000's1 (12.50)29.6817
2010's1 (12.50)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: 12.13

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 Index12.13 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.13)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]