Page last updated: 2024-12-11

brl 24682

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

Description

BRL 24682: RN given for (endo)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9797313
CHEMBL ID301039
SCHEMBL ID7292676
MeSH IDM0254482

Synonyms (13)

Synonym
PDSP2_001249
PDSP1_001265
CHEMBL301039
brl-24682
brl 24682
benzamide, 4-amino-5-chloro-2-methoxy-n-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)-, endo-
76272-78-1
cas_76272-78-1
4-amino-5-chloro-2-methoxy-n-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)benzamide
bdbm82519
SCHEMBL7292676
DTXSID20997625
4-amino-5-chloro-2-methoxy-n-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)benzene-1-carboximidic acid
[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)
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.02130.00020.484110.0000AID6133
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.02130.00020.502310.0000AID6133
[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)
5-hydroxytryptamine receptor 4Homo sapiens (human)EC50 (µMol)0.44010.00060.08791.1220AID6274; AID6275; AID6276
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
maintenance of gastrointestinal epithelium5-hydroxytryptamine receptor 4Homo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 4Homo sapiens (human)
mucus secretion5-hydroxytryptamine receptor 4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
large intestinal transit5-hydroxytryptamine receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 4Homo sapiens (human)
serotonin receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 4Homo sapiens (human)
endosome5-hydroxytryptamine receptor 4Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
synapse5-hydroxytryptamine receptor 4Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID61445-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum; Not tested1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
AID6133Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
AID6174Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
AID6274Tested for 5-hydroxytryptamine 4 binding affinity against cisapride2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
5-HT4 receptor ligands: applications and new prospects.
AID6256Antagonistic activity by ability to block serotonin induced relaxation (mediated by activation of 5-hydroxytryptamine 4 receptor) in carbamylcholine (10e-6 M) contracted esophagus at a concentration of 10e-6 M.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives.
AID6275Tested for 5-hydroxytryptamine 4 binding affinity against renzapride2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
5-HT4 receptor ligands: applications and new prospects.
AID64938Affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
AID6276Tested for 5-hydroxytryptamine 4 binding affinity against zacopride2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
5-HT4 receptor ligands: applications and new prospects.
AID6239Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
AID61565-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum; Not tested1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
AID6085Antagonistic activity against 5-hydroxytryptamine 3 receptor as inhibition of 5-HT-induced bradycardia (von Bezold-jarisch reflex) in anesthetized rat1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Benzotriazinones as "virtual ring" mimics of o-methoxybenzamides: novel and potent 5-HT3 receptor antagonists.
AID6255Antagonistic activity evaluated by ability to block serotonin induced relaxation (mediated by activation of 5-hydroxytryptamine 4 receptor) in carbamylcholine (10e-6 M) contracted esophagus at a concentration of 10e-5 M.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives.
[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's4 (66.67)18.2507
2000's2 (33.33)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: 12.31

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 Index12.31 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]