Page last updated: 2024-12-07

acetylcholine mustard

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

Description

acetylcholine mustard: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID93191
CHEMBL ID3290088
MeSH IDM0043214

Synonyms (17)

Synonym
methylamine, n-acetoxyethyl-n-chloroethyl-
2-chloroethylmethylaminoethyl acetate
2-((2-chloroethyl)methylamino)ethanol acetate
ethanol, 2-((2-chloroethyl)methylamino)-, acetate
brn 1759495
tl 1428
methyl-beta-acetoxyethyl-beta-chloroethylamine
methyl-2-acetoxyethyl-2'-chloroethylamine
diethylamine, 2-acetoxy-2'-chloro-n-methyl-
ethanol, 2-((2-chloroethyl)methylamino)-, acetate (ester)
acetylcholine mustard
36375-30-1
2-[2-chloroethyl(methyl)amino]ethyl acetate
3-04-00-00669 (beilstein handbook reference)
CHEMBL3290088
DTXSID20189902
methyl-2-acetoxyethyl-2-chloroethylamine

Research Excerpts

Overview

Acetylcholine mustard (AChM) is an analogue of acetyl choline (A Ch) in which the onium headgroup is replaced by a chemically reactive aziridinium moiety.

ExcerptReferenceRelevance
"Acetylcholine mustard (AChM) is an analogue of acetylcholine (ACh) in which the onium headgroup is replaced by a chemically reactive aziridinium moiety. "( Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors.
Birdsall, NJ; Curtis, CA; Hulme, EC; Spalding, TA, 1994
)
3.17

Dosage Studied

ExcerptRelevanceReference
" However, the dose-response for Aech-M was biphasic such that at high concentrations (greater than 50 microM) there was a reduction in its ability to attenuate cAMP formation."( Effect of acetylethylcholine mustard on muscarinic receptor-coupled attenuation of cAMP formation in intact GH3 cells.
Baker, SP; Bolden, CP, 1990
)
0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID1154130Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 10 mins prior to [3H]NMS addition measured after 4 hrs by whole cell radioligand displacement analysis (Rvb = 99.87%)2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1154129Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 5 mins prior to [3H]NMS addition measured after 4 hrs by whole cell radioligand displacement analysis (Rvb = 99.87%)2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1154131Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 15 mins prior to [3H]NMS addition measured after 4 hrs by whole cell radioligand displacement analysis (Rvb = 99.87%)2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1154133Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 30 mins prior to [3H]NMS addition measured after 4 hrs by whole cell radioligand displacement analysis relative to vehicle-treated control2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1154132Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 20 mins prior to [3H]NMS addition measured after 4 hrs by whole cell radioligand displacement analysis (Rvb = 99.87%)2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (36.36)18.7374
1990's3 (27.27)18.2507
2000's1 (9.09)29.6817
2010's3 (27.27)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: 11.78

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 Index11.78 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.78)

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]