Page last updated: 2024-12-05

edrophonium

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

Description

Edrophonium is a short-acting cholinesterase inhibitor that is used for the diagnosis and treatment of myasthenia gravis. It was synthesized in 1948 and was the first short-acting cholinesterase inhibitor to be used clinically. Edrophonium works by inhibiting the enzyme acetylcholinesterase, which breaks down acetylcholine. This leads to an increase in acetylcholine levels at the neuromuscular junction, which can improve muscle strength in patients with myasthenia gravis. Edrophonium can also be used to distinguish between myasthenia gravis and other disorders that cause muscle weakness. The drug is administered intravenously or intramuscularly. It is a relatively safe drug, but it can cause side effects such as bradycardia, hypotension, and bronchospasm. Edrophonium is important because it is a valuable tool for the diagnosis and treatment of myasthenia gravis. It is also studied to better understand the role of acetylcholine in neuromuscular transmission and to develop new treatments for myasthenia gravis and other disorders. '

Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
CuraregenusPlant extracts from several species, including genera STRYCHNOS and Chondodendron, which contain TETRAHYDROISOQUINOLINES that produce PARALYSIS of skeletal muscle. These extracts are toxic and must be used with the administration of artificial respiration.[MeSH]LoganiaceaeA plant family of the order Gentianales, subclass Asteridae, class Magnoliopsida. They have leaflike appendages at the base of the leafstalks, have terminal flower clusters. Petals have four or five overlapping lobes and the fruit is a capsule containing winged or wingless seeds.[MeSH]

Cross-References

ID SourceID
PubMed CID3202
CHEMBL ID1104
CHEBI ID251408
SCHEMBL ID34790
MeSH IDM0007057

Synonyms (72)

Synonym
edrofonio cloruro [dcit]
CHEMBL1104
KBIO1_000809
DIVK1C_000809
SPECTRUM_000442
NCGC00015409-01
lopac-e-3256
cas-116-38-1
NCGC00015409-02
SPECTRUM5_001531
IDI1_000809
BSPBIO_002386
BSPBIO_000006
LOPAC0_000511
AB00053796
312-48-1
C06976
edrophonium
edrophonium ion
n-ethyl-3-hydroxy-n,n-dimethylbenzenaminium
(3-hydroxyphenyl)dimethylethylammonium
n-ethyl-3-hydroxy-n,n-dimethylanilinium
edrophonium cation
DB01010
ethyl-(3-hydroxy-phenyl)-dimethyl-ammonium
3-hydroxy-n,n-dimethyl-n-ethylanilinium
PRESTWICK2_000083
PRESTWICK3_000083
tensilon
edrophonum
benzenaminium, n-ethyl-3-hydroxy-n,n-dimethyl-
enlon-plus
KBIOSS_000922
KBIOGR_001032
KBIO2_000922
KBIO2_003490
KBIO2_006058
SPBIO_001945
PRESTWICK1_000083
SPECTRUM2_001110
NINDS_000809
SPECTRUM4_000736
SPBIO_001220
PRESTWICK0_000083
BPBIO1_000008
NCGC00015409-03
NCGC00023975-03
CHEBI:251408 ,
NCGC00015409-07
edrophone chloride
ethyl-(3-hydroxyphenyl)-dimethylazanium
CCG-204602
NCGC00015409-05
NCGC00015409-06
NCGC00015409-04
NCGC00015409-08
unii-70fp3jly7n
70fp3jly7n ,
ethyl(m-hydroxyphenyl)dimethylammonium
edrophonium [who-dd]
edrophonium [vandf]
SCHEMBL34790
VWLHWLSRQJQWRG-UHFFFAOYSA-O
DTXSID4046943
edrophonium chloride, 3
cid_8307
bdbm120262
AB00053796_15
gtpl9073
Q3177745
NCGC00015409-15
ammonium, ethyl(m-hydroxyphenyl)dimethyl-(8ci)

Research Excerpts

Overview

Edrophonium is a widely used provocative agent in the evaluation of noncardiac chest pain. It has reported positivity rates of 30-55%.

ExcerptReferenceRelevance
"Edrophonium is a widely used provocative agent in the evaluation of noncardiac chest pain, with reported positivity rates of 30-55%. "( Interaction between patient and test administrator may influence the results of edrophonium provocative testing in patients with noncardiac chest pain.
Achkar, E; Falk, GW; Fleshler, B; Revta, R; Rose, S, 1993
)
1.96
"Edrophonium continues to be a relatively sensitive test for noncardiac chest pain."( Comparison of hypertonic glucose to other provocative tests in patients with noncardiac chest pain.
Hendrix, EA; Nasrallah, SM, 1987
)
0.99

Effects

ExcerptReferenceRelevance
"Edrophonium (EDR) has the advantages of a quick onset of action and reduced cholinergic effects compared to neostigmine (NST) when they are used to antagonize neuromuscular block (NMB). "( Edrophonium is better than neostigmine to antagonize residual vecuronium induced neuromuscular block.
Baer, GA; Puura, AI; Rorarius, MG, 1994
)
3.17

Actions

ExcerptReferenceRelevance
"Edrophonium may enhance (lower dose) or reduce (higher dose) cardiovascular autonomic drive in humans, as evidenced by the significant changes it evokes in HFP of the RRI (parasympathetic drive), and in the HFP and LFP of SBP (sympathetic drive)."( Effects of the anticholinesterase edrophonium on spectral analysis of heart rate and blood pressure variability in humans.
Backman, SB; Chartrand, D; Deschamps, A; Fiset, P; Novak, V; Plourde, G, 2002
)
1.32

Treatment

ExcerptReferenceRelevance
"Pretreatment with edrophonium (15-20 mg, i.v.) decreased, while atropine (2.4 mg, i.v.) increased by at least a factor of two, the dose of phenylephrine required to break ventricular tachycardia."( Termination of ventricular tachycardia by an increase in cardiac vagal drive.
Wald, RW; Waxman, MB, 1977
)
0.58

Toxicity

ExcerptReferenceRelevance
"To evaluate the safety of edrophonium chloride in the course of the Tensilon test by measurement of hemodynamic and ECG parameters and the observation of adverse events."( [Edrophonium chloride (Tensilon) test: a safe method in diagnosing myasthenia gravis].
Domanovits, H; Holzer, M; Laggner, AN; Mayr, N; Schillinger, M; Wenger, S; Zeitlhofer, J, 2000
)
1.52
" Blood pressure, heart rate, continuous ECG and adverse events were recorded 10 minutes following intravenous application of Tensilon."( [Edrophonium chloride (Tensilon) test: a safe method in diagnosing myasthenia gravis].
Domanovits, H; Holzer, M; Laggner, AN; Mayr, N; Schillinger, M; Wenger, S; Zeitlhofer, J, 2000
)
1.22
" Self-limiting adverse events of short duration were observed in 11 patients."( [Edrophonium chloride (Tensilon) test: a safe method in diagnosing myasthenia gravis].
Domanovits, H; Holzer, M; Laggner, AN; Mayr, N; Schillinger, M; Wenger, S; Zeitlhofer, J, 2000
)
1.22
"The Tensilon test appears to be a safe procedure."( [Edrophonium chloride (Tensilon) test: a safe method in diagnosing myasthenia gravis].
Domanovits, H; Holzer, M; Laggner, AN; Mayr, N; Schillinger, M; Wenger, S; Zeitlhofer, J, 2000
)
1.22
" Fourteen patients (64%) experienced daily cholinergic adverse effects, and muscarinic side effects correlated with AChE activity."( Electrophysiological signs and the prevalence of adverse effects of acetylcholinesterase inhibitors in patients with myasthenia gravis.
Punga, AR; Sawada, M; Stålberg, EV, 2008
)
0.35

Pharmacokinetics

No dose-dependency in pharmacokinetic behavior was observed within the range of 2-10 mumol/kg for edrophonium, 0. Except for a longer distribution half-life, the pharmacokinetics variables for edphonium did not differ significantly from those for neostigmine. Serum concentrations were assayed by high pressure liquid chromatography.

ExcerptReferenceRelevance
"min-1) and a prolonged elimination half-life (84."( Pharmacokinetics and pharmacodynamics of edrophonium in elderly surgical patients.
Diaz, J; Matteo, RS; Ornstein, E; Schwartz, AE; Silverberg, PA; Young, WL, 1990
)
0.54
" Only in the last few years, since the introduction of highly sensitive and selective analytical procedures based on gas and liquid chromatography, have proper pharmacokinetic studies of these drugs become possible."( Clinical pharmacokinetics of cholinesterase inhibitors.
Aquilonius, SM; Hartvig, P,
)
0.13
" Serum concentrations of edrophonium were assayed by high pressure liquid chromatography and pharmacokinetic variables computed using non-compartmental analysis."( Pharmacokinetics of edrophonium in anephric and renal transplant patients.
Cronnelly, R; Fahey, MR; Miller, RD; Morris, RB; Stanski, DR, 1981
)
0.89
" Except for a longer distribution half-life, the pharmacokinetic variables for edrophonium did not differ significantly from those for neostigmine."( Pharmacokinetics of edrophonium and neostigmine when antagonizing d-tubocurarine neuromuscular blockade in man.
Cronnelly, R; Fahey, MR; Miller, RD; Morris, RB; Stanski, DR, 1981
)
0.81
" A pharmacodynamic model was developed by considering acetylcholinesterase (AChE) inhibition, direct antagonism to the nicotinic receptor, and desensitization of the nicotinic receptor."( Pharmacodynamic analysis of contractile potentiation by cholinesterase inhibitors in rats.
Iga, T; Sawada, Y; Yamamoto, K, 1996
)
0.29
" A three-compartment pharmacokinetic model was justified."( Antagonism of rapacuronium using edrophonium or neostigmine: pharmacodynamics and pharmacokinetics.
Danjoux, G; Hing, JP; Hunter, JM; Mills, KG; Pollard, BJ; Scott, JM; Wright, PM, 1999
)
0.58

Compound-Compound Interactions

ExcerptReferenceRelevance
" The effect of a drug combination on retention was found to be dependent on the particular drugs in the combination, the ratio and the dose administered."( Two-drug combinations of memory enhancers: effect of dose ratio upon potency and therapeutic window, in mice.
Cherkin, A; Flood, JF; Smith, GE, 1988
)
0.27

Bioavailability

ExcerptReferenceRelevance
" The oral bioavailability of these hydrophilic ionised compounds is low: that of pyridostigmine is approximately 10% and the value for neostigmine is even lower."( Clinical pharmacokinetics of cholinesterase inhibitors.
Aquilonius, SM; Hartvig, P,
)
0.13

Dosage Studied

The inability of edrophonium to rapidly reverse a deep nondepolarizing neuromuscular block may be due to inadequate dosage or a ceiling effect. The dose-response and the doses required to prevent bradycardia in 50% and 95% of patients were determined for atropine.

ExcerptRelevanceReference
" The dose-response curve for acetylcholine after treatment of trypsin was similar to that in the presence of edrophonium."( Influences of trypsin and collagenase on acetylcholine responses of physically isolated single neurons of Aplysia californica.
Allen, CN; Carpenter, DO; Hori, N; Oyama, Y, 1990
)
0.49
"To determine the influence of enflurane on the ability of edrophonium to antagonize atracurium block, dose-response curves were constructed for edrophonium in the presence of 0%, 1% and 2% enflurane, and for 2% enflurane discontinued at the time of administration of edrophonium."( Edrophonium antagonism of atracurium during enflurane anaesthesia.
Bevan, DR; Donati, F; Gill, SS, 1990
)
1.97
"To determine the potencies of edrophonium and neostigmine as antagonists of nondepolarizing neuromuscular blockade produced by atracurium and vecuronium, dose-response curves were constructed for both antagonists when given at 10% spontaneous recovery of first twitch height."( Dose-response relationships for edrophonium and neostigmine as antagonists of atracurium and vecuronium neuromuscular blockade.
Bevan, DR; Donati, F; Smith, CE, 1989
)
0.85
" Our study revealed that both drugs have a strong effect on presynaptic sites and that these stimulating effects of edrophonium and neostigmine were about the same degree if 10 times as high a dosage as that of the former is used."( [The effect of neostigmine and edrophonium on the MEPP frequency].
Amaki, Y; Kaneko, M; Kobayashi, K, 1989
)
0.77
"To measure the ability of neostigmine and edrophonium to reverse moderate and profound atracurium blockade, dose-response relationships were established for these reversal agents given at 1% and 10% twitch height recovery."( Dose-response relationships for edrophonium and neostigmine as antagonists of moderate and profound atracurium blockade.
Bevan, DR; Donati, F; Smith, CE, 1989
)
0.82
" Both drugs reduced blood pressure without change in heart rate after acute dosing and after seven days."( Acute and chronic effects of the converting enzyme inhibitors enalapril and lisinopril on reflex control of heart rate in normotensive man.
Ajayi, AA; Campbell, BC; Howie, CA; Reid, JL, 1985
)
0.27
"The dose-response and the doses required to prevent bradycardia in 50% (ED50) and 95% (ED95) of patients were determined for atropine after antagonism of pancuronium-induced neuromuscular blockade in 72 patients with edrophonium-atropine mixtures."( Atropine-edrophonium mixture: a dose-response study.
Absood, GH; Gomaa, M; Naguib, M, 1988
)
0.88
" Some combinations of cholinergic drugs enhance retention even though the total drug dosage is reduced by as much as 97% compared to the dose needed to improve retention when the same drugs are administered singly."( Two-drug combinations of memory enhancers: effect of dose ratio upon potency and therapeutic window, in mice.
Cherkin, A; Flood, JF; Smith, GE, 1988
)
0.27
"To determine the potencies of neostigmine, pyridostigmine, and edrophonium in reversing pancuronium and d-tubocurarine blockade, dose-response curves were established for first twitch height recovery and train-of-four ratio."( Dose-response curves for edrophonium, neostigmine, and pyridostigmine after pancuronium and d-tubocurarine.
Antzaka, C; Bevan, DR; Donati, F; McCarroll, SM; McCready, D, 1987
)
0.82
" Concentrations of anticholinesterases spanned the clinical range and were extended beyond to establish dose-response curves."( Incomplete reversal of pancuronium neuromuscular blockade by neostigmine, pyridostigmine, and edrophonium.
Bartkowski, RR, 1987
)
0.49
" Dose-response relationships were established from the measurement of first twitch height (T1) ten minutes later."( Neostigmine, pyridostigmine and edrophonium as antagonists of deep pancuronium blockade.
Bevan, DR; Donati, F; Lahoud, J; McCready, D, 1987
)
0.56
" A dose-response curve was determined for each of four drugs (arecoline, edrophonium, oxotremorine, tacrine) and for each of the six possible two-drug combinations."( Memory enhancement: supra-additive effect of subcutaneous cholinergic drug combinations in mice.
Cherkin, A; Flood, JF; Smith, GE, 1985
)
0.5
" Accordingly, the dose-response relationship, onset and duration of action (n = 60), and pharmacokinetics (n = 22) of neostigmine, pyridostigmine, their metabolites 3-hydroxyphenyltrimethylammonium (PTMA) and 3-hydroxy-N-methylpyridinium (MP), and edrophonium were determined in dogs anesthetized with sodium pentobarbital."( Metabolites of neostigmine and pyridostigmine do not contribute to antagonism of neuromuscular blockade in the dog.
Cronnelly, R; Fisher, DM; Hennis, PJ; Miller, RD; Sharma, M, 1984
)
0.45
"The dose-response relationship, onset, duration of action, atropine requirement, and pharmacokinetic variables of edrophonium were determined in infants and children during N2O-halothane anesthesia."( Clinical pharmacology of edrophonium in infants and children.
Cronnelly, R; Fisher, DM; Miller, RD; Sharma, M, 1984
)
0.78
"125 mg/kg, however, the dose-response curve was not parallel to those for neostigmine or pyridostigmine."( Edrophonium: duration of action and atropine requirement in humans during halothane anesthesia.
Cronnelly, R; Miller, RD; Morris, RB, 1982
)
1.71
"The dose-response relationship for edrophonium during antagonism of vecuronium-induced neuromuscular blockade was studied in two groups of adult patients of mean (SD) age 35 (10."( Dose-responses for edrophonium during antagonism of vecuronium block in young and older adult patients.
Maddineni, VR; McCarthy, GJ; McCoy, EP; Mirakhur, RK, 1995
)
0.9
"The inability of edrophonium to rapidly reverse a deep nondepolarizing neuromuscular block may be due to inadequate dosage or a ceiling effect to antagonism of neuromuscular block by edrophonium."( The maximum depth of an atracurium neuromuscular block antagonized by edrophonium to effect adequate recovery.
Beemer, GH; Bjorksten, AR; Goonetilleke, PH, 1995
)
0.86
" Cumulative dose-response curves were constructed using the logit transformation of the neuromuscular effect versus the logarithm of the cumulative dose of edrophonium."( The maximum depth of an atracurium neuromuscular block antagonized by edrophonium to effect adequate recovery.
Beemer, GH; Bjorksten, AR; Goonetilleke, PH, 1995
)
0.72
" The dose-response relationships for neostigmine and edrophonium were studied during antagonism of neuromuscular block induced by rocuronium bromide."( Dose-response relationships for edrophonium and neostigmine antagonism of rocuronium bromide (ORG 9426)-induced neuromuscular blockade.
Abdulatif, M; al-Ghamdi, A; Naguib, M, 1993
)
0.82
"The dose-response curves for neostigmine- and edrophonium-assisted antagonism of rocuronium bromide neuromuscular blockade for the single twitch and TOF ratio were not parallel."( Dose-response relationships for edrophonium and neostigmine antagonism of rocuronium bromide (ORG 9426)-induced neuromuscular blockade.
Abdulatif, M; al-Ghamdi, A; Naguib, M, 1993
)
0.83
"We have studied the dose-response relationships for neostigmine and edrophonium during antagonism of neuromuscular block induced by mivacurium chloride."( Dose-response relationships for edrophonium and neostigmine antagonism of mivacurium-induced neuromuscular block.
Abdulatif, M; al-Ghamdi, A; Hamo, I; Naguib, M; Nouheid, R, 1993
)
0.8
"We have studied the dose-response relationships for neostigmine and edrophonium during antagonism of neuromuscular block induced by pipecuronium bromide."( Dose-response relationships for edrophonium and neostigmine antagonism of pipecuronium-induced neuromuscular block.
Abdulatif, M; Naguib, M, 1994
)
0.81
"The purpose of this study was to determine the dose-response relationships for edrophonium antagonism of mivacurium-induced neuromuscular block."( [Effects of different doses of edrophonium antagonism of mivacurium-induced neuromuscular block in the presence of nitrous oxide, propofol, and alfentanil anesthesia].
Drolet, P; Girard, M; Perreault, L; Ripart, J, 1996
)
0.81
"The purpose of this study was to determine the dose-response relationships for edrophonium antagonism of mivacurium-induced neuromuscular block."( Dose-response relationships for edrophonium antagonism of mivacurium-induced neuromuscular block during N2O-enflurane-alfentanil anaesthesia.
Drolet, P; Girard, M; Marcotte, J; Perreault, L, 1995
)
0.8
"A dose-response relationship study for edrophonium to examine the modification of volatile anaesthetics on reversal of vecuronium block."( Sevoflurane and isoflurane impair edrophonium reversal of vecuronium-induced neuromuscular block.
Fujita, T; Kurosaki, D; Morita, T; Saito, S; Sato, H; Sugaya, T; Tsukagoshi, H, 1996
)
0.84
" administration decreased at high doses of each drug and the dose-response curves were biphasic."( Pharmacodynamic analysis of contractile potentiation by cholinesterase inhibitors in rats.
Iga, T; Sawada, Y; Yamamoto, K, 1996
)
0.29
"To study the dose-response relationships for neostigmine and edrophonium during antagonism of neuromuscular block induced by atracurium and cisatracurium."( Dose-response relationships for edrophonium and neostigmine antagonism of atracurium and cisatracurium-induced neuromuscular block.
Naguib, M; Riad, W, 2000
)
0.83
" Unless contraindicated, patients with diplopia were recommended for therapy with prednisone, up to 40 to 60 mg/d, with the dosage tapered for 5 to 6 weeks."( Development of generalized disease at 2 years in patients with ocular myasthenia gravis.
Homel, P; Kupersmith, MJ; Latkany, R, 2003
)
0.32
" The type of inhibition (competitive, uncompetitive, or mixed), the dissociation constants for the inhibitors, and the inhibitor dose-response curves were also determined."( Automated method, based on micro-sequential injection, for the study of enzyme kinetics and inhibition.
Carroll, AD; Chen, Y; Ruzicka, J; Scampavia, L, 2006
)
0.33
" BW284c51 blockade was non-competitive and voltage-dependent, although it also affected the n(H) of the dose-response curve."( Diverse inhibitory actions of quaternary ammonium cholinesterase inhibitors on Torpedo nicotinic ACh receptors transplanted to Xenopus oocytes.
Ivorra, I; Morales, A; Olivera-Bravo, S, 2007
)
0.34
" Detailed pharmacologic dose-response curves of selected inhibitors were also measured in high-throughput fashion to validate the method."( Rapid and label-free screening of enzyme inhibitors using segmented flow electrospray ionization mass spectrometry.
Kennedy, RT; Li, Q; Pei, J, 2010
)
0.36
" In the presence of higher lidocaine doses, nicotinic receptors were blocked both at positive and negative potentials, acetylcholine dose-response curve shifted to the right and lidocaine pre-application, before its co-application with acetylcholine, enhanced the current inhibition, indicating all together that lidocaine also blocked resting receptors; besides, it increased the current decay rate."( Multiple inhibitory actions of lidocaine on Torpedo nicotinic acetylcholine receptors transplanted to Xenopus oocytes.
Alberola-Die, A; González-Ros, JM; Ivorra, I; Martinez-Pinna, J; Morales, A, 2011
)
0.37
" The PSL dosage was tapered without any worsening of clinical signs."( [Immune checkpoint inhibitor-induced anti-striational antibodies in myasthenia gravis and myositis: a case report].
Esa, Y; Kobayashi, J; Sugiyama, Y; Suzuki, S; Takahashi, D; Watanabe, A, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
EC 3.1.1.8 (cholinesterase) inhibitorAn EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of cholinesterase (EC 3.1.1.8).
diagnostic agentA substance administered to aid diagnosis of a disease.
antidoteAny protective agent counteracting or neutralizing the action of poisons.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
quaternary ammonium ionA derivative of ammonium, NH4(+), in which all four of the hydrogens bonded to nitrogen have been replaced with univalent (usually organyl) groups.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency2.31090.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency4.74440.100020.879379.4328AID488773; AID588453
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926; AID938
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.68580.035520.977089.1251AID504332
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency22.98330.00106.000935.4813AID943; AID944
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
CholinesteraseHomo sapiens (human)Ki99.50500.00001.51739.7300AID1799827
AcetylcholinesteraseMus musculus (house mouse)Ki0.25000.00001.42829.3000AID1800423
AcetylcholinesteraseHomo sapiens (human)Ki66.42000.00001.27869.7300AID1799827; AID1800423
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
POU domain, class 2, transcription factor 1Homo sapiens (human)Km26.40002.10005.39008.6000AID1769498
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
negative regulation of DNA-templated transcriptionPOU domain, class 2, transcription factor 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionPOU domain, class 2, transcription factor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIPOU domain, class 2, transcription factor 1Homo sapiens (human)
positive regulation of miRNA transcriptionPOU domain, class 2, transcription factor 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIPOU domain, class 2, transcription factor 1Homo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPOU domain, class 2, transcription factor 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingPOU domain, class 2, transcription factor 1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPOU domain, class 2, transcription factor 1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPOU domain, class 2, transcription factor 1Homo sapiens (human)
DNA bindingPOU domain, class 2, transcription factor 1Homo sapiens (human)
protein bindingPOU domain, class 2, transcription factor 1Homo sapiens (human)
sequence-specific DNA bindingPOU domain, class 2, transcription factor 1Homo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
nucleusPOU domain, class 2, transcription factor 1Homo sapiens (human)
nucleoplasmPOU domain, class 2, transcription factor 1Homo sapiens (human)
endoplasmic reticulumPOU domain, class 2, transcription factor 1Homo sapiens (human)
intracellular membrane-bounded organellePOU domain, class 2, transcription factor 1Homo sapiens (human)
chromatinPOU domain, class 2, transcription factor 1Homo sapiens (human)
RNA polymerase II transcription regulator complexPOU domain, class 2, transcription factor 1Homo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
AID1769499Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Vmax incubated for 2 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1769501Ratio of drug uptake in human OCT1 expressing HEK293 cells at 2.5 uM to drug uptake in empty vector transfected human HEK293 cells at 2.5 uM2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1769500Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring intrinsic clearance incubated for 2 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1769498Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Km incubated for 2 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5
Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1800423Assay of Substrate Hydrolysis from Article 10.1021/bi401043w: \\The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.\\2013Biochemistry, Oct-22, Volume: 52, Issue:42
The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.
AID1799827Inhibition Assay from Article 10.1021/bi300955k: \\Probing the peripheral site of human butyrylcholinesterase.\\2012Biochemistry, Sep-11, Volume: 51, Issue:36
Probing the peripheral site of human butyrylcholinesterase.
AID1345946Human acetylcholinesterase (Cartwright blood group) (Hydrolases)1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (938)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990573 (61.09)18.7374
1990's226 (24.09)18.2507
2000's87 (9.28)29.6817
2010's42 (4.48)24.3611
2020's10 (1.07)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 64.39

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index64.39 (24.57)
Research Supply Index7.00 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index111.55 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (64.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials112 (11.36%)5.53%
Reviews43 (4.36%)6.00%
Case Studies134 (13.59%)4.05%
Observational0 (0.00%)0.25%
Other697 (70.69%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Pathophysiology of Orthostatic Hypotension [NCT00748059]Phase 110 participants (Actual)Interventional1996-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]