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physostigmine

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Description

Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5983
CHEMBL ID94
CHEBI ID27953
SCHEMBL ID24044
MeSH IDM0016815

Synonyms (172)

Synonym
AC-15983
fysostigmin
BRD-K25650355-001-02-5
BRD-K25650355-059-02-3
wln: t b556 en gntt&j b1 e1 g1 kovm1
ezerin
antilirium
eserolein, methylcarbamate (ester)
pyrrolo[2, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3as-cis)-
physostol
NSC30782 ,
nsc-30782
erserine
carbamic acid, ester with eseroline
esromiotin
KBIO1_001421
DIVK1C_006477
SDCCGMLS-0066585.P001
(3as,8ar)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl methylcarbamate
EU-0100483
physostigmine (usp)
D00196
eserine (tn)
SPECTRUM_001789
SPECTRUM4_001631
SPECTRUM_000916
SPECTRUM4_001913
PRESTWICK3_000566
PRESTWICK2_000566
MEGXP0_001872
BSPBIO_000352
BPBIO1_000388
LOPAC0_000483
SPECTRUM5_000441
ACON1_000097
SPECTRUM5_000626
carbamic acid, methyl-, ester with eseroline
methyl-carbamic acid, ester with eseroline
einecs 200-332-8
1,2,3,3abeta,8abeta-hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)-indol-5-yl methylcarbamate
fysostigmin [czech]
calabarine
ccris 3422
rcra waste no. p204
nih 10421
pyrrolo(2,3-b)indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3as-cis)
pyrrolo(2,3-b)indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3as-cis)-
mcv 4484
hsdb 3161
nsc 30782
(3as-cis)-1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)indol-5-ol methylcarbamate (ester)
cs 58525
pyrrolo(2,3-b)indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate (ester), (3as,8ar)-
eserine
physostigmine
C06535
57-47-6
DB00981
physostigmine.salicylic acid
(3as,8ar)-1,3a,8-trimethyl-1h,2h,3h,3ah,8h,8ah-pyrrolo[2,3-b]indol-5-yl n-methylcarbamate; 2-hydroxybenzoic acid
(-)-physostigmine
bdbm11023
cid_657348
NCGC00093889-03
NCGC00093889-04
KBIOGR_001433
KBIO2_002278
KBIOGR_002533
KBIOSS_002279
KBIO3_001689
KBIO2_001396
KBIOGR_002061
KBIO2_006532
KBIO2_003964
KBIO3_001842
KBIO2_004846
KBIOSS_001396
KBIO2_007414
SPBIO_000774
SPBIO_000339
SPECTRUM2_001283
SPECPLUS_000381
SPECTRUM2_000330
SPBIO_002571
SPECTRUM3_000901
PRESTWICK1_000566
SPECTRUM4_000997
SPECTRUM2_000757
SPECTRUM3_000545
SPBIO_001285
PRESTWICK0_000566
SPECTRUM1500753
SPECTRUM5_001672
BSPBIO_002189
NCGC00093889-06
NCGC00093889-01
NCGC00093889-05
NCGC00093889-02
smr000718753
MLS001304022
CHEBI:27953 ,
E 8375
HMS2089M11
NCGC00093889-08
cogmine
eserinum
eserin
mcv-4484
CHEMBL94 ,
(3as,8ar)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl methylcarbamate hydrochloride
bdbm50222010
P0406
HMS1921G06
bdbm50004000
NCGC00093889-07
NCGC00093889-09
NCGC00093889-10
HMS3261B07
NCGC00255345-01
dtxsid3023471 ,
tox21_301591
dtxcid603471
cas-57-47-6
tox21_111228
HMS2236L08
CCG-38605
eserolein, methylcarbamate
physostigmine [usp:ban]
pyrrolo(2,3-b)indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, 5-(n-methylcarbamate), (3as,8ar)-
unii-9u1vm840sp
9u1vm840sp ,
LP00483
eserinum [hpus]
physostigmine [mi]
physostigmine [who-dd]
physostigmine [vandf]
1,2,3,3a.beta.,8a.beta.-hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)-indol-5-yl methylcarbamate
physostigmine [hsdb]
physostigmine [mart.]
physostigmine [usp impurity]
gtpl6598
SCHEMBL24044
tox21_111228_1
NCGC00093889-12
tox21_500483
NCGC00261168-01
PIJVFDBKTWXHHD-HIFRSBDPSA-N
(-) physostigmine
(3as,8ar)-1,3a,8-trimethyl-1h,2h,3h,3ah,8h,8ah-pyrrolo[2,3-b]indol-5-yl n-methylcarbamate
eserine, >=98.0% (n)
SR-01000075341-1
SBI-0050467.P004
NCGC00093889-13
eserine; antilirium; physostol; esromiotin; ezerin
BCP19735
Q410595
BRD-K25650355-059-12-2
SDCCGSBI-0050467.P005
CS-0034353
NCGC00093889-20
physostigmin
AKOS016843649
HY-N6608
physostigmine 100 microg/ml in acetonitrile
EN300-23839407
physostigmine (mart.)
(3as,8ar)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo(2,3-b)indol-5-yl methylcarbamate
eserolein, methylcarbamate(ester)
physostigmine (usp impurity)
physostigmine (usp:ban)
pyrrolo(2,3-b)indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, methylcarbamate(ester),(3as-cis)-
(-)-eserine

Research Excerpts

Overview

Physostigmine is a parasympathomimetic drug used to treat a variety of neurological disorders. It can activate, potentiate, and inhibit acetylcholine receptors, including neuronal nicotinic receptors.

ExcerptReferenceRelevance
"Physostigmine functions as a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier."( Oral and Transdermal Rivastigmine for the Treatment of Anticholinergic Delirium: A Case Report.
Fratta, KA; Ginder, M; Haggerty, DA, 2023
)
1.63
"Physostigmine is a tertiary amine carbamate acetylcholinesterase inhibitor. "( Adverse Effects of Physostigmine.
Arens, AM; Kearney, T, 2019
)
2.29
"Physostigmine is a parasympathomimetic drug used to treat a variety of neurological disorders, including Alzheimer's disease and glaucoma. "( Unusual acetylation-dependent reaction cascade in the biosynthesis of the pyrroloindole drug physostigmine.
Ad, O; Liu, J; Ng, T; Rui, Z; Zhang, W, 2014
)
2.06
"Physostigmine is a well known inhibitor of acetylcholinesterase, which can also activate, potentiate, and inhibit acetylcholine receptors, including neuronal nicotinic receptors comprising α4 and β2 subunits. "( The E Loop of the Transmitter Binding Site Is a Key Determinant of the Modulatory Effects of Physostigmine on Neuronal Nicotinic α4β2 Receptors.
Akk, G; Germann, AL; Jin, X; McCollum, MM; Steinbach, JH, 2017
)
2.12
"Physostigmine is a carbamate inhibitor of acetylcholinesterase that is reported to attenuate the sedative effects of a number of drugs, including gamma-hydroxybutyrate."( Physostigmine as a treatment for gamma-hydroxybutyrate toxicity: a review.
Hoffman, RS; Nelson, LS; Traub, SJ, 2002
)
2.48
"Physostigmine is an anti-cholinesterase used for the pretreatment of a poisoning caused by highly toxic organophosphorus neurotoxins. "( Design of physostigmine-loaded polymeric microparticles for pretreatment against exposure to organophosphate agents.
Chaw, CS; Moochhala, S; Tan, CW; Wang, L; Yang, YY, 2003
)
2.16
"Physostigmine is a cholinesterase inhibitor, which crosses the blood-brain barrier and elevates brain acetylcholine level."( Continuous physostigmine combined with morphine-based patient-controlled analgesia in the postoperative period.
Beilin, B; Bessler, H; Papismedov, L; Shavit, Y; Weinstock, M, 2005
)
1.44
"Physostigmine is an acetylcholinesterase inhibitor and can produce fasciculations, seizures, bradycardia, and asystole. "( Physostigmine does not effect arousal but produces toxicity in an animal model of severe gamma-hydroxybutyrate intoxication.
Bania, TC; Chu, J, 2005
)
3.21
"Physostigmine is a safe alternative to nefopam, significantly reducing the incidence and severity of postanaesthetic shivering without affecting postanaesthetic recovery."( Physostigmine for the prevention of postanaesthetic shivering following general anaesthesia - a placebo-controlled comparison with nefopam.
Boldt, J; Piper, SN; Riechmann, J; Röhm, KD; Schuler, S; Suttner, SW, 2005
)
2.49
"Physostigmine is a commonly used therapy for the anticholinergic manifestations of tricyclic antidepressant (TCA) overdose. "( Asystole complicating physostigmine treatment of tricyclic antidepressant overdose.
Pentel, P; Peterson, CD, 1980
)
2.02
"Physostigmine is an antidote in cases of overdosage with intravenous anaesthetics such as dehydrobenzperidol, benzodiazepines and ketamine. "( [On the use of physostigmine in anesthesia and intensive care].
Abel, M; George, G; Kiss, I, 1982
)
2.06
"(-)Physostigmine acts as a channel-activating ligand at low concentrations and as a direct channel blocker at elevated concentrations."( Biochemical characterization of a novel channel-activating site on nicotinic acetylcholine receptors.
Albuquerque, EX; Coban, T; Kuhlmann, J; Maelicke, A; Okonjo, KO; Pereira, EF; Schrattenholz, A; Schröder, B, 1993
)
0.8
"Physostigmine is a less effective yawning-inducer in HY than in LY rats."( Two inbred rat sublines that differ in spontaneous yawning behavior also differ in their responses to cholinergic and dopaminergic drugs.
Eguíbar, JR; Holmgren, B; Santos, A; Urbá-Holmgren, R, 1993
)
1.01
"Physostigmine is an unspecific antagonist of the central anticholinergic syndrome, an acute psychosis that may be caused by numerous drugs used in anaesthesia."( [Antagonists in anesthesia].
Calaminus, JM; Lauven, PM, 1995
)
1.01
"Physostigmine is a cholinesterase inhibitor which enhances central and peripheral cholinergic activity. "( Oral physostigmine in Alzheimer's disease: effects on norepinephrine and vasopressin in cerebrospinal fluid and plasma.
Bodenheimer, S; Dorsa, DM; Pascualy, M; Peskind, ER; Raskind, MA; Thal, L; Veith, RC; Wingerson, D, 1995
)
2.25
"Physostigmine is a plant alkaloid of great interest as a therapeutic candidate for the treatment of Alzheimer's disease. "( Development of a defined medium fermentation process for physostigmine production by Streptomyces griseofuscus.
Brix, T; Buckland, B; Chartrain, M; Greasham, R; Marcin, C; Salmon, P; Shifflet, MA; Zhang, J, 1996
)
1.98
"Physostigmine is a tertiary carbamate that is utilised as a pretreatment against organophosphate intoxication. "( The electrostability and electrically assisted delivery of an organophosphate pretreatment (physostigmine) across human skin in vitro.
Chilcott, RP; Rowland, CA, 2000
)
1.97
"Physostigmine is an AChE inhibitor originally extracted from calabar beans."( Physostigmine for Alzheimer's disease.
Birks, J; Coelho, F, 2001
)
2.47
"Physostigmine appears to be a safe, rapidly effective agent for reversing the prolonged somnolence of this sedation regimen."( Physostigmine reversal of sedation in parturients.
Clark, RB; Hyde, ML; Sherman, RL; Smith, DB; Stephens, SR,
)
2.3
"Physostigmine is considered to be a potential pretreatment agent against organophosphate intoxication. "( Interactive effects of physostigmine and exercise on cholinesterase activity in red blood cells and tissues of rat.
Colliver, JA; Dube, SN; Somani, SM,
)
1.88
"Physostigmine (PHY) is an anticholinergic drug used in the treatment of neuromuscular disorders and organophosphate poisoning. "( Determination of physostigmine in plasma by high-performance liquid chromatography and fluorescence detection.
Elsayed, NM; Ferraris, S; Korte, DW; Ryabik, JR; Wheeler, CR, 1989
)
2.06
"Physostigmine is an approved antidote in the treatment of intoxication as well as in the management of overdoses of numerous medications--many of which are used in the course of pre-medication or anesthesia induction or maintenance. "( [Modification of vigilance in the postanesthetic phase using physostigmine].
Brosch, R; Schneck, HJ; Tempel, G; von Hundelshausen, B, 1985
)
1.95

Effects

Physostigmine salicylate has proved to be a very useful agent for use in the recovery room. It has been shown to be effective as a pretreatment against potent anticholinesterase poisons (e.g., soman) Yet it is short acting and causes undesirable side effects in mammals.

ExcerptReferenceRelevance
"Physostigmine has a half-life of 16, 23 and 30 min in rat, dog and man, respectively."( Physostigmine--an overview as pretreatment drug for organophosphate intoxication.
Dube, SN; Somani, SM, 1989
)
2.44
"Physostigmine has long been recognized as an antidote to reverse anticholinergic delirium. "( Safety and effectiveness of physostigmine: a 10-year retrospective review.
Al-Abri, S; Arens, AM; Kearney, T; Olson, KR; Shah, K, 2018
)
2.22
"The physostigmine regimen has excellent antidotal capacity, but the very narrow therapeutic window (< 10 min) makes it unsuitable for use in the field."( Determination of anti-convulsant and life-preserving capacities of three types of auto-injector therapies against soman intoxication in rats.
Aas, P; Enger, S; Myhrer, T, 2013
)
0.87
"Physostigmine has been proposed as an antidote for gamma hydroxybutyrate (GHB) intoxication, based on associated awakenings in 1) patients anesthetized with GHB and 2) five of six patients administered physostigmine for GHB intoxication. "( Physostigmine for gamma-hydroxybutyrate coma: inefficacy, adverse events, and review.
Litonjua, R; Smith, SW; Westfal, RE; Zvosec, DL, 2007
)
3.23
"Physostigmine has been reported to improve the memory function of some patients with Alzheimer's Disease (AD). "( Transdermal physostigmine in the treatment of Alzheimer's disease.
Brandeis, R; Dachir, S; Feiler, D; Glikfeld, P; Grunwald, J; Levy, A; Mawassi, F; Meshulam, Y; Treves, TA; Wengier, A, 1994
)
2.11
"Physostigmine has different effects on allodynia and nociception, which suggests that different cholinergic (muscarinic) mechanisms may be involved in neuropathic and nociceptive pain."( Systemic physostigmine shows antiallodynic effects in neuropathic rats.
Kalso, E; Kontinen, VK; Paananen, S; Pöyhiä, R; Xu, M, 1999
)
2.16
"Physostigmine has also been shown to reverse benzodiazepine sedation in anecdotal reports."( Physostigmine reversal of midazolam-induced electroencephalographic changes in healthy subjects.
Ebert, U; Kirch, W; Oertel, R, 2000
)
2.47
"Physostigmine has no effect on BIS values or on the tests assessing recovery."( Physostigmine does not antagonize sevoflurane anesthesia assessed by bispectral index or enhances recovery.
Fassoulaki, A; Melemeni, A; Papadopoulos, G; Papilas, K; Paraskeva, A, 2002
)
2.48
"Physostigmine salicylate has proved to be a very useful agent for use in the recovery room. "( Experiences with physostigmine in the reversal of adverse post-anaesthetic effects.
Brebner, J; Hadley, L, 1976
)
2.04
"Physostigmine has been important for our understanding of neurohumoral chemical transmission, and in mapping the cholinergic nerves."( [Development of physostigmine from a poisonous plant to an antidote. One of the most important drugs in the development of modern medicine?].
Rygnestad, T, 1992
)
1.35
"Physostigmine has been shown to be effective as a pretreatment against potent anticholinesterase poisons (e.g., soman) in experimental animals, yet it is short acting and causes undesirable side effects in mammals."( Acetylcholinesterase inhibition and anti-soman efficacy of homologs of physostigmine.
Anderson, DR; Bowersox, SL; Harris, LW; Lennox, WJ; Pastelak, AM; Vanderpool, BA, 1992
)
1.24
"Physostigmine (PHY) has the advantage over pyridostigmine of minimizing OP-induced incapacitation because it penetrates into the CNS. "( Assessing the efficacy of azaprophen and physostigmine as a pretreatment for soman-induced incapacitation in guinea pigs by response-surface modeling.
Boyle, RM; Campbell, ED; Carchman, RA; Carter, WH; Gennings, C; Harris, LW; Solana, RP; Talbot, BG, 1990
)
1.99
"Physostigmine has a half-life of 16, 23 and 30 min in rat, dog and man, respectively."( Physostigmine--an overview as pretreatment drug for organophosphate intoxication.
Dube, SN; Somani, SM, 1989
)
2.44
"Physostigmine has been reported to reverse the sedation and paradoxical delirium induced by benzodiazepines. "( Cerebrovascular and cerebral metabolic effects of physostigmine, midazolam, and a benzodiazepine antagonist.
Albrecht, RF; Cook, JM; Hagen, TJ; Hoffman, WE; Miletich, DJ, 1986
)
1.97
"Physostigmine (Phy) has gained prominence recently because of its use in the treatment of Alzheimer's disease and also as a prophylactic agent in the treatment of organophosphate intoxication. "( Drug interaction for plasma protein binding: physostigmine and other drugs.
McFadden, DL; Somani, SM; Unni, LK, 1987
)
1.98
"Physostigmine has been demonstrated to improve the abnormal movements in patients with tardive dyskinesia while scopolamine tends to aggravate abnormal movements and in some cases elicits abnormal movement not previously observed."( Effect of cholinergic and anticholinergic agents on tardive dyskinesia.
Klawans, HL; Rubovits, R, 1974
)
0.97

Actions

Physostigmine enhanced the increase in acetylcholine level but did not modify the time course nor the intensity of the convulsions. It did not increase the slope or alter the position of the CO2-response curves of subjects given droperidol alone. Physostigmin was found to enhance odor discrimination performance on the more difficult discrimination tasks in a dose-related manner.

ExcerptReferenceRelevance
"Physostigmine can produce analgesia by itself, and enhance opiate analgesia; but these effects are of short duration following bolus administration."( Continuous physostigmine combined with morphine-based patient-controlled analgesia in the postoperative period.
Beilin, B; Bessler, H; Papismedov, L; Shavit, Y; Weinstock, M, 2005
)
1.44
"Physostigmine did not produce a 50% change in arousal as measured by a return of righting reflex but did produce physostigmine toxicity (fasciculations and seizures) in this rat model of severe GHB intoxication."( Physostigmine does not effect arousal but produces toxicity in an animal model of severe gamma-hydroxybutyrate intoxication.
Bania, TC; Chu, J, 2005
)
3.21
"Physostigmine did not increase the slope or alter the position of the CO2-response curves of subjects given droperidol alone."( Physostigmine antagonizes morphine-induced respiratory depression in human subjects.
Bahar, M; Davidson, JT; Snir-Mor, I; Weinstock, M, 1983
)
2.43
"Physostigmine enhanced the increase in acetylcholine level but did not modify the time course nor the intensity of the convulsions."( Methionine sulfoximine increases acetylcholine level in the rat brain: no relation with epileptogenesis.
Hevor, T; Richard, O, 1995
)
1.01
"Physostigmine was found to enhance odor discrimination performance on the more difficult discrimination tasks in a dose-related manner, suggesting that cholinergic activation may sharpen the ability of rats to discern subtle differences among complex odor stimuli."( Physostigmine enhances performance on an odor mixture discrimination test.
Bagla, R; Doty, RL; Kim, N,
)
2.3
"Physostigmine-induced increase in tension was also significantly greater in tissue from lead-treated rats."( The effect of lead on cholinergic contractile function in the rat forestomach.
Ryden, EB; Walsh, CT, 1987
)
0.99

Treatment

Physostigmine given as post-treatment resulted in a time-dependent reduction of the protection from soman inhibition and recovery of AChE. Physostig mine treatment also increased the heat dissipation by decreasing core temperature threshold for vasodilation. The physostIGmine-treated animals that died before the hour showed a dose-related increase in survival time from 4.3 min (untreated controls) to 27.6 min (0.3 mg/kg physostigmin)

ExcerptReferenceRelevance
"Physostigmine treatment also increased the heat dissipation by decreasing core temperature threshold for vasodilation."( Heat loss during exercise is related to serotonin activity in the preoptic area.
Coimbra, CC; Marubayashi, U; Rodrigues, AG; Soares, DD, 2009
)
1.07
"Physostigmine given as post-treatment resulted in a time-dependent reduction of the protection from soman inhibition and recovery of AChE."( Pre- and post-treatment effect of physostigmine on soman-inhibited human erythrocyte and muscle acetylcholinesterase in vitro.
Hatz, RA; Herkert, NM; Schulz, S; Thiermann, H; Wille, T; Worek, F, 2011
)
1.37
"Physostigmine pretreatment augmented the depressant effect of alcohol on the early components P1 and N1, while attenuating alcohol's influence on components P2 and P3."( Cholinergic role in alcohol's effects on evoked potentials in visual cortex of the albino rat.
Hetzler, BE; Smith, TM,
)
0.85
"Physostigmine pretreatment increases the dose of propofol required to produce loss of consciousness."( Physostigmine increases the dose of propofol required to induce anaesthesia.
Derveniotis, C; Fassoulaki, A; Sarantopoulos, C, 1997
)
3.18
"Physostigmine pretreatment (0.2 mg/kg i.p.) also enhanced the motor depression produced by ethanol."( Cholinergic mediation of motor effects of ethanol in rats.
Makowski, E; Newman, B; Pohorecky, LA; Rassi, E, 1979
)
0.98
"The physostigmine-treated animals that died before the hour showed a dose-related increase in survival time from 4.3 min (untreated controls) to 27.6 min (0.3 mg/kg physostigmine)."( Physostigmine-induced cerebral protection against hypoxia.
Scremin, AM; Scremin, OU,
)
2.05
"Physostigmine-pretreatment diminished the rise in blood pressure by O-acetyltyramine, but the effect of tyramine remained unchanged."( Effect of acetyl derivatives of some sympathomimetic amines on the blood pressure of the rat.
Friström, S; Halmekoski, J; Klinge, E; Marvola, M, 1977
)
0.98
"Physostigmine treatment increased levels of alternation whereas reserpine was without effect."( Interaction between cholinergic and catecholaminergic agents in a spontaneous alternation task.
Anisman, H; Kokkinidis, L, 1976
)
0.98
"Physostigmine treatment of the patients induced a speeding of responses to invalidly cued targets as a function of the duration of the disease."( Effects of physostigmine on spatial attention in patients with progressive supranuclear palsy.
Kertzman, C; Litvan, I; Robinson, DL, 1990
)
1.39
"Physostigmine, as a pretreatment candidate for nerve agent poisoning, was examined for cardiopulmonary side effects. "( Effects of physostigmine on the cardiopulmonary system of conscious pigs.
Corcoran, KD; Hurt, HH; Jaeger, JJ; Kaminskis, A; Parrish, JH; Stemler, FW; Tezak-Reid, TM, 1990
)
2.11
"For physostigmine-treated rats the level of cholinesterase inhibition 1 h after ultrasound application was 53 +/- 5% in the ultrasound-treated group and 35 +/- 5% in the controls."( Effect of ultrasound on transdermal drug delivery to rats and guinea pigs.
Kost, J; Langer, R; Levy, D; Meshulam, Y, 1989
)
0.76
"Physostigmine pretreatment significantly altered the lethality of cocaine, increasing the LD 50 from 82.5 mg/kg to 96.9 mg/kg in male F344 rats."( Modulation of the lethal effects of cocaine by cholinomimetics.
Goldberg, SR; Katz, JL; Kuhar, MJ; Witkin, JM, 1989
)
1
"Physostigmine treatment was associated with marginal and inconsistent changes in long-term memory, suggesting that cholinergic therapy alone is insufficient to restore cognitive function."( Physostigmine treatment of progressive supranuclear palsy.
Atack, JR; Chase, TN; Gillespie, M; Gomez, C; Kask, AM; Litvan, I; Mouradian, MM, 1989
)
2.44
"Physostigmine treatment also improved the search strategy during the spatial probe trial compared to the untreated NBM-lesioned rats."( Continuous physostigmine infusion in rats with excitotoxic lesions of the nucleus basalis magnocellularis: effects on performance in the water maze task and cortical cholinergic markers.
Chen, AD; Connor, DJ; Mandel, RJ; Thal, LJ, 1989
)
1.39
"With physostigmine pretreatment, 8 mg/m2 can be administered."( A phase I trial of spirohydantoin mustard (NSC 172112) in patients with advanced cancer.
Brown, TD; Donehower, RC; Ettinger, DS, 1986
)
0.73
"Physostigmine treatment appeared to improve memory with or without concomitant lecithin therapy."( Acute and chronic effects of oral physostigmine and lecithin in Alzheimer's disease.
Davies, P; Fuld, PA; Masur, DM; Sharpless, NS; Thal, LJ, 1986
)
1.27
"Physostigmine pretreatment (0.1 mg/kg) significantly reduced the incidence of ventricular arrhythmias after myocardial ischaemia but had no effect on any of the other arrhythmias.3."( Studies on the effect of physostigmine on experimental cardiac arrhythmias in dogs.
Bhattacharya, SK; Das, PK, 1972
)
1.28
"Treatment with physostigmine salicylate was feasible and safe. "( Effect of physostigmine on recovery from septic shock following intra-abdominal infection - Results from a randomized, double-blind, placebo-controlled, monocentric pilot trial (Anticholium® per Se).
Brenner, T; Bruckner, T; Hofer, S; Hoppe-Tichy, T; Knebel, P; Larmann, J; Lehmann, M; Motsch, J; Pinder, N; Swoboda, S; Weigand, MA; Zimmermann, JB, 2019
)
1.27
"Treatment with physostigmine resulted in at least 50% inhibition of muscle ChE activity, but produced minimal changes in the MCD values in adults or juveniles."( Single fiber electromyographic jitter and detection of acute changes in neuromuscular function in young and adult rats.
Finley, DB; Graff, JE; Herr, DW; Wang, X,
)
0.47
"The treatment with physostigmine in endotoxemia may be of interest for clinical use, and further studies should be performed."( Effects of physostigmine on microcirculatory alterations during experimental endotoxemia.
Hofer, S; Martin, E; Peter, C; Schmidt, K; Stephan, M; Walther, A; Weigand, MA, 2010
)
1.07
"Treatment with physostigmine salicylate (two doses of 2 mg i.m., I hr apart) was effective in counteracting the paralysis, as well as other symptoms, beginning in as little as 17 min after the first dose, and the whale was back to swimming on its own after 8 hr."( Subacute atropine toxicity in a pygmy sperm whale, Kogia breviceps.
Byrd, L; Cunningham-Smith, P; Manire, CA; Rhinehart, HL; Smith, DR, 2002
)
0.65
"Treatment with physostigmine significantly reduced lethality (p < or = .01) as efficiently as direct stimulation of the cholinergic anti-inflammatory pathway with nicotine (p < or = .05). "( Pharmacologic cholinesterase inhibition improves survival in experimental sepsis.
Bierhaus, A; Bode, K; Brueckmann, M; Dalpke, AH; Eisenbach, C; Encke, J; Hofer, S; Krammer, PH; Lukic, IK; Martin, E; Mautner, S; Nawroth, PP; Schneider, L; Stremmel, W; Weigand, MA; Wente, MN; Werner, J, 2008
)
0.7
"Treatment with physostigmine (IM) produced a rapid and sustained reversal of these symptoms."( A case of phenylcyclohexylpyrrolidine (PHP) intoxication treated with physostigmine.
Castellani, S; Giannini, AJ, 1982
)
0.84
"Pretreatment with physostigmine offered marked protection against inhibition of AChE by soman, as shown by enzyme activity determination in different brain regions and in diaphragm muscle."( Efficacy of antidotes against soman poisoning in female physostigmine-protected rats.
Sket, D, 1993
)
0.86
"Treatment with physostigmine does not improve the conditions of patients with ataxia."( Double-blind crossover study with physostigmine in patients with degenerative cerebellar diseases.
Kömpf, D; Langenberger, K; Nitschke, MF; Wessel, K, 1997
)
0.93
"Pretreatment with physostigmine salicylate and scopolamine hydrochloride at dose rates of 2.5 and 1 microg x kg(-1) x h(-1), respectively, was administered via Alzet mini-osmotic pumps."( Prophylaxis against organophosphate poisoning by sustained release of scopolamine and physostigmine.
Alkalai, D; Chapman, S; Cohen, G; Levy, A; Meshulam, Y, 2001
)
0.86
"Treatment with physostigmine reversed the central anticholinergic syndrome as well as the electrocardiographic abnormalities."( Physostigmine for cardiac and neurologic manifestations of phenothiazine poisoning.
Goldbarg, A; Klawans, HL; Kramer, J; Weisdorf, D, 1978
)
2.04
"Rats treated with physostigmine pre- or postsession learned significantly more reversals over 50 sessions than animals injected with vehicle."( Effects of physostigmine on operant serial discrimination/reversal learning in rats.
Clissold, DB; Heise, GA, 1990
)
0.99
"Rats treated with physostigmine (0.9 mg/kg) showed a reduced number of muscarinic receptors, but no change in nicotinic receptors."( Tetrahydroaminoacridine induces opposite changes in muscarinic and nicotinic receptors in rat brain.
Lai, Z; Nilsson-Håkansson, L; Nordberg, A, 1990
)
0.6
"Pretreatment with physostigmine briefly decreased the amplitude of the ketamine-induced positive spike, augmented the amplitude of the succeeding positive component, and also increased most peak latencies."( Effects of ketamine, naloxone, and physostigmine on flash evoked potentials in rat superior colliculus.
Hetzler, BE; Melk, AM, 1989
)
0.88
"Pre-treatment with physostigmine prevented curare-induced tetanic fade in the tibialis anterior, but not the soleus."( Activity-dependent differences between rat fast and slow neuromuscular systems.
Baker, T; Storella, RJ, 1988
)
0.59
"Treatment with physostigmine reduced the number of avoidances made, and did so similarly for all prenatal treatment groups."( Effects of physostigmine on shuttle avoidance in rats exposed prenatally to ethanol.
Blanchard, BA; Riley, EP,
)
0.86
"Treatment with physostigmine in vivo reduced binding in all regions without affecting apparent affinity."( High-affinity hemicholinium-3 binding to brain membranes: reduction by treatment with physostigmine in vivo.
Guynn, RW; Hewitt, LO; Swann, AC, 1986
)
0.83
"Pretreatment with physostigmine augmented the salivary response to both nerve stimulation and PGF(2alpha).4."( Salivation induced by prostaglandin F 2 and modification of the response by atropine and physostigmine.
Hahn, RA; Patil, PN, 1972
)
0.79

Toxicity

physostigmine is a safe and effective antidote for the treatment of antimuscarinic toxicity. HC-3 increased the LD50 values for both physstigmine and neostigmin but did not alter the effect on brain ACh levels produced by these agents.

ExcerptReferenceRelevance
" The effect of pretreatment with five different beta-adrenoceptor blocking drugs (propranolol, alprenolol, practolol, metoprolol or tolamolol), p physostigmine, or atropine on these toxic actions of doxepin was investigated."( Effect of beta-adrenoceptor blocking drugs, physostigmine, and atropine on the toxicity of doxepin in mice.
Elonen, E, 1975
)
0.72
" Treatment is aimed at removing plant material from the gastrointestinal tract, keeping the patient safe and reversing severe anticholinergic sequelae."( Jimson weed toxicity: management of anticholinergic plant ingestion.
Mosser, KH; Vanderhoff, BT, 1992
)
0.28
" Initially, considerable information will have to be gathered from various laboratories to form the background data on which decisions of toxic effects can be made."( Correlation between behavioral and pathological changes in the evaluation of neurotoxicity.
Beyrouty, P; Broxup, B; Losos, G; Robinson, K, 1989
)
0.28
"The aim of the present study was to compare the reliability of LD50 determination using the traditional Litchfield and Wilcoxon method with that obtained by four alternative tests requiring smaller numbers of animals, for the purpose of classifying chemicals according to their acute toxicity."( Comparison of five methods for the determination of lethal dose in acute toxicity studies.
Carvalho, RR; Cunha, FQ; Fingola, FF; Freitas, JC; Menezes, MA; Paumgartten, FJ; Presgrave, OA, 1989
)
0.28
" However, pharmacological agents that enhance central cholinergic and noradrenergic neurotransmission, like physostigmine and clonidine, might have serious adverse effects."( Combined administration of physostigmine and clonidine to patients with dementia of the Alzheimer type: a pilot safety study.
Bierer, LM; Davidson, M; Davis, KL; Kaminsky, R; Ryan, TM, 1989
)
0.79
" The signs of toxicity in the guinea pigs which received the low dose appeared within 2 or 3 days and then the animals recovered, while toxic signs in the guinea pigs treated with the high dose of the drug persisted throughout the experiments."( Toxicity study of continuous administration of physostigmine salicylate.
Ho, IK; Hoskins, B; Ito, Y; Lim, DK; Stewart, T, 1988
)
0.53
"The ability of the carbamates pyridostigmine and physostigmine to protect against the lethal effects of soman, an extremely toxic anticholinesterase agent, was measured in rats, guinea pigs and rabbits."( Effect of carboxylesterase inhibition on carbamate protection against soman toxicity.
Brecht, KM; Lenz, DE; Maxwell, DM; O'Neill, BL, 1988
)
0.53
" HC-3 increased the LD50 values for both physostigmine and neostigmine but did not alter the effect on brain ACh levels produced by these agents."( Antagonism of acute physostigmine and neostigmine toxicity in mice by hemicholinium-3.
Freeman, JJ; Kosh, JW; Lin, J, 1987
)
0.86
" An additive toxic effect of atropine was suggested with its combinations with TMB4, mecamylamine, and diazepam, whereas no additive toxicity occurred with combinations involving hexamethonium or benactyzine (i."( Efficacy and toxicity of drug combinations in treatment of physostigmine toxicosis.
Klemm, WR, 1983
)
0.51
" The toxic arrhythmogenic effects of the tricyclic antidepressants can be measured by RET and are partly autonomic tone manipulation."( Cardiotoxicity of amitriptyline and doxepin.
Aronow, WS; Tobis, JM, 1981
)
0.26
" Intravenous physostigmine, the treatment of choice, was used to resolve the toxic crisis."( Atropine toxicity in identical twins.
Burke, MJ; Sanitato, JJ, 1983
)
0.64
" This suggested a predominantly central site for the toxic interaction."( Synergism of the toxicity of physostigmine and neostigmine by lithium or by a reserpine-like agent (Ro4-1284).
Davis, WM; Hatoum, NS, 1980
)
0.55
" Although drugs can ameliorate certain toxic effects, indiscriminate use of purported antidotes can have deleterious results."( Toxicity of tricyclic antidepressants--kinetics, mechanism, intervention: a review.
Irwin, HA; Preskorn, SH, 1982
)
0.26
" The LD50 of diazepam and chlordiazepoxide were not modified by physostigmine administration, but that of flurazepam was significantly decreased."( Effects of physostigmine on benzodiazepine toxicity.
Bamonte, F; Ongini, E; Parravicini, L, 1981
)
0.89
" All patients completed the study without intolerable or severe adverse events."( A multiple-dose safety trial of eptastigmine in Alzheimer's disease, with pharmacodynamic observations of red blood cell cholinesterase.
Barchowsky, A; Block, GA; Cutler, NR; Reines, SA; Sawin, SF; Sramek, JJ, 1995
)
0.29
" LD50 of soman was determined at various time intervals after pretreatment."( Huperzine A as a pretreatment candidate drug against nerve agent toxicity.
Ashani, Y; Doctor, BP; Grunwald, J; Raveh, L, 1994
)
0.29
" No significant cardiac side effects were noted, though other systemic adverse effects were noted, requiring dose reduction in four patients."( Safety and efficacy of oral physostigmine in the treatment of Alzheimer disease.
Bell, K; Marder, K; Mayeux, R; Sano, M; Stern, Y; Stricks, L, 1993
)
0.58
" After subchronically administered PHY or PHY + SCO, the treated animals were protected against a 3 x LD50 dose of soman."( Subchronic physostigmine pretreatment in guinea pigs: effective against soman and without side effects.
Bruijnzeel, PL; Busker, RW; Melchers, BP; Olivier, B; Philippens, IH; Wolthuis, OL, 1998
)
0.69
" Eleven patients on placebo (7%), 13 patients on eptastigmine 15 mg three times daily (8%), and 12 patients on eptastigmine 20 mg three times daily (8%) discontinued study treatment because of adverse events."( Efficacy and safety of eptastigmine for the treatment of patients with Alzheimer's disease.
Imbimbo, BP; Lucca, U; Lucchelli, F; Martelli, P; Thal, LJ; Troetel, WM, 1999
)
0.3
" Although the cholinergic tolerability of eptastigmine was found to be favorable, its potential adverse hematologic effects limit its clinical utility."( Efficacy and safety of eptastigmine for the treatment of patients with Alzheimer's disease.
Imbimbo, BP; Lucca, U; Lucchelli, F; Martelli, P; Thal, LJ; Troetel, WM, 1999
)
0.3
" Furthermore, this treatment regime, followed by atropine as postintoxication therapy, protected the marmosets against lethality after a 2 x LD50 dose of soman with negligible postintoxication incapacitation."( Subchronic physostigmine pretreatment in marmosets: absence of side effects and effectiveness against soman poisoning with negligible postintoxication incapacitation.
Bruijnzeel, PL; Groen, B; Melchers, BP; Olivier, B; Philippens, IH; Vanwersch, RA, 2000
)
0.7
"Phosphorus oxychloride (POCl(3)) is an intermediate in the synthesis of many organophosphorus insecticides and chemical warfare nerve gases that are toxic to insects and mammals by inhibition of acetylcholinesterase (AChE) activity."( Phosphoacetylcholinesterase: toxicity of phosphorus oxychloride to mammals and insects that can be attributed to selective phosphorylation of acetylcholinesterase by phosphorodichloridic acid.
Casida, JE; Quistad, GB; Sparks, SE; Zhang, N, 2000
)
0.31
"Spontaneously active neuronal networks grown from embryonic murine frontal cortex on substrate integrated electrode arrays with 64 recording sites were used to assess acute neurobiological and toxic effects of a series of seven symmetrical, bifunctional alkylene-linked bis-thiocarbonate compounds designed to possess anticholinesterase activity."( Acute toxicity screening of novel AChE inhibitors using neuronal networks on microelectrode arrays.
Boyle, NA; Gross, GW; Keefer, EW; Norton, SJ; Talesa, V, 2001
)
0.31
" Although physostigmine is considered an acceptable antidote for severe DPH toxicity, adverse effects such as seizures and cholinergic crisis may occur."( Physostigmine, sodium bicarbonate, or hypertonic saline to treat diphenhydramine toxicity.
Engebretsen, KM; Harris, CR; Holger, JS, 2002
)
2.16
" The latter combinations also had milder adverse impact on the animals' interest in the test environment and activity measures than the former combinations."( Cognitive side effects in rats caused by pharmacological agents used to prevent soman-induced lethality.
Aas, P; Enger, S; Myhrer, T, 2004
)
0.32
" The authors hypothesized that in the setting of severe GHB intoxication, physostigmine would reverse sedation without producing adverse effects such as a decrease in heart rate, seizures, and fasciculations."( Physostigmine does not effect arousal but produces toxicity in an animal model of severe gamma-hydroxybutyrate intoxication.
Bania, TC; Chu, J, 2005
)
2
" The onset of differentiation intensified the adverse effects on DNA synthesis and changed the rank order in keeping with a shift away from noncholinergic mechanisms and toward cholinergic mechanisms."( Screening for developmental neurotoxicity using PC12 cells: comparisons of organophosphates with a carbamate, an organochlorine, and divalent nickel.
MacKillop, EA; Ryde, IT; Seidler, FJ; Slotkin, TA; Tate, CA, 2007
)
0.34
" Results suggest that DEET may have some toxic actions that are similar to those of formamidine pesticides."( Synergism of toxicity of N,N-diethyl-m-toluamide to German cockroaches (Orthoptera: Blattellidae) by hydrolytic enzyme inhibitors.
Moss, JI, 1996
)
0.29
" None demonstrated response and, further, there were associated adverse events, including atrial fibrillation (2), pulmonary infiltrates (1) and significant bradycardia (1), and hypotension (1)."( Physostigmine for gamma-hydroxybutyrate coma: inefficacy, adverse events, and review.
Litonjua, R; Smith, SW; Westfal, RE; Zvosec, DL, 2007
)
1.78
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" The transdermal patches did not induce any adverse reactions such as erythema and edema on intact skin sites."( Acute dermal irritation, sensitization, and acute toxicity studies of a transdermal patch for prophylaxis against ({+/-}) anatoxin-a poisoning.
Banerjee, S; Chattopadhyay, P; Ghosh, A; Pathak, MP; Singh, S; Veer, V, 2013
)
0.39
" The method can easily be scaled up to serve as a high-throughput screening tool to detect sublethal toxic effects of a variety of chemicals."( Optical bioassay for measuring sublethal toxicity of insecticides in Daphnia pulex.
Kashian, DR; McElmurry, SP; Pitts, DK; Savolainen, PT; Zein, MA, 2014
)
0.4
" Recent literature has demonstrated that physostigmine is a safe and effective antidote for the treatment of antimuscarinic toxicity."( Use of a physostigmine continuous infusion for the treatment of severe and recurrent antimuscarinic toxicity in a mixed drug overdose.
Acquisto, NM; Gorodetsky, RM; Phillips, MA; Wiegand, TJ, 2014
)
1.09
" The patient did not experience any adverse effects of physostigmine administration."( Use of a physostigmine continuous infusion for the treatment of severe and recurrent antimuscarinic toxicity in a mixed drug overdose.
Acquisto, NM; Gorodetsky, RM; Phillips, MA; Wiegand, TJ, 2014
)
1.07
" Despite controversy, studies have shown that physostigmine is relatively safe and effective in reversing this toxidrome."( The Use of Physostigmine by Toxicologists in Anticholinergic Toxicity.
Arroyo-Plasencia, AM; Mullins, ME; Schwarz, ES; Watkins, JW, 2015
)
1.07
"To describe effectiveness, adverse events, and dosing associated with the use of physostigmine to reverse anticholinergic delirium."( Safety and effectiveness of physostigmine: a 10-year retrospective review.
Al-Abri, S; Arens, AM; Kearney, T; Olson, KR; Shah, K, 2018
)
1
"3%), had no documented adverse effects."( Safety and effectiveness of physostigmine: a 10-year retrospective review.
Al-Abri, S; Arens, AM; Kearney, T; Olson, KR; Shah, K, 2018
)
0.77
" No adverse events were reported from physostigmine administration."( Datura and Brugmansia plants related antimuscarinic toxicity: an analysis of poisoning cases reported to the Taiwan poison control center.
Doan, UV; Mendez Rojas, B; Phua, DH; Wu, ML; Yang, CC, 2019
)
0.78
" We completed a narrative literature review to identify reported adverse effects associated with physostigmine administration."( Adverse Effects of Physostigmine.
Arens, AM; Kearney, T, 2019
)
1.06
" Adverse effects occurred in 415 (18."( Adverse Effects of Physostigmine.
Arens, AM; Kearney, T, 2019
)
0.84
"In conclusion, significant adverse effects associated with the use of physostigmine were infrequently reported."( Adverse Effects of Physostigmine.
Arens, AM; Kearney, T, 2019
)
1.08

Pharmacokinetics

The pharmacokinetic changes of parathion and paraoxon were investigated. The elimination half-life of physostigmine was 16.

ExcerptReferenceRelevance
" After a single dose, heptastigmine remained for a long time in plasma (the terminal half-life was about 12 h), distributed widely in tissues (the volume of distribution was about 61) and brain concentrations were very high (4-22 times those found in plasma)."( Pharmacokinetics of heptastigmine in rats.
Baldi, A; Cerretani, D; Segre, G; Urso, R,
)
0.13
" The concentration-time profile for each animal was fitted to standard pharmacokinetic models."( Pharmacokinetics of physostigmine intramuscularly administered to guinea pigs.
Clark, CR; Lukey, BJ; Marlow, DD; Parrish, JH; Sidell, FR, 1990
)
0.6
"A sensitive high-performance liquid chromatographic method was developed to determine pharmacokinetic parameters of [3H]physostigmine from serial plasma samples from guinea pigs."( Application of a new radiometric high-performance liquid chromatographic assay to define physostigmine pharmacokinetics in guinea pigs.
Clark, CR; Lieske, CN; Lukey, BJ; Marlow, DD; McCluskey, MP, 1989
)
0.71
" The half-life of Phy in liver after iv and im administration was found to be 24 and 26 min, respectively, indicating that Phy does not show dose-dependent kinetics."( Hepatic and muscle clearance of physostigmine in the rat.
Somani, SM; Unni, LK,
)
0.41
" The pharmacokinetic constants A, B, alpha, beta, AUC, K10 half-life, alpha-half-life, beta-half-life, K10, K12, and K21 were obtained."( Pharmacokinetics and pharmacodynamics of physostigmine in the rat after intravenous administration.
Khalique, A; Somani, SM,
)
0.4
"A pediatric Phase I and pharmacokinetic study of the lipophilic alkylating agent spirohydantoin mustard (SHM) was conducted in 23 patients."( A pediatric phase I and pharmacokinetic study of spirohydantoin mustard.
Balis, F; Doherty, KM; Ettinger, LJ; Heideman, RL; Jeffries, SL; Kelley, JA; Packer, RJ; Poplack, DG; Reaman, GH; Roth, JS, 1988
)
0.27
" 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
" Pharmacokinetic parameters, obtained in the dog, were compared to previously published data in rat and man."( Pharmacokinetics and pharmacodynamics of physostigmine after intravenous administration in beagle dogs.
Downen, M; Giacobini, E; Hallak, M; McIlhany, M; Somani, S, 1987
)
0.54
" The half-life of Phy in plasma and brain was 17 and 16 min, respectively."( Distribution and pharmacokinetics of physostigmine in rat after intramuscular administration.
Khalique, A; Somani, SM, 1986
)
0.54
" A fraction of the dose was probably hydrolyzed in blood since its blood elimination half-life in vitro was approximately 190 min."( Pharmacokinetics of physostigmine after intravenous, intramuscular and subcutaneous administration in surgical patients.
Hartvig, P; Lindström, B; Wiklund, L, 1986
)
0.59
" The half-life of Phy was found to be 21."( Pharmacokinetics of biliary excretion of physostigmine in rat.
Boyer, AW; Somani, SM, 1985
)
0.54
" Pharmacokinetic parameters obtained by this method after a single oral dose of 900 mg soluble, effervescent acetylsalicylic acid in normal healthy subjects suggest that absorption, distribution, and elimination of acetylsalicylic acid are rapidly occurring events."( Measurement and pharmacokinetics of acetylsalicylic acid by a novel high performance liquid chromatographic assay.
Bochner, F; Cham, BE; Imhoff, DM; Ross-Lee, L, 1980
)
0.26
"To study the pharmacokinetic and pharmacodynamic properties of physostigmine in subjects with Alzheimer's disease."( Clinical pharmacokinetics of physostigmine in patients with Alzheimer's disease.
Asthana, S; Greig, NH; Hegedus, L; Holloway, HH; Raffaele, KC; Schapiro, MB; Soncrant, TT, 1995
)
0.82
"The elimination half-life of physostigmine was 16."( Clinical pharmacokinetics of physostigmine in patients with Alzheimer's disease.
Asthana, S; Greig, NH; Hegedus, L; Holloway, HH; Raffaele, KC; Schapiro, MB; Soncrant, TT, 1995
)
0.87
" Furthermore, during single-dose conditions, the dynamic half-life is five-fold longer than the kinetic half-life."( Clinical pharmacokinetics of physostigmine in patients with Alzheimer's disease.
Asthana, S; Greig, NH; Hegedus, L; Holloway, HH; Raffaele, KC; Schapiro, MB; Soncrant, TT, 1995
)
0.58
"The pharmacokinetic of some centrally acting cholinesterase inhibitors that have been used to improve memory in patients with dementia of Alzheimer's type, was compared."( Pharmacokinetic studies of cholinesterase inhibitors.
Johansson, M; Nordberg, A, 1993
)
0.29
" A preliminary evaluation of its pharmacodynamic and pharmacokinetic profiles in the elderly has now been made in 6 healthy subjects (63-84 years of age) given 30 mg eptastigmine as a single oral dose."( Pharmacodynamics and pharmacokinetics of eptastigmine in elderly subjects.
Auteri, A; Imbimbo, BP; Lattuada, N; Luzzana, M; Mosca, A; Radice, D; Zecca, L, 1993
)
0.29
" Drug interactions with cholinesterase inhibitors may occur by pharmacokinetic or pharmacodynamic mechanisms."( Pharmacokinetics and drug interactions of cholinesterase inhibitors administered in Alzheimer's disease.
Crismon, ML,
)
0.13
" Pharmacodynamic activity of eptastigmine was evaluated with an assay of AChE activity in red blood cells."( Maximum tolerated dose and pharmacodynamics of eptastigmine in elderly healthy volunteers.
Imbimbo, BP; Mant, T; Troetel, WM, 1998
)
0.3
" Its long duration of action, coupled with its short pharmacokinetic half-life, reduces dosing frequency, decreases body drug exposure and minimizes the dependence of drug action on the individual variations of drug metabolism commonly found in the elderly."( The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics.
Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS, 2000
)
0.31
" The pharmacokinetic changes of parathion and paraoxon were investigated after intravenous administration of parathion, 3 mg/kg, to control Sprague-Dawley rats, and the rats pretreated with physostigmine (100 microg/kg, intraperitoneal injection 30 min before parathion administration)."( Effects of physostigmine on the pharmacokinetics of intravenous parathion in rats.
Hurh, E; Kim, SH; Kim, SY; Kim, YC; Kim, YG; Lee, EJ; Lee, MG, 2000
)
0.89
" Pharmacokinetic studies have revealed that after oral administration eptastigmine is rapidly distributed to the tissues and readily enters the CNS, where it can be expected to inhibit AChE for a prolonged period."( Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies.
Braida, D; Sala, M, 2001
)
0.31
" The method is rapid, simple and reliable, thus it is suitable for pharmacokinetic studies in the rat."( Simple liquid chromatographic method for the determination of physostigmine and its metabolite eseroline in rat plasma: application to a pharmacokinetic study.
Chaw, CS; Moochhala, SM; Yang, YY; Zhao, B, 2003
)
0.56
" The Cmax and AUC(0-24) of phenserine increased with dose, but neither were dose-proportional."( Anticholinesterase and pharmacokinetic profile of phenserine in healthy elderly human subjects.
Brownell, L; Burford, RG; Canfield, CJ; Comer, P; Flanagan, DR; Greig, NH; Holloway, HW; Ruckle, J, 2005
)
0.33
"Posiphen single and multiple ascending dose phase 1 randomised, double blind, placebo-controlled safety, tolerance, pharmacokinetic studies were undertaken in a total of 120 healthy volunteers to define a dose that was then used in a small non-randomised study of five MCI subjects, used as their own controls, to define target engagement."( Posiphen as a candidate drug to lower CSF amyloid precursor protein, amyloid-β peptide and τ levels: target engagement, tolerability and pharmacokinetics in humans.
Chang, MY; Greig, NH; John, V; Maccecchini, ML; Pan, C; Zetterberg, H, 2012
)
0.38
" Pharmacodynamic analyses of ChEIs provide paradoxical observations."( Pharmacodynamics of cholinesterase inhibitors suggests add-on therapy with a low-dose carbamylating inhibitor in patients on long-term treatment with rapidly reversible inhibitors.
Darreh-Shori, T; Hosseini, SM; Nordberg, A, 2014
)
0.4
"In the present study, a simple reverse-phase high-performance liquid chromatography method with diode array detection has been developed and validated for the simultaneous determination and quantification of eserine and pralidoxime chloride in rabbit plasma and its application to pharmacokinetic study."( Pharmacokinetic and biodistribution study of eserine and pralidoxime chloride in rabbits following a single application of a transdermal patch.
Banerjee, S; Bhatnagar, A; Chattopadhyay, P; Ghosh, A; Veer, V, 2016
)
0.43
" Remarkably low plasma concentrations can be quantified after LLE with gradient elution and fluorescence detection, making this a suitable method for pharmacokinetic studies in a clinical setting."( Revival of physostigmine - a novel HPLC assay for simultaneous determination of physostigmine and its metabolite eseroline designed for a pharmacokinetic study of septic patients.
Brenner, T; Gubbe, U; Hofer, S; Hoppe-Tichy, T; Pinder, N; Swoboda, S; Weigand, MA; Zimmermann, JB, 2015
)
0.81

Compound-Compound Interactions

Physostigmine combined with morphine in the postoperative period reduced morphine consumption, enhanced analgesia, and attenuated production of the proinflammatory cytokine, IL-1beta.

ExcerptReferenceRelevance
" In each case, a double-blind, placebo-controlled, single-subject, A-B-A design was used with A representing the base-line phases, B constituting the memory training combined with medication phase and A representing the return to base-line condition."( Memory training combined with the use of oral physostigmine.
Bergerud, DB; Cardenas, DD; McLean, A; Stanton, KM,
)
0.39
"Atropine, in combination with 1 of 6 other drugs, was tested in mice for the ability to prevent death by an otherwise lethal dose of the cholinesterase inhibitor, physostigmine."( Efficacy and toxicity of drug combinations in treatment of physostigmine toxicosis.
Klemm, WR, 1983
)
0.7
" We describe here our experience from a programme based on assisted ejaculation combined with in vitro fertilization (IVF)."( Assisted ejaculation combined with in vitro fertilisation: an effective technique treating male infertility due to spinal cord injury.
Garoff, L; Hillensjö, T; Hultling, C; Levi, R; Nylund, L; Rosenborg, L; Sjöblom, P, 1994
)
0.29
" This may be particularly important in cases in which hypotensive action is exerted by the agent used in combination with the calcium channel blocker."( Shuttle-box avoidance behavior of mice treated with nifedipine in combination with nicotine or physostigmine.
Battaglia, M; Sansone, M; Vetulani, J,
)
0.35
"We compared pain intensity and morphine consumption in two postoperative treatment groups: One group received continuous physostigmine infusion combined with morphine-based patient-controlled analgesia (PCA), and the other received PCA alone."( Continuous physostigmine combined with morphine-based patient-controlled analgesia in the postoperative period.
Beilin, B; Bessler, H; Papismedov, L; Shavit, Y; Weinstock, M, 2005
)
0.93
"Continuous infusion of physostigmine combined with morphine-based PCA in the postoperative period significantly reduced opiate consumption, and enhanced the analgesic response."( Continuous physostigmine combined with morphine-based patient-controlled analgesia in the postoperative period.
Beilin, B; Bessler, H; Papismedov, L; Shavit, Y; Weinstock, M, 2005
)
1.03
"Physostigmine combined with morphine in the postoperative period reduced morphine consumption, enhanced analgesia, and attenuated production of the proinflammatory cytokine, IL-1beta."( Continuous physostigmine combined with morphine-based patient-controlled analgesia in the postoperative period.
Beilin, B; Bessler, H; Papismedov, L; Shavit, Y; Weinstock, M, 2005
)
2.16

Bioavailability

Physostigmine nasal bioavailability was 100% as compared with iv bioavailability, and that of arecoline was 85% when compared with bioavailability following im administration. The physostigmin emulsion apparently increased the bioavailability compared with the conventional injectable solution.

ExcerptReferenceRelevance
" Physostigmine nasal bioavailability was 100% as compared with iv bioavailability, and that of arecoline was 85% when compared with bioavailability following im administration."( Intranasal absorption of physostigmine and arecoline.
Hussain, MA; Mollica, JA, 1991
)
1.49
" Oral bioavailability was 25."( Reversal of postoperative somnolence using a two-rate infusion of physostigmine.
Hartvig, P; Lindström, B; Pettersson, E; Wiklund, L, 1989
)
0.51
" The bioavailability of Phy is very low (about 2%) and it is extensively metabolized in the liver."( Physostigmine--an overview as pretreatment drug for organophosphate intoxication.
Dube, SN; Somani, SM, 1989
)
1.72
" The preliminary pharmacokinetic analysis showed that the physostigmine emulsion apparently increased the bioavailability compared with the conventional injectable solution."( Pharmacological evaluation of an injectable prolonged release emulsion of physostigmine in rabbits.
Benita, S; Friedman, D; Weinstock, M, 1986
)
0.75
" 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
"The relations between motility, tone, water absorption rate (Jv) and lymph flow (J1), were studied in an exteriorized upper jejunal preparation in vivo, with its serosal side bathed in Krebs-Ringer or other solutions."( Relationship between intestinal motility, tone, water absorption and lymph flow in the rat.
Lee, JS, 1983
)
0.27
" A mean absolute bioavailability of 36% was determined for the transdermal system and 3% for the oral solution."( Pharmacokinetics of physostigmine in man following a single application of a transdermal system.
Barkworth, MF; Müller, M; Nieciecki, AV; Stanislaus, F; Walter, K, 1995
)
0.61
"The ingestion of food significantly reduces the bioavailability of eptastigmine estimated by the assay of red blood cell acetylcholinesterase activity."( Effect of food on the absorption of eptastigmine.
Bjornsson, TD; Imbimbo, BP; Troetel, WM, 1998
)
0.3
" In this study, the bioavailability of aspirin was compared in plain aspirin tablets, chewed tablets, effervescent tablets and Enteric-coated aspirin tablets."( A comparative bioavailability study of different aspirin formulations using on-line multidimensional chromatography.
Sagar, KA; Smyth, MR, 1999
)
0.3
" doses provided an estimate of oral bioavailability of 100%."( The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics.
Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS, 2000
)
0.31
" Like many oral drugs, bioavailability and plasma concentrations of PST are regulated by hepatic and gastrointestinal first-pass effects."( Preclinical investigation of the topical administration of phenserine: transdermal flux, cholinesterase inhibition, and cognitive efficacy.
Greig, NH; Holloway, HW; Ingram, DK; Irie, T; Irikura, M; Mamczarz, J; Moriuchi, H; Spangler, EL; Uchimura, N; Utsuki, T; Yu, QS, 2007
)
0.34
" The bioavailability (plasma level) after intravenous administration was 82."( Preparation and in vivo evaluation of a water-soluble prodrug for 2R-gamma-tocotrienol and as a two-step prodrug for 2,7,8-trimethyl-2S-(beta-carboxyethyl)-6-hydroxychroman (S-gamma-CEHC) in rat.
Akaho, N; Fujioka, T; Fukui, K; Fukushima, T; Hattori, A; Hidaka, R; Imai, K; Karube, Y; Matsunaga, K; Takata, J; Yoshida, M, 2007
)
0.34
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs."( Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
Bajusz, D; Balogh, GT; Dargó, G; Müller, J; Simon, K, 2020
)
0.56

Dosage Studied

physostigmine was used to reverse anticholinergic delirium. It did not alter the effective opening rate for a subsaturating dosage of carbachol. pretreatment with an antisense oligonucleotide (aODN) against type 1 or type 3 RyR prevented cholinergic antin.

ExcerptRelevanceReference
" It can be administered only subcutaneously or orally, and adequate dosage is necessary for a successful response."( Uropharmacology: v. choline esters and other parasympathomimetic drugs.
Bissada, NK; Finkbeiner, AE; Welch, LT, 1977
)
0.26
" This theory attributes the thousand-fold increase in sensitivity to exogenous acetylcholine produced by anticholinesterases in chick biventer cervicis muscles largely to an alteration in acetylcholine concentration gradient within the muscle and accounts satisfactorily for the shift in the dose-response curve for acetylcholine which occurs after treatment of the muscles with various concentrations of physostigmine."( The relationship between cholinesterase inhibition in the chick biventer cervicis muscle and its sensitivity to exogenous acetylcholine.
Green, AL; Lord, JA; Marshall, IG, 1978
)
0.42
" SHPGE2, PGE2, and C did not cause catalepsy and did not show statistically significant dose-response antagonism of rotational behavior at less than toxic doses."( Neuropharmacological and behavioral evaluation of prostaglandin E2 and 11-thiol-11-desoxy prostaglandin E2 in the mouse and rat.
Bloss, JL; Singer, GH, 1978
)
0.26
" FS-32 showed anti-reserpine activity in a dose-dependent manner, whereas imipramine exhibited a bell-shaped dose-response pattern."( Pharmacological studies on a new thymoleptic antidepressant, 1-[3-(dimethylamino)propyl]-5-methyl-3-phenyl-1H-indazole (FS-32).
Fujimura, Y; Ikeda, Y; Iwasaki, T; Koide, T; Matsushita, H; Nagashima, R; Shindo, M; Shiraki, Y; Suzuki, S; Takano, N, 1979
)
0.26
"20 mg/kg IM) caused only decreases in response rates, the dose-response curve for atropine being particularly flat over a wide range of doses."( Effects of phencyclidine, atropine and physostigmine, alone and in combination, on variable-interval performance in the squirrel monkey.
Balster, RL; Chait, LD, 1979
)
0.53
" Methods for presenting dose-response data for the ganglionic actions of cholinergic agonists (e."( The pharmacology of an insect ganglion: actions of carbamylcholine and acetylcholine.
Callec, JJ; Dowson, RJ; McClay, AS; Sattelle, DB, 1976
)
0.26
" The dose-response curve for ATP is then more than half-maximal at 1 mM and the ranking of the other nucleotides relative to ATP is the same as without predigestion."( Potentiation of postjunctional cholinergic sensitivity of rat diaphragm muscle by high-energy-phosphate adenine nucleotides.
Ewald, DA, 1976
)
0.26
" Drug vs no drug training showed that discriminability was proportional to dosage for low doses, but was constant over a range of higher doses."( Discriminable effects of antimuscarinics: dose response and substitution test studies.
Overton, DA, 1977
)
0.26
"2 x 10(-6) M) displaced the dose-response curve for tetraethylammonium-methohexitone-induced contractures to the right."( Contractures elicited by tetraethylammonium in avian muscle treated with methohexitone.
Elliott, RC, 1979
)
0.26
" Dose-response curves showed a positive, linear relationship between dose (0."( Physostigmine: effects on fear or defense responses in the rat.
Mollenauer, S; Plotnik, R; Tiffany, PB; White, M, 1979
)
1.7
" All these compounds led to abnormalities of the cervical vertebrae; at higher dosage interference with normal morphogenesis involved the whole vertebral column."( Cholinomimetic teratogens: studies with chicken embryos.
Landauer, W, 1975
)
0.25
" Incremental doses of amphetamine and pilocarpine correspondingly suppressed PhAD parameters in a dose-response fashion."( Pharmacological suppression of photically evoked after-discharges in rats: incremental dose, hippocampal EEG and behavioral activity correlates.
Bigler, ED; Fleming, DE, 1976
)
0.26
" The assay has been fully validated in the concentration range 50-2000 pg/ml and utilized for the analysis of clinical samples from subjects dosed with heptylphysostigmine."( Determination of picogram levels of heptylphysostigmine in human plasma using high-performance liquid chromatography with fluorescence detection.
Constanzer, ML; Herold, ML; Matuszewski, BK, 1992
)
0.74
" Acute tetrahydroaminoacridine (THA) dosing caused lower brain (68%) and higher plasma (90%) ChE inhibition than the other drugs studied and increased levels of brain dihydroxyphenylacetic acid (DOPAC) (236%), homovanillic acid (HVA) (197%) and 5-hydroxyindoleacetic acid (5-HIAA) (130%)."( Effect of acute and chronic cholinesterase inhibition on biogenic amines in rat brain.
Shillcutt, S; Soininen, H; Unni, L, 1990
)
0.28
" However, it was necessary to determine the dose-response effects of PH administration before PH-treated exercising rats could be used as a model with which to examine the relative anticholinergic potency of drugs."( Physostigmine: dose-response effects on endurance and thermoregulation during exercise.
Francesconi, RP; Hubbard, RW; Matthew, CB, 1992
)
1.73
"2 mg/kg) of pilocarpine, a muscarinic agonist, showed a significant improvement of both types of memory deficit with bell shaped dose-response curves."( Differential effects of physostigmine and pilocarpine on the spatial memory deficits produced by two septo-hippocampal deafferentations in rats.
Maeda, N; Matsuoka, N; Ohkubo, Y; Yamaguchi, I, 1991
)
0.59
" Reducing stimulus control did not impair performance and did not alter the dose-response curve for induction of a deficit by scopolamine."( Evidence against a specific effect of cholinergic drugs on spatial memory in primates.
Field, MJ; Iversen, SD; Rupniak, NM; Samson, NA; Tye, SJ, 1991
)
0.28
" Subacute dosing for 7 days was done via 14-day osmotic minipumps (OMPs)."( Effects of subacute pretreatment with carbamate together with acute adjunct pretreatment against nerve agent exposure.
Anderson, DR; Harris, LW; Lennox, WJ; Solana, RP, 1991
)
0.28
" The 5 events during continuous infusion intoxication only happened in high dosed patients."( Intrathecal baclofen overdose: report of 7 events in 5 patients and review of the literature.
Brouwers, JR; Delhaas, EM, 1991
)
0.28
" Dose-response studies of intestinal muscle after 3 mo of untreated diabetes showed normal tension development to both bethanechol chloride and physostigmine."( Adaptation of cholinergic enteric neuromuscular transmission in diabetic rat small intestine.
Harrington, B; Kalbfleisch, J; Nowak, TV, 1990
)
0.48
" Dose-response curves to the muscarinic agonist bethanechol (BCh) alone were compared with responses to BCh plus U46619."( Airway generation-dependent induction of muscarinic hyperresponsiveness by thromboxane mimetic in vitro.
Barger, LW; Evans, JN, 1991
)
0.28
"These results indicate a longer period of biological activity for physostigmine than previously considered and extend previous reports of improved verbal learning after oral physostigmine treatment to a more convenient dosing schedule."( Improved verbal learning after outpatient oral physostigmine therapy in patients with dementia of the Alzheimer type.
Guterman, A; Sevush, S; Villalon, AV, 1991
)
0.78
" In vitro dose-response studies of circular and longitudinal small intestinal muscle from the diabetic animals showed normal tension development and sensitivity to both bethanechol chloride and physostigmine."( Structural and functional characteristics of muscle from diabetic rodent small intestine.
Harrington, B; Kalbfleisch, JH; Nowak, TV; Weisbruch, JP, 1990
)
0.47
" For all dosage groups, physostigmine concentrations peaked in approximately 30 min."( Pharmacokinetics of physostigmine intramuscularly administered to guinea pigs.
Clark, CR; Lukey, BJ; Marlow, DD; Parrish, JH; Sidell, FR, 1990
)
0.91
"A selective and stability-indicating high-performance liquid chromatographic assay with diazepam as the internal standard was developed for simultaneously analyzing physostigmine and tetrahydroaminoacridine in skin samples, permeation diffusates and dosage form."( Simultaneous determination of physostigmine and tetrahydroaminoacridine in a transdermal permeation study by high-performance liquid chromatography.
Chow, D; Feldman, S; Lau, SW, 1990
)
0.76
" In 2-h dose-response studies, there was a fivefold increase in sensitivity to acetylcholine when fragments were preincubated 1 h with iso-OMPA."( Inhibition of acetyl- and butyrylcholinesterase and amylase release from canine pancreas.
Borner, JW; Dressel, TD; Goodale, RL; Miller, J; Oguchi, Y, 1989
)
0.28
") shifted the dose-response curves for the positive inotropic effect of plasma-dissolved (PD) ibopamine (0."( Analysis of the positive inotropic effect of ibopamine in the blood-perfused canine papillary muscle.
Inui, J; Kawahara, K,
)
0.13
" The indication to treat unwanted central effects of benzodiazepines either with flumazenil or with physostigmine after anaesthesia should be restricted to cases of distinctly prolonged sedation after adequate dosage or adverse side effects."( Flumazenil (Ro 15-1788) and physostigmine.
Lauven, PM; Stoeckel, H, 1988
)
0.79
" The physostigmine dose-response curve for the stimulation of [3H]IP1 accumulation was similar to its dose-response curve to inhibit acetylcholinesterase activity in the neostriatum."( Physostigmine stimulates phosphoinositide breakdown in the rat neostriatum.
Aceves, J; Góngora, JL; Mariscal, S; Sierra, A, 1988
)
2.23
" The time course of radioactivity per gram of liver after iv dosing (100 micrograms/kg), showed the major metabolite to be M1, followed by M2 and Es, whereas after im dosing (650 micrograms/kg), Es was present in larger amounts than were other metabolites."( Hepatic and muscle clearance of physostigmine in the rat.
Somani, SM; Unni, LK,
)
0.41
" Addition of the acetylcholinesterase inhibitor, physostigmine, caused a leftward shift in the GABA dose-response curve and increased by 10-fold the sensitivity of the antral preparation to GABA stimulation."( Cholinergic mediation of gamma-aminobutyric acid-induced gastrin and somatostatin release from rat antrum.
Franklin, PA; Harty, RF, 1986
)
0.53
" At the corresponding dosage rates, rat whole blood acetylcholinesterase (AChE) activity was suppressed by approximately 11, 42, and 66%, respectively."( Effects of subacute administration of physostigmine on blood acetylcholinesterase activity, motor performance, and soman intoxication.
Anderson, DR; Harris, LW; Lennox, WJ; Solana, RP, 1989
)
0.55
" The dose-response curves were bell-shaped."( Relation between yawning behavior and central serotonergic neuronal system in rats.
Aihara, H; Hashimoto, S; Okuyama, S; Shimamura, H, 1987
)
0.27
" Following depletion of brain DA, but not NE, animals exhibited a "supersensitive" increase in plasma ACTH values, which was evidenced by a sixfold left shift in the dose-response properties of PHY."( Supersensitive endocrine response to physostigmine in dopamine-depleted rats: a model of depression?
Britton, KT; Downs, NS; Gibbs, DM; Koob, GF; Swerdlow, NR, 1986
)
0.54
" Partial protection was seen in three out of three birds dosed prior to DFP challenge with sufficient C(-)P(+) isomer of soman (1."( High doses of soman protect against organophosphorus-induced delayed polyneuropathy but tabun does not.
Benschop, HP; De Bisschop, HC; Johnson, MK; Read, DJ; Willems, JL, 1988
)
0.27
" All of the drugs, with the exception of vinconate, exhibited a monotonic dose-response curve and caused 100% survival at some dose."( Protective effects of vinpocetine and structurally related drugs on the lethal consequences of hypoxia in mice.
King, GA, 1987
)
0.27
" Injection of spiromustine on a split-dose schedule decreased the acute neurological toxicity in mice and allowed a larger total dosage to be delivered (compared to single bolus dosage)."( Phase I trial of spiromustine (NSC 172112) and evaluation of toxicity and schedule in a murine model.
Baker, LH; Corbett, T; Pazdur, R; Phillips, M; Redman, BG, 1987
)
0.27
" Mechanical responses of sensitized TSM were characterized by hyperreactivity (upward shift of the dose-response relationship) to acetylcholine (ACh), atropine-sensitive spontaneous base line activity and prolonged isometric force plateaus."( Local parasympathetic mechanisms for ragweed-sensitized canine trachealis hyperresponsiveness.
Kepron, W; Kroeger, EA; Mitchell, RW; Stephens, NL, 1987
)
0.27
" The physiology of the anticholinergic system and physostigmine are discussed along with the indications, toxicity, and dosing of physostigmine."( Central anticholinergic syndrome in a child: a case report.
Richmond, M; Seger, D, 1985
)
0.52
" As dosage of these compounds increased, only small effects on accuracy were observed, followed at still larger doses by an abrupt and non-selective decrease in all responding."( Effects of pesticides and drugs on working memory in rats: continuous non-match.
Heise, GA; Hudson, JD, 1985
)
0.27
" In both species at 30 min after im injection of Py and Ph, a linear relationship was found between percentage of whole blood AChE inhibition and ln dosage of carbamate."( Relationship between reversible acetylcholinesterase inhibition and efficacy against soman lethality.
Anderson, DR; Harris, LW; Lennox, WJ; Talbot, BG, 1985
)
0.27
" Log dose-response curves for acetylcholine and carbachol were constructed in the presence of triethylcholine, tubocurarine and physostigmine, in both innervated and denervated chick biventer cervicis muscles."( Actions of acetylcholine and carbachol on the chick biventer cervicis muscle.
Marshall, IG, 1971
)
0.45
" Occlusion of the right vertebral artery shifted the dose-response curve to the left."( Central cardiovascular effects of physostigmine in the cat; possible cholinergic aspects of blood pressure regulation.
de Wildt, DJ; Porsius, AJ, 1981
)
0.54
" On the other hand, in the presence of prostaglandin (PG)-inhibitors the dose-response curve of acetylcholine shifts to the right."( In vitro effect of acetylcholine and bethanechol on the contractions of the human detrusor muscle. Influence of prostaglandins.
Borda, E; Contreras-Ortiz, N; Gimeno, MF; Gutnisky, R, 1982
)
0.26
") produced about a 10 fold rightward shift of the dose-response curve for guanoxabenz."( alpha 2-Adrenoceptor agonists induced mydriasis in the rat by an action within the central nervous system.
Berridge, TL; Gadie, B; Roach, AG; Tulloch, IF, 1983
)
0.27
" Thus, the dose-response curve shows an U-shaped form."( The impairment of retention induced by beta-endorphin in mice may be mediated by a reduction of central cholinergic activity.
Baratti, CM; Introini, IB, 1984
)
0.27
" Because the endplate potential (EPP) amplitude is a composite of pre- and post-junctional effects, the dose-response curve for neostigmine on EPP amplitude approximately paralleled that obtained on MEPP amplitude, whereas the effect of physostigmine on EPP amplitude was depressed because of its action to decrease transmitter release."( Further comparison of the effects of physostigmine and neostigmine on frog neuromuscular transmission.
Alderdice, MT,
)
0.59
" A BDF dosage of each carbamate (0."( Toxicity of anticholinesterases: interactions of pyridostigmine and physostigmine with soman.
Anderson, DR; Harris, LW; Lennox, WJ; Swanson, DR; Talbot, BG, 1984
)
0.5
" DA and 5-HT turnover rates were little affected by the same dosage of MCI-2016."( [Effects of 4-(o-benzylphenoxy)-N-methylbutylamine hydrochloride (MCI-2016) on monamine metabolism in the brain].
Egawa, M; Ida, S; Inokuchi, T; Tobe, A, 1983
)
0.27
" All patients had their best performance following one of the doses of physostigmine rather than saline although dose-response curves varied from one patient to another."( A signal detectability analysis of the effect of physostigmine on memory in patients with Alzheimer's disease.
Davis, KL; Mohs, RC, 1982
)
0.75
" The recorded tremor intensity showed a clear dose-response relationship for physostigmine."( Quantification of tremor in rats induced by physostigmine.
Gothóni, P; Lehtinen, M; Silen, L, 1981
)
0.75
" This confirms a previous report of a lethal synergism of physostigmine after subacute dosing with lithium."( Synergism of the toxicity of physostigmine and neostigmine by lithium or by a reserpine-like agent (Ro4-1284).
Davis, WM; Hatoum, NS, 1980
)
0.8
" While our findings are discrepant with two previous studies, our use of multiple self-ratings, and some differences in physostigmine dosage and infusion times might have contributed to this difference."( Physostigmine induction of depressive symptomatology in normal human subjects.
Cohen, RM; Gillin, JC; Janowsky, DS; Kalin, NH; Murphy, DL; Risch, SC; Sitaram, N, 1981
)
1.91
" Steady-state TCA plasma levels correlate well with tissue concentrations and permit adjustment of dosage to minimize the risk of iatrogenic poisoning."( Toxicity of tricyclic antidepressants--kinetics, mechanism, intervention: a review.
Irwin, HA; Preskorn, SH, 1982
)
0.26
"In the light of studies on the duration of action and pharmacokinetics of intravenous neostigmine, it is recommended that, depending upon the dosage administered, at least 1 hour should elapse before a depolarizer can safely be given after neuromuscular reversal with neostigmine, and at least 90 - 120 minutes after reversal with physostigmine."( Administration of depolarizing muscle relaxants after non-depolarizer reversal: when is it safe?
De Roubaix, JA, 1982
)
0.44
" We have not seen any side effects after physostigmine administration, but the possibility of undesired parasympathomimetic activity demands correct indication, well calculated dosage and continuous surveillance of the patient."( [On the use of physostigmine in anesthesia and intensive care].
Abel, M; George, G; Kiss, I, 1982
)
0.88
" The extent of inhibition was in parallel with the dosage of the drugs used."( The inhibition and protection of cholinesterase by physostigmine and pyridostigmine against Soman poisoning in vivo.
Pei, SQ; Wang, LX; Xia, DY,
)
0.38
" 3 Hemicholinium-3 (HC-3) caused a rightward shift of the dose-response curve to DL-muscarine on the ileal longitudinal muscle of the guinea-pig ileum."( Mechanism of action of muscarine on the longitudinal muscle of the guinea-pig isolated ileum.
Ochillo, RF; Tsai, CS; Tsai, MH, 1981
)
0.26
" All active compounds gave inverted U-shaped dose-response curves."( Cognition-activating properties of 3-(Aryloxy)pyridines.
Butler, DE; Marriott, JG; Poschel, BP, 1981
)
0.26
" For the use of the equation, the parallel shift of the dose-response curve and the unchanged maximum response are prerequisites."( An extension of pA principle to the potentiation of drug effects, and its application to the biological assay of some anticholinesterases and cardenolides.
Ichikawa, T; Ishikawa, N; Shigei, T; Tsuru, H, 1980
)
0.26
" The dose-response curve showed a U-shaped form."( The impairment of retention induced by insulin in mice may be mediated by a reduction in central cholinergic activity.
Baratti, CM; Kopf, SR, 1995
)
0.29
" To evaluate the functional implications of this neuronal deficit, dose-response curves were obtained in patients with progressive supranuclear palsy and normal control subjects undergoing intravenous cholinergic blockade (scopolamine) and stimulation (physostigmine)."( Pharmacological evaluation of the cholinergic system in progressive supranuclear palsy.
Atack, JR; Blesa, R; Chase, TN; Clark, K; Grafman, J; Litvan, I; Mouradian, MM; Nichelli, P, 1994
)
0.47
"Transdermal delivery of cholinesterase inhibitors (ChEI) for treatment of dementia would have advantages associated with continuous dosing and enhanced compliance, but feasibility depends on achieving desired levels of central nervous system enzyme inhibition."( Transdermal patch delivery of acetylcholinesterase inhibitors.
Becker, RE; Moriearty, PL; Thornton, SL,
)
0.13
" There was little evidence of a dose-response relationship for either compound, and a loss of efficacy for ondansetron was seen at 3 mg/kg."( Ondansetron improves cognitive performance in the Morris water maze spatial navigation task.
Daniels, SE; Eglen, RM; Fontana, DJ; Henderson, C; Wong, EH, 1995
)
0.29
" Thus, the dose-response curve adopted an inverted U-shaped form."( Effects of posttraining administration of glucose on retention of a habituation response in mice: participation of a central cholinergic mechanism.
Baratti, CM; Kopf, SR, 1996
)
0.29
" Drug dosing was limited by the occurrence of adverse effects."( Treatment of Alzheimer disease by continuous intravenous infusion of physostigmine.
Asthana, S; Berardi, A; Greig, NH; Haxby, JV; Raffaele, KC; Schapiro, MB; Soncrant, TT, 1995
)
0.53
" The reversal of scopolamine-induced impairment was characterized by the presence of an inverted U-shaped dose-response curve."( An inverted U-shaped curve for heptylphysostigmine on radial maze performance in rats: comparison with other cholinesterase inhibitors.
Braida, D; Griffini, P; Lamperti, M; Maggi, A; Paladini, E; Sala, M, 1996
)
0.57
" Dosage was escalated by a forced upward titration during the first 6 to 9 weeks of the trial, then maintained at a constant dose to 24 weeks."( A 24-week randomized trial of controlled-release physostigmine in patients with Alzheimer's disease.
Ferguson, JM; Mintzer, J; Raskin, A; Targum, SD; Thal, LJ, 1999
)
0.56
" Studies were carried out in control animals and after dosing with phenserine, a selective centrally active AChE inhibitor; neostigmine, a peripheral cholinesterase inhibitor; and a combination of the two drugs."( Simplified methods for in vivo measurement of acetylcholinesterase activity in rodent brain.
Kilbourn, MR; Sherman, PS; Snyder, SE, 1999
)
0.3
"A multi-dimensional column chromatographic method employing UV spectrometric detection was optimised and successfully used in a comparative bio-availability study of aspirin obtained from different commercially available oral dosage forms."( A comparative bioavailability study of different aspirin formulations using on-line multidimensional chromatography.
Sagar, KA; Smyth, MR, 1999
)
0.3
" Constant infusion of physostigmine at a dosage of 250 microg/kg/min produced an identical increase in radioligand binding."( Acetylcholinesterase inhibition increases in vivo N-(2-[18F]fluoroethyl)-4-piperidyl benzilate binding to muscarinic acetylcholine receptors.
Kilbourn, MR; Sherman, PS; Skaddan, MB; Snyder, SE, 2001
)
0.63
" Its long duration of action, coupled with its short pharmacokinetic half-life, reduces dosing frequency, decreases body drug exposure and minimizes the dependence of drug action on the individual variations of drug metabolism commonly found in the elderly."( The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics.
Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS, 2000
)
0.31
" Dosing continued for 4 consecutive days."( Concurrent quantification of tremor and depression of locomotor activity induced in rats by harmaline and physostigmine.
Fowler, SC; Wang, G, 2001
)
0.52
" The relationship between patient performance and average steady-state AChE inhibition was described by an inverted U-shaped dose-response curve."( Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies.
Braida, D; Sala, M, 2001
)
0.31
" A sustained-release of physostigmine with a low initial burst over 1 week was achieved from RG 502 microparticles, which would be used as an injectable dosage form in our further animal studies."( Design of physostigmine-loaded polymeric microparticles for pretreatment against exposure to organophosphate agents.
Chaw, CS; Moochhala, S; Tan, CW; Wang, L; Yang, YY, 2003
)
1.03
" In chlorpyrifos-treated animals, pilocarpine dose-response curves were shifted significantly to the right, demonstrating decreased responsiveness of neuronal M2 receptors."( Mechanisms of organophosphate insecticide-induced airway hyperreactivity.
Beckles, RA; Fryer, AD; Howard, AS; Jett, DA; Lein, PJ; Yost, BL, 2004
)
0.32
" Dose-response curves for tremor (central effect) and salivation (peripheral effect) showed that donepezil and icopezil possess a more favourable therapeutic index than the nonselective inhibitors, tacrine and heptylphysostigmine."( Pharmacology of selective acetylcholinesterase inhibitors: implications for use in Alzheimer's disease.
Chapin, D; Hubbard, ST; Jones, SB; Liston, DR; Nason, D; Nielsen, JA; Ramirez, A; Shalaby, IA; Villalobos, A; White, WF, 2004
)
0.51
" Indeed, atropine-induced suppression of the DCE was found to be an inverted U-shaped dose-response curve."( Cholinergic effects on fear conditioning I: the degraded contingency effect is disrupted by atropine but reinstated by physostigmine.
Carnicella, S; Oberling, P; Pain, L, 2005
)
0.54
" Particular benefits over oral therapies might include avoiding first-pass metabolic effects and improved dosing compliance."( Preclinical investigation of the topical administration of phenserine: transdermal flux, cholinesterase inhibition, and cognitive efficacy.
Greig, NH; Holloway, HW; Ingram, DK; Irie, T; Irikura, M; Mamczarz, J; Moriuchi, H; Spangler, EL; Uchimura, N; Utsuki, T; Yu, QS, 2007
)
0.34
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" Phenserine is also unique because of differing actions of its enantiomers: (-)-phenserine is the active enantiomer for inhibition of AChE, whereas (+)-phenserine ('posiphen') has weak activity as an AChE inhibitor and can be dosed much higher."( Phenserine.
Klein, J, 2007
)
0.34
" A shift to the right of the physostigmine dose-response curve was obtained after anti-type 2 IP3R2 and anti-type 3 IP3R treatments."( Knockdown of the type 2 and 3 inositol 1,4,5-trisphosphate receptors suppresses muscarinic antinociception in mice.
Bartolini, A; Galeotti, N; Ghelardini, C; Quattrone, A; Vivoli, E, 2007
)
0.63
" pretreatment with an antisense oligonucleotide (aODN) against type 1 or type 3 RyR prevented cholinergic antinociception in the hotplate test shifting to the right of the physostigmine dose-response curve."( Type 1 and type 3 ryanodine receptors are selectively involved in muscarinic antinociception in mice: an antisense study.
Bartolini, A; Galeotti, N; Ghelardini, C; Quattrone, A; Vivoli, E, 2008
)
0.54
" The presence of physostigmine did not alter the effective opening rate for a subsaturating dosage of carbachol, suggesting that physostigmine does not interact with the nicotinic agonist binding site."( Activation and block of the adult muscle-type nicotinic receptor by physostigmine: single-channel studies.
Akk, G; Ma, BW; Militante, J; Steinbach, JH, 2008
)
0.92
"This article provides an evaluation of the dose-response features of drugs that are intended to improve memory, some of which have been used in the treatment of Alzheimer's disease (AD)."( Alzheimer's disease drugs: an application of the hormetic dose-response model.
Calabrese, EJ, 2008
)
0.35
" Drug assay, content uniformity of the dosage unit, drug dissolution and accelerated stability studies were done on the optimum formulation as further experiments."( Development and optimization of a sublingual tablet formulation for physostigmine salicylate.
Bolourchian, N; Foroutan, SM; Hadidi, N; Shafaghi, B, 2009
)
0.59
" 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
" We have assessed in vivo the mortality-reducing efficacy of a group of known AChE inhibitors, when given in equitoxic dosage before exposure to the OPC paraoxon."( Usefulness of administration of non-organophosphate cholinesterase inhibitors before acute exposure to organophosphates: assessment using paraoxon.
Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA; Shafiullah, M, 2013
)
0.39
" It could be also used with reliability for the determination of the drug in other pharmaceutical dosage forms."( Development and validation of a reverse phase liquid chromatography method for the simultaneous quantification of eserine and pralidoxime chloride in drugs-in-adhesive matrix type transdermal patches.
Banerjee, S; Chattopadhyay, P; Ghosh, A; Kaity, S; Veer, V, 2013
)
0.39
" Protection was quantified using Cox analysis by determining the relative risk (RR) of death in rats that were administered these AChE inhibitors in equitoxic dosage (25% of LD01) 30 min before azinphos-methyl exposure."( Reversible cholinesterase inhibitors as pre-treatment for exposure to organophosphates: assessment using azinphos-methyl.
Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA, 2015
)
0.42
" Cholinesterase inhibitors, such as physostigmine, are effective but widespread use has been limited by concerns about safety, optimal dosing and variable supply."( Pharmacological management of anticholinergic delirium - theory, evidence and practice.
Buckley, NA; Dawson, AH, 2016
)
0.71
" These actions translated into amelioration of spatial and visual memory impairments in a mouse model of closed head mild TBI (mTBI) two days following cessation of clinically translatable dosing with phenserine (2."( Cognitive Impairments Induced by Concussive Mild Traumatic Brain Injury in Mouse Are Ameliorated by Treatment with Phenserine via Multiple Non-Cholinergic and Cholinergic Mechanisms.
Barak, S; Becker, KG; Becker, RE; Fukui, K; Greig, NH; Hoffer, BJ; Holloway, HW; Lehrmann, E; Li, Y; Luo, Y; Perez, E; Pick, CG; Rubovitch, V; Tamargo, IA; Tweedie, D; Van Praag, H; Wood, WH; Yu, QS; Zhang, Y, 2016
)
0.43
" However, its effectiveness, safety profile, and dosing have been disputed."( Safety and effectiveness of physostigmine: a 10-year retrospective review.
Al-Abri, S; Arens, AM; Kearney, T; Olson, KR; Shah, K, 2018
)
0.77
"To describe effectiveness, adverse events, and dosing associated with the use of physostigmine to reverse anticholinergic delirium."( Safety and effectiveness of physostigmine: a 10-year retrospective review.
Al-Abri, S; Arens, AM; Kearney, T; Olson, KR; Shah, K, 2018
)
1
" (-)-Phenserine mitigated OGD/PR-induced SH-SY5Y cell death, providing an inverted U-shaped dose-response relationship between concentration and survival."( (-)-Phenserine inhibits neuronal apoptosis following ischemia/reperfusion injury.
Becker, RE; Chang, CF; Chen, KY; Chen, YH; Chiang, YH; Greig, NH; Kang, SJ; Lai, JH; Luo, Y; Wu, JC, 2017
)
0.46
" We hence developed an extended controlled release formulation of (-)-phenserine to provide individualized dosing and stable therapeutic brain concentrations, to pharmacologically interrogate PPCD as a drug development target."( (-)-Phenserine and Inhibiting Pre-Programmed Cell Death: In Pursuit of a Novel Intervention for Alzheimer's Disease.
Aarsland, D; Ballard, C; Becker, RE; Bledsoe, J; Ferrucci, L; Flanagan, D; Govindarajan, R; Greig, NH; Kapogiannis, D; Lahiri, DK; Majercik, S; Sano, M; Schneider, LS, 2018
)
0.48
" EtOH-PHY treatment rescued mPFC expression of c-Fos in ethanol-exposed rats and increased Arc and Npas4 regardless of dosing condition."( Cholinergic rescue of neurocognitive insult following third-trimester equivalent alcohol exposure in rats.
Heroux, NA; Horgan, CJ; Rosen, JB; Stanton, ME, 2019
)
0.51
"0 mg/kg), donepezil tended to promote depression-like behavior, suggesting a u-shaped dose-response curve for FST immobility."( Multiple cholinesterase inhibitors have antidepressant-like properties in the mouse forced swim test.
Fitzgerald, PJ; Ghimire, A; Hale, PJ; Watson, BO, 2021
)
0.62
" This can be delivered orally or via nasogastric tube with dosing each hour until resolution of symptoms."( Oral and Transdermal Rivastigmine for the Treatment of Anticholinergic Delirium: A Case Report.
Fratta, KA; Ginder, M; Haggerty, DA, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
mioticAn agent causing contraction of the pupil of the eye. Because the size of the pupil is under the antagonistic control of the sympathetic and parasympathetic systems, drugs affecting either system can cause miosis. Drugs that mimic or potentiate the parasympathetic input to the circular constrictor muscle and drugs that inhibit sympathetic input to the radial dilator muscle tend to contract the pupils.
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).
antidote to curare poisoningA role borne by a molecule that acts to counteract or neutralize the deleterious effects of curare.
[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
indole alkaloidAn alkaloid containing an indole skeleton.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[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]

Pathways (2)

PathwayProteinsCompounds
superpathway of melatonin degradation526
melatonin degradation II014

Protein Targets (51)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.81140.140911.194039.8107AID2451
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
acetylcholinesteraseHomo sapiens (human)Potency0.53810.002541.796015,848.9004AID1347395; AID1347397; AID1347398; AID1347399
thioredoxin reductaseRattus norvegicus (Norway rat)Potency29.93490.100020.879379.4328AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency15.95560.006038.004119,952.5996AID1159521; AID1159523
GLS proteinHomo sapiens (human)Potency14.18060.35487.935539.8107AID624146; AID624170
TDP1 proteinHomo sapiens (human)Potency9.44110.000811.382244.6684AID686979
GLI family zinc finger 3Homo sapiens (human)Potency61.13060.000714.592883.7951AID1259392
AR proteinHomo sapiens (human)Potency6.85900.000221.22318,912.5098AID743042
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency14.12540.011212.4002100.0000AID1030
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency25.11890.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency27.59010.000214.376460.0339AID720692
pregnane X nuclear receptorHomo sapiens (human)Potency34.37620.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.00490.000229.305416,493.5996AID743075
cytochrome P450 2D6Homo sapiens (human)Potency0.97720.00108.379861.1304AID1645840
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
IDH1Homo sapiens (human)Potency12.99530.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency29.01990.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency61.53610.000723.06741,258.9301AID743085; AID743122
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.28180.540617.639296.1227AID2364; AID2528
hexokinase-4 isoform 1Homo sapiens (human)Potency10.00002.511913.800328.1838AID743205
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency23.93410.134610.395030.1313AID1347049
glucokinase regulatory proteinHomo sapiens (human)Potency10.00002.511913.800328.1838AID743205
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency44.53460.000627.21521,122.0200AID651741; AID743202; AID743219
gemininHomo sapiens (human)Potency1.45810.004611.374133.4983AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency21.60270.005612.367736.1254AID624032; AID624044
survival motor neuron protein isoform dHomo sapiens (human)Potency28.18380.125912.234435.4813AID1458
M-phase phosphoprotein 8Homo sapiens (human)Potency31.62280.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency0.00400.891312.067628.1838AID1487
[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)
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)3.10170.00000.94539.9400AID1143297; AID1185413; AID1312273; AID1377833; AID1615656; AID1615707; AID1695066; AID1801485; AID30541; AID30849; AID30999; AID355917; AID361188; AID386741; AID444034; AID692822
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki0.03400.00121.25638.9000AID692827
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1209455
AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC50 (µMol)0.30230.00570.42855.1200AID1153516; AID1801938; AID30660
CholinesteraseHomo sapiens (human)IC50 (µMol)1,455,053,270,767.98490.00001.559910.0000AID1142531; AID1240268; AID1570277; AID1657596; AID1796572; AID1801485; AID1801528; AID1801939; AID1807566; AID1820979; AID1916836; AID241042; AID276346; AID282008; AID355918; AID44271; AID44277; AID44284; AID44292; AID44421; AID44422; AID44423; AID44437; AID44450; AID44580
CholinesteraseHomo sapiens (human)Ki5.00000.00001.51739.7300AID44301
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)0.20000.00002.015110.0000AID625249
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)160.00000.00053.314249.5000AID142802
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.85700.00021.874210.0000AID355918
AcetylcholinesteraseMus musculus (house mouse)IC50 (µMol)0.02690.00071.11818.4000AID31781; AID464986; AID465031
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)0.91140.00000.933210.0000AID1240265; AID1290205; AID1308877; AID1389195; AID1657516; AID1657594; AID1742993; AID1796572; AID1801527; AID1807563; AID1820943; AID1853195; AID1916835; AID240779; AID241106; AID241692; AID262754; AID276345; AID282007; AID31013; AID31015; AID31020; AID31021; AID31023; AID31035; AID31165; AID31174; AID31176; AID31496; AID31499; AID31501; AID31504; AID31505; AID31627; AID31768; AID31771; AID31775; AID32279; AID32720; AID491761; AID511766; AID625193; AID654699; AID758230
Acetylcholinesterase Bos taurus (cattle)IC50 (µMol)0.71970.00000.61068.7000AID30678; AID30679; AID30685; AID462833
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.85700.00021.270410.0000AID355918
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)1.18210.00010.729810.0000AID276346
AcetylcholinesteraseGallus gallus (chicken)IC50 (µMol)0.02000.02000.02000.0200AID1123609
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)0.04160.00020.52597.2000AID31964; AID31966; AID32107; AID32108; AID465959
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.85700.00001.819410.0000AID355918
CholinesteraseEquus caballus (horse)IC50 (µMol)0.40810.00002.22149.4000AID1143296; AID1153518; AID1185414; AID1290203; AID1308869; AID1312274; AID1377834; AID361189; AID462834; AID692823
CholinesteraseEquus caballus (horse)Ki0.04100.00203.45989.3700AID692829
CholinesteraseMus musculus (house mouse)IC50 (µMol)0.28000.00910.56021.9920AID464987; AID465032
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC50 (µMol)0.01890.00600.98467.6000AID31035
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC50 (µMol)0.01800.00041.48119.8700AID44422; AID44437; AID44445
Carboxylic ester hydrolase Equus caballus (horse)IC50 (µMol)1.26300.00512.69848.5000AID43950; AID44452; AID654701
[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)
AcetylcholinesteraseElectrophorus electricus (electric eel)K0.03430.03430.03430.0343AID1185422
AcetylcholinesteraseHomo sapiens (human)Kc0.25000.25000.25000.2500AID31613
CholinesteraseEquus caballus (horse)K0.12080.04100.12080.2803AID1143303; AID1185423; AID1290211
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo 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)
retina layer formationAcetylcholinesteraseGallus gallus (chicken)
acetylcholine catabolic processAcetylcholinesteraseGallus gallus (chicken)
choline metabolic processAcetylcholinesteraseGallus gallus (chicken)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo 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)
amyloid-beta bindingAcetylcholinesterase Bos taurus (cattle)
protein bindingAcetylcholinesterase Bos taurus (cattle)
acetylcholinesterase activityAcetylcholinesteraseGallus gallus (chicken)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
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)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo 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)
synapseAcetylcholinesterase Bos taurus (cattle)
side of membraneAcetylcholinesterase Bos taurus (cattle)
synapseAcetylcholinesteraseGallus gallus (chicken)
plasma membraneAcetylcholinesteraseGallus gallus (chicken)
extracellular spaceAcetylcholinesteraseGallus gallus (chicken)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (367)

Assay IDTitleYearJournalArticle
AID1796572Cholinesterase Inhibition Assay from Article 10.1021/jm010491d: \\Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.\\2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
AID1801939Butyrylcholinesterase Assay from Article 10.1016/j.bioorg.2016.07.005: \\Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases.\\2016Bioorganic chemistry, 10, Volume: 68Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases.
AID1801527Acetylcholinesterase Assay from Article 10.1016/j.bioorg.2015.11.002: \\Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.\\2016Bioorganic chemistry, Feb, Volume: 64Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.
AID1801485AChE and BChE Assay from Article 10.1016/j.bioorg.2015.09.008: \\Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast a-glucosidase, acetyl2015Bioorganic chemistry, Dec, Volume: 63Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase.
AID1801528Butyrylcholinesterase Assay from Article 10.1016/j.bioorg.2015.11.002: \\Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.\\2016Bioorganic chemistry, Feb, Volume: 64Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.
AID1801938Acetylcholinesterase Assay from Article 10.1016/j.bioorg.2016.07.005: \\Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases.\\2016Bioorganic chemistry, 10, Volume: 68Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID44293In vitro inhibition of human plasma butyrylcholinesterase.2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.
AID194871Effect after an intraperitoneal dose of 0.1 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID282010Antagonist activity at muscarinic M2 receptor assessed as contraction of electrically stimulated guinea pig left atrium at 10 uM2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
AID44456Inhibitory activity against Butyrylcholinesterase in cortex1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
AID30999Inhibitory activity against Acetylcholinesterase in electric eel1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
AID142655Compound was evaluated for the competitive inhibition of [3H]methylscopolamine binding to muscarinic acetylcholine receptor M2 of mouse cerebral cortex1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID44271In vitro inhibition of Butyrylcholinesterase from human serum1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.
AID31505The compound was evaluated for the inhibition of human Acetylcholinesterase1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID31015Anticholinesterase activity against erythrocyte acetylcholinesterase (AChE) in humans.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
AID464986Inhibition of mouse brain AChE after 1 hr by modified Ellman's colorimetric method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.
AID361188Inhibition of electric eel AChE by Ellman's method2001Journal of natural products, Jun, Volume: 64, Issue:6
Steroidal alkaloids from the leaves of Sarcococca coriacea of Nepalese origin.
AID14399Biodistribution in rat cerebellum, expressed as percent I.D./g tissue1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
AID30864In vitro inhibitory activity against acetylcholinesterase from electric eel1988Journal of medicinal chemistry, Dec, Volume: 31, Issue:12
Synthesis and anticholinesterase activity of (-)-N1-norphysostigmine, (-)-eseramine, and other N(1)-substituted analogues of (-)-physostigmine.
AID227796Concentration required to potentiate the contraction of isolated rat ileum produced by 1 x 10 e -7 M Ach by 20 %1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID44422Inhibitory concentration against butyrylcholinesterase from human serum2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
AID1615656Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 5 mins by Ellman's method2019Journal of natural products, 09-27, Volume: 82, Issue:9
Labdanes, Withanolides, and Other Constituents from
AID117434Compound was evaluated for the approximate lethal dose when mice were administered increasing or decreasing doses of compound intraperitoneally until one fatality was observed1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID465031Inhibition of mouse brain AChE after 1 hr by modified Ellman's colorimetric method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
AID31499Inhibition of human acetylcholinesterase from erythrocytes (RBC)1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.
AID424999Inhibition of AChE assessed as minimum drug level required for white zone of inhibition by bioautography2009Journal of natural products, May-22, Volume: 72, Issue:5
Alkaloids from the roots of Stemona aphylla.
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.
AID282009Selectivity for human BChE over human AChE2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
AID241042Inhibition of isolated human BuChE2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
AID1143301Inhibition of electric eel AChE at 10 uM by Ellman's method2014European journal of medicinal chemistry, Jun-23, Volume: 81Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
AID1377836Inhibition of equine serum BCHE at 0.5 mM using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by Ellman's method relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of novel 5-(aroylhydrazinocarbonyl)escitalopram as cholinesterase inhibitors.
AID31771Inhibitory concentration against acetylcholinesterase from human erythrocytes2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
AID625294Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID399289Inhibition of acetylcholinesterase from nerve tissue of Lymnaea acuminata at 0.23 ug w/v relative to control
AID241106Inhibition of recombinant human AChE2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
AID1820979Inhibition of BuChE (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease.
AID110196Ability to antagonize paraoxon (1.0 mg/kg sc)-induced motor incoordination in mice.1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity.
AID355917Inhibition of electric eel AChE by modified Ellman method2003Journal of natural products, Jun, Volume: 66, Issue:6
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.
AID355918Inhibition of BChE2003Journal of natural products, Jun, Volume: 66, Issue:6
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.
AID1240266Inhibition of BChE (unknown origin) using butyrylthiocholine chloride as substrate at 0.5 mM preincubated for 30 mins before substrate addition measured after 30 mins by Ellman method relative to control2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.
AID654699Inhibition of human erythrocyte AChE assessed as acetylthiocholine iodide hydrolysis after 10 mins preincubation by spectrophotometry2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID491761Inhibition of human whole RBC AChE pretreated for 30 mins by Ellman technique2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
AID1142531Inhibition of BChE (unknown origin) using BCh iodide as substrate preincubated for 15 mins prior to substrate addition measured after 10 mins by Ellman's method2014European journal of medicinal chemistry, Jun-10, Volume: 80Dual inhibition of the α-glucosidase and butyrylcholinesterase studied by molecular field topology analysis.
AID240779Inhibitory concentration against acetylcholinesterase2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.
AID1312276Selectivity ratio, ratio of IC50 for electric eel AChE to equine serum BChE2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).
AID444035Selectivity for human BuChe over electric eel AChE type 6S2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
AID444034Inhibition of electric eel AChE type 6S2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
AID31035Concentration required to inhibit 50% of Acetylcholinesterase obtained from human erythrocytes was determined in vitro1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1695066Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured for 15 mins by Ellman's method relative to control2020RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors.
AID1240263Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate at 0.5 mM preincubated for 30 mins before substrate addition measured after 30 mins by Ellman method relative to control2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.
AID1312275Selectivity ratio, ratio of IC50 for equine serum BChE to electric eel AChE2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).
AID130103Minimal dose to produce side effects was determined for diarrhea in mice1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
AID1377835Inhibition of electric eel AChE at 0.5 mM using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by Ellman's method relative to control2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of novel 5-(aroylhydrazinocarbonyl)escitalopram as cholinesterase inhibitors.
AID242939Ratio of IC50 for human BuChE and AChE2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
AID1313250Binding affinity to AChE in human assessed as enzyme reactivation half life at 1.5 mg/kg, iv dosed over 60 mins infusion2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
AID1185422Inhibition of electric eel AChE assessed as stability constant of inhibitor-enzyme complex pre-incubated for 2 to 20 mins by enzyme kinetic assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1389195Inhibition of AChE (unknown origin)2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.
AID692822Inhibition of Electric eel AChE using acetylthiocholine as substrate after 2 mins2012ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11
Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.
AID31013In vitro inhibition of Acetylcholinesterase from human erythrocytes1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.
AID1308877Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 30 mins by Ellman's microplate assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Natural cholinesterase inhibitors from Myristica cinnamomea King.
AID262757Selectivity for BChE over AChE2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID44457Inhibitory activity against Butyrylcholinesterase in plasma1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
AID1820943Inhibition of AChE (unknown origin)2022European journal of medicinal chemistry, Feb-05, Volume: 229Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease.
AID32279In vitro inhibitory activity against acetylcholinesterase1992Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.
AID27142Compound was evaluated for equilibrium constant2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID114803Compound was evaluated for the cholinergic activity in vivo in mice, by administering the compound intraperitoneally and observation of the salivation was made after 30 min.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID654700Mixed type inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate by Lineweaver-Burk double-reciprocal-plot and dixon plot analysis2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.
AID282008Inhibition of human recombinant BChE2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
AID1615707Inhibition of electric eel AChE incubated for 15 mins by Ellman's method2019Journal of natural products, 09-27, Volume: 82, Issue:9
Cholinesterase Inhibitory Arisugacins L-Q from a
AID31504Inhibitory activity against Acetylcholinesterase in erythrocyte1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
AID139927Percent change in brain Acetylcholine content in the mouse brain using GC/MS methodology.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID1916836Inhibition of BChE (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
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.
AID229262Ratio of IC50 for BuChE to AChE1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
AID127611Minimal dose to produce side effects was determined for tremor in mice1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
AID465960Inhibition of rat plasma BChE by Ellman's method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
AID1807567Selectivity index, ratio of IC50 for human AChE to IC50 for human BuChe2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID14400Biodistribution in rat superior coliculus, expressed as percent I.D./g tissue1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
AID444042Inhibition of BuChE in human liver microsomes assessed as dissociation constant for Michaelis complex formation by enzyme kinetic study2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
AID141321Binding affinity against mouse muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID1853195Inhibition of human acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies.
AID464988Selectivity ratio of IC50 for mouse serum BChE over IC50 for mouse brain AChE2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID230415It is the ratio of IC50 for butyrl cholinesterase (BuChE ) to that of acetylcholinesterase (AChE)1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.
AID44437Butyrylcholinesterase1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
AID44581Ratio of IC50 values obtained for BChE/ AChE1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID1290213Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as carbamoylation rate of inhibitor from reversible enzyme inhibitor complex to carbamoylated enzyme using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins foll2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
AID235621Therapeutic index is the ratio of LD50 to ED501990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hemicholinium-3 congeners as potential antagonists to organophosphate-induced toxicity.
AID241692Inhibitory concentration against human erythrocyte Acetylcholinesterase2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
AID194873Effect after an intraperitoneal dose of 1 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID44452Compound was evaluated for the in vitro inhibition of the Butyrylcholinesterase from horse serum1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.
AID44451Ratio of IC50(BChE-I) to IC50(AChE-I)1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID44423Inhibition of Butyrylcholinesterase (BChE) of human erythrocytes [-log IC50 (uM)]1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
AID31782In vitro inhibitory concentration against acetylcholinesterase (AChE) obtained from mouse brain homogenate.1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine and related derivatives.
AID1143297Inhibition of electric eel AChE by Ellman's method2014European journal of medicinal chemistry, Jun-23, Volume: 81Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
AID1916835Inhibition of AChE (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
AID672240Inhibition of AChE in Wistar rat brain homogenate using acetylthiocholine iodide as substrate after 0.5 hrs by Ellman's method2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities.
AID1570277Inhibition of BuChE (unknown origin) using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by Ellman's method2019European journal of medicinal chemistry, Oct-15, Volume: 180Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.
AID672241Inhibition of BuChE in Wistar rat plasma using acetylthiocholine iodide as substrate after 0.5 hrs by Ellman's method2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities.
AID1143303Binding affinity to equine serum BChE assessed as compound-enzyme complex stability2014European journal of medicinal chemistry, Jun-23, Volume: 81Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID466871Inhibition of electric eel AChE assessed as purple zones of inhibition after 20 mins by TLC bioautography2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Acetylcholinesterase inhibitory pyridine alkaloids of the leaves of Senna multijuga.
AID482623Inhibition of human LAL at 10 uM after 30 mins by fluorescence assay2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann-Pick type C disease therapeutics.
AID386741Inhibition of electric eel AchE by Ellman's method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
AID1807563Inhibition of human AChE using acetylthiocholine as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID262754Anticholinesterase activity against human erythrocyte AChE2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID660797Inhibition of electric eel AChE using acetylthiocholine as substrate at 350 uM by Ellman's method2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Pyridine alkaloids from Senna multijuga as acetylcholinesterase inhibitors.
AID276345Inhibition of AChE2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID31775Inhibition of acetylcholinesterase (AChE) of human erythrocytes1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
AID79858Ability to reverse the D-tubocurarine-induced neuromuscular blockade in guinea pig left atrium2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID44292Inhibition of human Butyrylcholinesterase1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.
AID1143298Selectivity ratio of IC50 for Electrophorus electricus acetylcholinesterase to IC50 for equine serum butyrylcholinesterase2014European journal of medicinal chemistry, Jun-23, Volume: 81Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
AID1308870Selectivity index, ratio of IC50 for equine serum BChE to IC50 for AChE (unknown origin)2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Natural cholinesterase inhibitors from Myristica cinnamomea King.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540235Phospholipidosis-negative literature compound
AID26934Compound was evaluated for rate constant (K5)2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
AID672242Selectivity ratio of IC50 for BuChE in Wistar rat plasma to IC50 for AChE in Wistar rat brain homogenate2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID118783Compound was tested for cognitive activity by measuring retention for passive avoidance learning in mice at dose 0.15 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID282011Inhibition of AChE mediated aggregation of amyloid beta relative to control2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1290203Inhibition of equine serum butyrylcholinesterase using butyrylcholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 2.5 mins by Ellman's spectrophotometric method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
AID1153518Inhibition of BChE in horse serum using butyrylthiocholine iodide as substrate after 120 mins by Ellman's method2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Preparation, anticholinesterase activity and molecular docking of new lupane derivatives.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1143296Inhibition of equine serum BChE by Ellman's method2014European journal of medicinal chemistry, Jun-23, Volume: 81Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
AID511766Inhibition of human AChE by Ellmans test2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology.
AID1185413Inhibition of electric eel AChE using ATC iodide substrate by DTNB based assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID44450In vitro inhibition of human butryl cholinesterase.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID1312273Inhibition of electric eel AChE preincubated for 15 mins followed by addition of acetylthiocholine iodide as substrate measured after 30 mins by Ellman's microplate assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).
AID25333Apparent dissociation constant of compound was evaluated; n.d. indicates not determined2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
AID660796Inhibition of electric eel AChE assessed as minimum concentration required to inhibit enzyme activity after 20 mins by TLC bioautographic assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Pyridine alkaloids from Senna multijuga as acetylcholinesterase inhibitors.
AID465959Inhibition of rat brain AChE by Ellman's method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
AID465033Selectivity ratio of IC50 for mouse serum BChE over IC50 for mouse brain AChE2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID194869Effect after an intraperitoneal dose of 0.01 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID1807565Inhibition of human BuChE at 100 uM using butyrylthiocholine chloride as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID241560Inhibitory concentration against human plasma Butyrylcholinesterase2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
AID1185421Inhibition of equine serum BChE assessed as rate constant of carbamoyl-enzyme formation pre-incubated for 2 to 20 mins by enzyme kinetic assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID462836Selectivity ratio of IC50 for equine serum BChE to IC50 for bovine AChE2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
AID30685Concentration required to inhibit hydrolytic activity of Acetylcholinesterase by 50%1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity.
AID32108Inhibitory concentration against rat brain acetylcholinesterase AChE1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.
AID1377834Inhibition of equine serum BCHE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by Ellman's method2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of novel 5-(aroylhydrazinocarbonyl)escitalopram as cholinesterase inhibitors.
AID386742Selectivity ratio of IC50 for electric eel AchE to IC50 for human plasma BuchE2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
AID692823Inhibition of equine serum BChE using acetylthiocholine as substrate after 2 mins2012ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11
Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.
AID1657596Inhibition of human BuChE using butyrylthiocholine iodide as substrate measured for 1 min by spectrophotometric based Ellman's method2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID44420Anticholinesterase activity and the bimolecular rate constant was determined from the inhibition of butyrylcholinesterase purified from human serum1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
AID654839Mixed type inhibition of equine BChE using butyrylthiocholine iodide as substrate by Lineweaver-Burk double-reciprocal-plot and dixon plot analysis2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.
AID240567Inhibitory activity towards acetylcholine esterase (AChE)2004Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20
Efficient method for high-throughput virtual screening based on flexible docking: discovery of novel acetylcholinesterase inhibitors.
AID692824Selectivity ratio of IC50 for Electric eel AChE to IC50 for equine serum BChE2012ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11
Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.
AID31637Selectivity towards acetylcholinesterase over butyrylcholinesterase2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
AID31627Inhibition against Acetylcholinesterase (AChE)1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
A comparative molecular field analysis study of N-benzylpiperidines as acetylcholinesterase inhibitors.
AID1615701Induction of paralysis in AB/TU zebra fish at 100 uM treated at 7 hpf and measured after 72 hrs2019Journal of natural products, 09-27, Volume: 82, Issue:9
Cholinesterase Inhibitory Arisugacins L-Q from a
AID26933Compound was evaluated for rate constant (K3)2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
AID116900Compound was evaluated for the cholinergic activity by the induction of amnesia at high toxic doses and lethal dose was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID227700Anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID31768Inhibitory activity against acetylcholinesterase in human erythrocytes2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID31613Kc is compound-acetylcholinesterase complex constant2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
AID117516Ability to antagonize paraoxon-induced lethality in mice.(umol/kg required to protect 50% of the mice for 24 h versus a LD99 dose of paraoxon)1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity.
AID654701Inhibition of equine BChE assessed as butyrylthiocholine iodide hydrolysis after 10 mins preincubation by spectrophotometry2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.
AID1308869Inhibition of equine serum BChE using S-butyrylthiocholine chloride as substrate incubated for 30 mins by Ellman's microplate assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Natural cholinesterase inhibitors from Myristica cinnamomea King.
AID1185414Inhibition of equine serum BChE using ATC iodide substrate by DTNB based assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID1657516Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine as substrate preincubated for 30 mins followed by substrate addition and measured after 2 mins by Ellman's method
AID1377833Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by Ellman's method2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis of novel 5-(aroylhydrazinocarbonyl)escitalopram as cholinesterase inhibitors.
AID1312274Inhibition of equine serum BChE preincubated for 15 mins followed by addition of S-butyrylthiocholine chloride as substrate measured after 30 mins by Ellman's microplate assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).
AID140930Ratio of IC50 (muscarinic acetylcholine receptor M2) to IC50 (muscarinic acetylcholine receptor M1)1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID1529186Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID44277In vitro inhibition of human serum Butyrylcholinesterase.2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
AID142661Selectivity was defined as the ratio between M2-IC50/M1-IC501992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID496772Modulation of neurological behavior in zebrafish assessed as effect on touch response by high-throughput screening2010Nature chemical biology, Mar, Volume: 6, Issue:3
Rapid behavior-based identification of neuroactive small molecules in the zebrafish.
AID127609Minimal dose to produce side effects was determined for salivation in mice1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
AID1153516Inhibition of Pacific electric ray AChE using acetylthiocholine iodide as substrate after 60 mins by Ellman's method2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Preparation, anticholinesterase activity and molecular docking of new lupane derivatives.
AID1185423Inhibition of equine serum BChE assessed as stability constant of inhibitor-enzyme complex pre-incubated for 2 to 20 mins by enzyme kinetic assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID30541Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in electric eel1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.
AID1657594Inhibition of human AChE using acetylthiocholine iodide as substrate measured for 1 min by spectrophotometric based Ellman's method2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID462834Inhibition of equine serum BChE by Ellman's method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
AID31964In vitro inhibitory effect on rat Acetylcholinesterase1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation.
AID781325pKa (acid-base dissociation constant) as determined by Liao ref: J Chem Info Model 20092014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1185420Inhibition of electric eel AChE assessed as rate constant of carbamoyl-enzyme formation pre-incubated for 2 to 20 mins by enzyme kinetic assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID1240265Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 30 mins before substrate addition measured after 30 mins by Ellman method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.
AID1529185Protein binding in human serum albumin after 4.5 hrs by LC-MS based rapid equilibrium dialysis method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID462833Inhibition of bovine AChE by Elman's method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
AID464987Inhibition of mouse serum BChE after 1 hr by modified Ellman's colorimetric method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.
AID361189Inhibition of horse BChE2001Journal of natural products, Jun, Volume: 64, Issue:6
Steroidal alkaloids from the leaves of Sarcococca coriacea of Nepalese origin.
AID692829Time dependent inhibition of equine serum BChE assessed as stability constants of inhibitor-enzyme complex using acetylthiocholine as substrate after 60 mins2012ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11
Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.
AID31503Inhibitory activity against Acetylcholinesterase in cortex1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
AID44445Inhibition of isolated Butyrylcholinesterase (BuChE )1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.
AID130225Evaluated for the percentage change from control in mouse brain ACh concentrations1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID230724Ratio of the IC50 values of BuChE and AcHe1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.
AID32109Inhibitory dose for anticholinesterase activity by ex vivo determination in rat forebrain after intraperitoneal administration1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID758230Inhibition of acetylcholinesterase (unknown origin) using acetylcholine iodide as substrate preincubated for 15 mins prior to substrate addition by spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
New bioactive dihydrofuranocoumarins from the roots of the Tunisian Ferula lutea (Poir.) Maire.
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID14401Biodistribution in rat thalamus, expressed as percent I.D./g tissue1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
AID1123609Inhibition of acetylcholine esterase in chicken biventer cervicis muscle assessed as rate of acetylcholine hydrolysis by Ellman's method1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Actions of two dopamine derivatives at adreno- and cholinoceptors.
AID1529184Protein binding in immobilized human serum albumin by HPLC analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1742993Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method2020European journal of medicinal chemistry, Nov-15, Volume: 206Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies.
AID231128Ratio of the inhibitory concentrations against BuChE and AChE1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.
AID140901Antagonistic potency against Muscarinic acetylcholine receptor M1; nd= Not determined1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1308871Selectivity index, ratio of IC50 for AChE (unknown origin) to IC50 for equine serum BChE2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Natural cholinesterase inhibitors from Myristica cinnamomea King.
AID32720Inhibition acetylcholinesterase (AChE) enzyme.1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.
AID31781Inhibitory activity against acetylcholinesterase1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
AID1240268Inhibition of BChE (unknown origin) using butyrylthiocholine chloride as substrate preincubated for 30 mins before substrate addition measured after 30 mins by Ellman method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.
AID30660Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in Torpedo californica1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.
AID44584Ratio of inhibitory concentration against butyrylcholinesterase to that of acetylcholinesterase1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine and related derivatives.
AID142802Inhibition of [3H]N-methylscopolamine to rat muscarinic acetylcholine receptor M2 from heart tissue1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID1657598Effective permeability of the compound at pH 7.4 at 100 uM measured after 3 to 6 hrs by PAMPA assay2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID234907The relative potency was evaluated1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity.
AID194872Effect after an intraperitoneal dose of 0.30 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1290217Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as decarbamoylation rate using butyrylcholine iodide as substrate preincubated for 1 hr followed by 1000 fold dilution2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
AID44582In vitro inhibitory concentration against butyrylcholinesterase (BuChE) obtained from rat plasma1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine and related derivatives.
AID32110Inhibitory dose for anticholinesterase activity by ex vivo determination in rat salivary gland after intraperitoneal administration1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID444031Inhibition of BuChE in human liver microsomes2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
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.
AID1807564Selectivity index, ratio of IC50 for human BuChe to IC50 for human AChE2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID31021Evaluated for the in vitro inhibition of the Acetylcholinesterase (AChE) from human erythrocytes1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.
AID1682221Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate at 10 mg/ml by Ellman's method relative to control2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID31020In vitro inhibition of human erythrocyte Acetylcholinesterase.2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
AID117061In vitro lethality measured at 24 hours in mice following intraperitoneal administration1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogues.
AID142248Antagonistic potency of compound towards Muscarinic acetylcholine receptor M2 in guinea pig left atrium.2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1615705Inhibition of electric eel AChE at 50 uM incubated for 15 mins by Ellman's method relative to control2019Journal of natural products, 09-27, Volume: 82, Issue:9
Cholinesterase Inhibitory Arisugacins L-Q from a
AID44580The compound was evaluated for the inhibition human of Butyrylcholinesterase1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID44275Anticholinesterase activity against plasma Butyrylcholinesterase (BChE) in humans.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
AID44421Inhibitory activity against butyrylcholinesterase (BChE) in human erythrocyte2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
AID141427Compound was evaluated for the competitive inhibition of [3H]pirenzepine binding to muscarinic acetylcholine receptor M1 of mouse cerebral cortex1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID276347Selectivity for AChE over BChE2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID139720Approximate lethal dose in mice.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID194870Effect after an intraperitoneal dose of 0.03 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID114805Compound was evaluated for the cholinergic activity in vivo in mice by administering the compound intraperitoneally and observation of the tremors was made after 30 min.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID183622Concentration required to potentiate the contraction of isolated rat ileum produced by 1*10e-7 M ACh by 20 percent1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
AID32107Inhibition of rat acetylcholinesterase (AChE)1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID252039Inhibition of human AChE induced beta-amyloid aggregation in thioflavin T-based fluorometric assay2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
AID465961Selectivity ratio of IC50 for rat plasma BChE to IC50 for rat brain AChE2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
AID31496Inhibitory activity against Acetylcholinesterase1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors.
AID44301Inhibition of anticholinesterase activity by their ability to inactivate human serum butyrylcholinesterase1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID31023Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in human erythrocytes1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.
AID465032Inhibition of mouse serum BChE after 1 hr by modified Ellman's colorimetric method2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID118784Compound was tested for cognitive activity by measuring retention for passive avoidance learning in mice at dose 0.32 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID31174In vitro inhibitory activity against human acetylcholinesterase1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
AID31501In vitro inhibition of human erythrocyte acetylcholinesterase.2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.
AID44284Concentration required to inhibit 50% of Butyrylcholinesterase obtained from human serum was determined in vitro1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.
AID118800Compound was tested for lethality in mice at a dose 0.63 mg/kg intraperitoneally; L denotes lethal at this dose1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID134750Tested for its ability to protect mice against paraoxon-induced lethality.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hemicholinium-3 congeners as potential antagonists to organophosphate-induced toxicity.
AID692827Time dependent inhibition of Electric eel AChE assessed as stability constants of inhibitor-enzyme complex using acetylthiocholine as substrate after 60 mins2012ACS medicinal chemistry letters, Nov-08, Volume: 3, Issue:11
Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.
AID30679Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in bovine erythrocytes1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.
AID282830Inhibition of human AChE-induced beta amyloid peptide(1-40) aggregation by thioflavin T-based fluorometric assay2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
AID23402In vivo half life of the compound1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.
AID355919Selectivity ratio of IC50 for electric eel AChE to IC50 for BChE2003Journal of natural products, Jun, Volume: 66, Issue:6
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.
AID1143300Inhibition of equine serum BChE at 10 uM by Ellman's method2014European journal of medicinal chemistry, Jun-23, Volume: 81Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
AID142126Antagonistic potency against Muscarinic acetylcholine receptor M2 (1 uM) receptor; nd= Not determined1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
AID491762Inhibition of human plasma BChE pretreated for 30 mins by Ellman technique2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
AID43950Compound was evaluated for its inhibitory concentration against Horse serum Butyrylcholinesterase1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Conformationally restricted carbamate inhibitors of horse serum butyrylcholinesterase.
AID282007Inhibition of human recombinant AChE2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
AID31966Inhibitory activity against acetylcholine esterase (AChE)1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1290215Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as ratio of carbamoylation rate of inhibitor to apparent affinity between enzyme and inhibitor at equilibrium state using p-nitrophenyl butyrate as substrate preincubated for 5 2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
AID122461Compound was evaluated for therapeutic index (LD50 / ED50), in mice1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Structure-activity studies on a potent antagonist to organophosphate-induced toxicity.
AID1290211Pseudo-irreversible inhibition of equine serum butyrylcholinesterase assessed as apparent affinity between enzyme and inhibitor at equilibrium state using p-nitrophenyl butyrate as substrate preincubated for 5 to 40 mins followed by substrate addition by 2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
AID31176In vitro inhibitory activity against human AchE (Acetylcholinesterase)1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogues.
AID30678Compound was evaluated for the inhibition of acetylcholinesterase (AChE) in bovine brain1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1290205Inhibition of human acetylcholinesterase using acetylcholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 2.5 mins by Ellman's spectrophotometric method2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
AID466872Inhibition of electric eel AChE at 350 mM by microplate assay2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Acetylcholinesterase inhibitory pyridine alkaloids of the leaves of Senna multijuga.
AID31638Acetylcholinesterase inhibitory activity is assessed from the rate constant2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
AID1657597Selectivity index, ratio of IC50 for inhibition of human AChE using acetylthiocholine iodide as substrate to inhibition of human BuChE using butyrylthiocholine iodide as substrate2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID423207Inhibition of AChE assessed as white zone of inhibition after 20 mins by TLC bioautography2009Journal of natural products, Apr, Volume: 72, Issue:4
Semisynthesis and biological activity of stemofoline alkaloids.
AID134728Lethal dose was measured at 24 hour in mice following intraperitoneal administration.1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
AID1615706Inhibition of equine serum BChE at 50 uM using S-butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method relative to control2019Journal of natural products, 09-27, Volume: 82, Issue:9
Cholinesterase Inhibitory Arisugacins L-Q from a
AID131547Protecting activity after paraoxon induced toxicity.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hemicholinium-3 congeners as potential antagonists to organophosphate-induced toxicity.
AID1185415Selectivity index, ratio of IC50 for electric eel AChE to IC50 for quine serum BChE2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Cyclic acyl guanidines bearing carbamate moieties allow potent and dirigible cholinesterase inhibition of either acetyl- or butyrylcholinesterase.
AID232610Ratio of IC50 against BuChE to that of AChE2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Acetylcholinesterase inhibitors: SAR and kinetic studies on omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl derivatives.
AID491764Selectivity ratio of IC50 for human whole RBC AChE to IC50 for human plasma BChE2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
AID262755Anticholinesterase activity against human plasma BChE2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID31165In vitro inhibition of human acetylcholinesterase.1992Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
AID282831Inhibition of beta amyloid protein 40 aggregation at 100 uM by thioflavin T-based fluorometric assay2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
AID386739Inhibition of human plasma BuchE by Ellman's method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
AID141204Antagonistic potency against Muscarinic acetylcholine receptor M3 (10 uM); nd= Not determined1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
AID276346Inhibition of BChE2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID30849In vitro inhibitory activity against acetylcholinesterase from electric eel1988Journal of medicinal chemistry, Dec, Volume: 31, Issue:12
Synthesis and anticholinesterase activity of (-)-N1-norphysostigmine, (-)-eseramine, and other N(1)-substituted analogues of (-)-physostigmine.
AID1807566Inhibition of human BuChE using butyrylthiocholine chloride as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347159Primary screen GU Rhodamine 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.
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.
AID1345946Human acetylcholinesterase (Cartwright blood group) (Hydrolases)2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID1345972Human butyrylcholinesterase (Hydrolases)2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5,844)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904013 (68.67)18.7374
1990's957 (16.38)18.2507
2000's485 (8.30)29.6817
2010's330 (5.65)24.3611
2020's59 (1.01)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 70.17

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 Index70.17 (24.57)
Research Supply Index8.78 (2.92)
Research Growth Index4.19 (4.65)
Search Engine Demand Index128.04 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (70.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials252 (4.04%)5.53%
Reviews177 (2.84%)6.00%
Case Studies298 (4.78%)4.05%
Observational2 (0.03%)0.25%
Other5,501 (88.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Acetylcholine, Tobacco Smoking, Genes and Nicotinic Receptors [NCT02008292]80 participants (Actual)Interventional2013-09-30Completed
[NCT01121497]160 participants (Anticipated)Interventional2010-07-31Not yet recruiting
Influence of Physostigmine on Patient-Controlled Analgesia [NCT01394445]Phase 320 participants (Actual)Interventional2011-06-30Completed
The Use of Physostigmine in Elderly Patients in the Postoperative Recovery-phase After General Anesthesia [NCT00850850]50 participants (Anticipated)Interventional2009-12-31Recruiting
Pharmacological Intervention in Insulin Resistance Targeting Autonomic Nerve Activity - a Concept Study in Mani [NCT00689208]Early Phase 112 participants (Anticipated)Interventional2007-05-31Completed
Monocenter, Double Blind, Randomised, Placebo Controlled Study to Evaluate Physostigmine for the Treatment of Delirium in Perioperative Intensive Care Medicine [NCT02216266]Phase 3120 participants (Anticipated)Interventional2014-04-30Recruiting
Anticholium® Per Se a Randomized, Double-blind, Placebo-controlled, Monocentric Trial on the Adjunctive Use of Physostigmine Salicylate (Anticholium®) in Perioperative Sepsis and Septic Shock [NCT03013322]20 participants (Actual)Interventional2015-01-28Completed
Phamacological Reversal of Airway Instability During Sedation [NCT01171118]10 participants (Actual)Interventional2009-08-31Completed
A Randomized Trial Comparing Physostigmine vs Lorazepam for Treatment of Adolescent Antimuscarinic (Anticholinergic) Toxidrome [NCT03090620]Phase 419 participants (Actual)Interventional2017-03-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01171118 (1) [back to overview]AHI - Apnea Hypopnea Index
NCT02008292 (2) [back to overview]Change in Acetylcholine (ACh) Levels After Physostigmine Administration as Confirmed by PET Images.
NCT02008292 (2) [back to overview]Change in Dopamine (DA) Levels After Amphetamine Administration as Confirmed by PET Images.
NCT03090620 (7) [back to overview]Comparison of RASS Score Between Physostigmine and Lorazepam: 4 Hours
NCT03090620 (7) [back to overview]Comparison of RASS Score Between Physostigmine and Lorazepam: After Bolus
NCT03090620 (7) [back to overview]Comparison of RASS Score Between Physostigmine and Lorazepam: Before Bolus
NCT03090620 (7) [back to overview]Comparison of the Effectiveness in Control of Delirium Between Physostigmine and Lorazepam: 4 Hours
NCT03090620 (7) [back to overview]Comparison of the Effectiveness in Control of Delirium Between Physostigmine and Lorazepam: After Bolus
NCT03090620 (7) [back to overview]Comparison of the Effectiveness in Control of Delirium Between Physostigmine and Lorazepam: Before Bolus
NCT03090620 (7) [back to overview]Safety and Effectiveness of Physostigmine Infusion in the Setting of Antimuscarinic Toxidrome.

AHI - Apnea Hypopnea Index

This is a standard metric used to describe severity of disordered breathing during sleep.Normal healthy subjects would have an AHI value of zero during sleep. Mild disordered breathing would correspond to a value of 5 to 10 events per hours; moderate 10-25; severe would be over 25 (NCT01171118)
Timeframe: 2- 2 1/2 hours during study visit

Interventionevents per hour (Mean)
Physostigmine/Oxygen14.5
Placebo/Oxygen27.9
Physostigmine/Room Air11.3
Placebo/Room Air12.1

[back to top]

Change in Acetylcholine (ACh) Levels After Physostigmine Administration as Confirmed by PET Images.

PET images will be obtained in healthy controls and smoker subjects after physostigmine administration. Change in ACh levels will be determined by change in binding potential of Norchloro-fluoro-homoepibatidine (NCFHEB) (NCT02008292)
Timeframe: first 150 minute scan at baseline, second 150 minute scan start 10 minutes post physostigmine administration

Interventionpercentage of change (Mean)
ACH Levels in Healthy Controls After Physostigmine Administration5.9
ACH Levels in Smokers After Physostigmine Administration4.3

[back to top]

Change in Dopamine (DA) Levels After Amphetamine Administration as Confirmed by PET Images.

PET images will be obtained in all subjects after amphetamine administration. Change in DA levels will be determined by change in binding potential of PHNO, a selective dopamine D2 receptor agonist. (NCT02008292)
Timeframe: first 120 min scan at baseline, second 120 scan 2.5 hours after amphetamine administration

Interventionpercentage of change (Mean)
Healthy Controls After Dextroamphetamine26.5
Healthy Smoker After Dextroamphetamine19.6

[back to top]

Comparison of RASS Score Between Physostigmine and Lorazepam: 4 Hours

Determine the effectiveness of physostigmine as compared with lorazepam for control of antimuscarinic agitation. Richmond Agitation Sedation Scores (RASS) will be compared throughout treatment protocol. The Richmond Agitation-Sedation Scale (RASS) measures sedation and agitation. Possible scores range from -5 (unarousable) to 0 (alert & calm) to +4 (combative). Scores closer to 0 indicate a better outcome for this measurement. (NCT03090620)
Timeframe: 4 hours

Interventionscore on a scale (Median)
Physostigmine0
Lorazepam0.25

[back to top]

Comparison of RASS Score Between Physostigmine and Lorazepam: After Bolus

Determine the effectiveness of physostigmine as compared with lorazepam for control of antimuscarinic agitation. Richmond Agitation Sedation Scores (RASS) will be compared throughout treatment protocol. The Richmond Agitation-Sedation Scale (RASS) measures sedation and agitation. Possible scores range from -5 (unarousable) to 0 (alert & calm) to +4 (combative). Scores closer to 0 indicate a better outcome for this measurement. (NCT03090620)
Timeframe: Immediately after bolus, up to 10 minutes post-Baseline

Interventionscore on a scale (Median)
Physostigmine0
Lorazepam1

[back to top]

Comparison of RASS Score Between Physostigmine and Lorazepam: Before Bolus

Determine the effectiveness of physostigmine as compared with lorazepam for control of antimuscarinic agitation. Richmond Agitation Sedation Scores (RASS) will be compared throughout treatment protocol. The Richmond Agitation-Sedation Scale (RASS) measures sedation and agitation. Possible scores range from -5 (unarousable) to 0 (alert & calm) to +4 (combative). Scores closer to 0 indicate a better outcome for this measurement. (NCT03090620)
Timeframe: Baseline, immediately before bolus

Interventionscore on a scale (Median)
Physostigmine1.5
Lorazepam1

[back to top]

Comparison of the Effectiveness in Control of Delirium Between Physostigmine and Lorazepam: 4 Hours

"Determine the effectiveness of physostigmine as compared with lorazepam in the reversal of antimuscarinic delirium. Confusion Assessment Method for the ICU (CAM-ICU) scores will be evaluated throughout the study. This measurement is a dichotomous outcome (yes or no for presence of delirium is indicated rather than a score). The number of participants exhibiting delirium is reported." (NCT03090620)
Timeframe: 4 hours

InterventionParticipants (Count of Participants)
Physostigmine2
Lorazepam10

[back to top]

Comparison of the Effectiveness in Control of Delirium Between Physostigmine and Lorazepam: After Bolus

"Determine the effectiveness of physostigmine as compared with lorazepam in the reversal of antimuscarinic delirium. Confusion Assessment Method for the ICU (CAM-ICU) scores will be evaluated throughout the study. This measurement is a dichotomous outcome (yes or no for presence of delirium is indicated rather than a score). The number of participants exhibiting delirium is reported." (NCT03090620)
Timeframe: Immediately after bolus, up to 10 minutes post-Baseline

InterventionParticipants (Count of Participants)
Physostigmine4
Lorazepam10

[back to top]

Comparison of the Effectiveness in Control of Delirium Between Physostigmine and Lorazepam: Before Bolus

"Determine the effectiveness of physostigmine as compared with lorazepam in the reversal of antimuscarinic delirium. Confusion Assessment Method for the ICU (CAM-ICU) scores will be evaluated throughout the study. This measurement is a dichotomous outcome (yes or no for presence of delirium is indicated rather than a score). The number of participants exhibiting delirium is reported." (NCT03090620)
Timeframe: Baseline, immediately before bolus

InterventionParticipants (Count of Participants)
Physostigmine9
Lorazepam9

[back to top]

Safety and Effectiveness of Physostigmine Infusion in the Setting of Antimuscarinic Toxidrome.

Evaluation of clinical antimuscarinic symptoms, along with presence of any adverse effects, during the infusion to report tolerability, safety profile, and effectiveness of the infusion. the number of participants exhibiting adverse events will be reported, by type. (NCT03090620)
Timeframe: Up to 4 hours

,
InterventionParticipants (Count of Participants)
SeizuresBradycardiaBronchorrheaBronchospasmDiaphoresisIntubationVomitingOversedation
Lorazepam00000011
Physostigmine00000011

[back to top]