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scopolamine hydrobromide

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Description

scopolamine hydrobromide (anhydrous) : A hydrobromide that is obtained by reaction of scopolamine with hydrogen bromide. [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]

Cross-References

ID SourceID
PubMed CID11968014
CHEMBL ID1187846
MeSH IDM0019553
PubMed CID6603108
CHEMBL ID3185877
CHEBI ID61271
SCHEMBL ID40627
MeSH IDM0019553

Synonyms (70)

Synonym
scopolamine ,
51-34-3
isoptpo hyoscine
CHEMBL1187846
bdbm50452855
[(1s,2r,4s,5s)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2s)-3-hydroxy-2-phenylpropanoate
[(1r,2s,4s,5s)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2s)-3-hydroxy-2-phenylpropanoate
STECJAGHUSJQJN-ODICJLLRSA-N
scopos
AC-3389
scopolamine hydrobromide anhydrous
benzeneacetic acid, alpha-(hydroxymethyl)-, (1alpha,2beta,4beta,5alpha,7beta)-9-methyl-3-oxa-9-azatricyclo(3.3.1.02,4)non-7-yl ester, hydrobromide, (alphas)-
1-alpha-h,5-alpha-h-tropan-3-alpha-ol, 6-beta,7-beta-epoxy-, (-)-tropate (ester), hydrobromide
1alphah,5alphah-tropan-3alpha-ol, 6beta,7beta-epoxy-, (-)-tropate (ester), hydrobromide
scopolamine hydrobromide (anhydrous)
einecs 204-050-6
benzeneacetic acid, alpha-(hydroxymethyl)-, 9-methyl-3-oxa-9-azatricyclo(3.3.1.02,4)non-7-yl ester, hydrobromide, (7(s)-(1alpha,2beta,4beta,5alpha,7beta))-
1alphah,5alphah-tropan-3-alpha-ol, 5beta,7beta-epoxy-, (-)-tropate (ester), hydrobromide
nsc 61806
smr000058594
MLS000069527 ,
tox21_302019
dtxcid8012029
dtxsid0032029 ,
cas-114-49-8
NCGC00255166-01
CHEBI:61271 ,
scopolamine bromide (anhydrous)
(-)-hyoscine hydrobromide (anhydrous)
(-)-scopolamine bromide (anhydrous)
scopolaminium bromide (anhydrous)
(1r,2r,4s,5s,7s,9s)-7-{[(2s)-3-hydroxy-2-phenylpropanoyl]oxy}-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.0(2,4)]nonane bromide
(1r,2r,4s,5s,7s)-9-methyl-3-oxa-9-azatricyclo[3.3.1.0(2,4)]non-7-yl (2s)-3-hydroxy-2-phenylpropanoate hydrobromide
(-)-scopolamine hydrobromide (anhydrous)
scopolammonium bromide (anhydrous)
hyoscine bromide (anhydrous)
tox21_110035
NCGC00013722-01
AKOS015965267
r3k67drl3j ,
benzeneacetic acid, alpha-(hydroxymethyl)-, (1alpha,2beta,4beta,5alpha,7beta)-9-methyl-3-oxa-9-azatricyclo(3.3.1.02,4)non-7-yl ester, hydrobromide (1:1), (alphas)-
ec 204-050-6
unii-r3k67drl3j
S2508
hyoscine hydrobromide [who-dd]
6.beta.,7.beta.-epoxy-1.alpha.h,5.alpha.h-tropan-3.alpha.-ol (-)-tropate (ester) hydrobromide
scopolamine hydrobromide [mi]
scopolamine (hydrobromide)
HY-N0296A
CS-2000
SCHEMBL40627
tox21_110035_1
NCGC00024357-07
REGID_FOR_CID_6603108
(?,s)-?-(hydroxymethyl)benzeneacetic acid (1?,2?,4?,5?,7?)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]non-7-yl ester hydrobromide
W-108599
CHEMBL3185877
OPERA_ID_496
scopine hydrobromide
sr-01000597758
SR-01000597758-1
SW199343-2
(-)-scopolamine hydrobromide;hyoscine hydrobromide;scopine hydrobromide
WTGQALLALWYDJH-WYHSTMEOSA-N
AS-35324
Q27130957
CCG-268451
benzeneacetic acid, .alpha.-(hydroxymethyl)-, (1.alpha.,2.beta.,4.beta.,5.alpha.,7.beta.)-9-methyl-3-oxa-9-azatricyclo3.3.1.02,4non-7-yl ester, (.alpha.s)- hydrobromide
A935283
PD087159

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Cycloplegics are very safe and useful medications."( Avoiding adverse effects of cycloplegics in infants and children.
Gray, LG, 1979
)
0.26
" In a double-blind study, the effects and above all the side effects of TTS-scopolamine (TTS-s) and TTS-placebo (TTS-p) were investigated in elderly patients (greater than 50 years), who are particularly susceptible to adverse drug reactions."( [Effects and side effects of transdermal scopolamine for premedication in general anesthesia in elderly patients].
Baumann, S; Heine, C; Hettenbach, A; Tolksdorf, W, 1986
)
0.27
"The oral LD50 for bis(trichloromethyl) sulfone (N-1386 Biocide) in male rats was 691 mg/kg."( Anticholinesterase effect and toxicity of bis(trichloromethyl) sulfone (N-1386 Biocide) in rats.
Castles, TR; Sprague, GL, 1987
)
0.27
" The discussion concerns the recognition and treatment of these adverse effects."( Side effects of transdermal scopolamine.
Wilkinson, JA,
)
0.13
" Prescription of Scopolamine eye drops should be followed by information of possible adverse effects."( Toxic effect of scopolamine eye drops in children.
Hamborg-Petersen, B; Nielsen, MM; Thordal, C, 1984
)
0.27
" These seeds produce various toxic effects and contain mainly the alkaloids scopolamine and hyoscyamine."( Toxicity study of the main alkaloids of Datura ferox in broilers.
Flaskos, J; Kotsaki-Kovatsi, VP; Kovatsis, A; Nikolaidis, E; Papaioannou, N; Tsafaris, F, 1993
)
0.29
" These properties suggest that P10358 may be a safe and promising symptomatic treatment for Alzheimer's disease."( Pharmacological activity and safety profile of P10358, a novel, orally active acetylcholinesterase inhibitor for Alzheimer's disease.
Bores, GM; Brooks, KM; Camacho, F; Cunningham, DM; Davis, L; Fishkin, R; Hartman, HB; Li, M; Petko, W; Roehr, J; Rush, DK; Selk, DE; Smith, CP; Vargas, HM; Winslow, JT, 1997
)
0.3
" 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
)
0.3
"The combined use of scopolamine, naltrexone and naloxone is a rapid, safe and effective detoxification treatment protocol for heroin addicts."( [The combined use of scopolamine, naltrexone and naloxone as a rapid, safe and effective detoxification treatment for heroin addicts].
Xu, K; Yang, G; Zhou, W, 1999
)
0.3
" 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
" Strict time requirements for review of incoming adverse drug reaction reports and close involvement of the highly skilled national drug regulatory laboratory resulted in early identification of the cause of the outbreak and led in turn to the identification of malpractice by the contract manufacturer."( Widespread hyoscine hydrobromide toxicity due to contract manufacturer malpractice : the travacalm episode.
Kelly, LF; Krauss, AS; McEwen, J; Purcell, PM; Thompson, BR, 2007
)
0.34
"Plasma scopolamine concentrations, physiologic (heart rate and blood pressure), visual, and cognitive function parameters, and adverse effects were assessed before the first session (baseline) and after each 24-hour session."( Safety of double-dose transdermal scopolamine.
Bar, R; Gil, A; Tal, D, 2009
)
0.35
"Double-dose transdermal scopolamine may improve treatment in patients who fail to respond to a single patch by increasing the plasma scopolamine concentration, without aggravating systemic, visual, or cognitive adverse effects."( Safety of double-dose transdermal scopolamine.
Bar, R; Gil, A; Tal, D, 2009
)
0.35
" However, dose-limiting adverse effects restrict its tolerability and clinical outcomes."( Peripheral cholinoceptor antagonist anisodamine counteracts cholinergic adverse effects and facilitates cognitive amelioration of rivastigmine.
Chen, HZ; Cui, YY; Li, J; Shao, BY; Song, MK; Wang, H; Xia, Z; Xu, ZP; Zhang, WW, 2009
)
0.35
" These alkaloids can be very toxic at high dose."( Atropa belladonna neurotoxicity: Implications to neurological disorders.
Aschner, M; Jiménez, J; Jiménez, JA; Kwakye, GF, 2018
)
0.48
" No adverse effects were reported."( Efficacy and safety of oral hyoscine used for outpatient cervical ripening among primiparous women with term pregnancy.
Mirzamoradi, M; Moridi, A; Naeiji, Z; Naghshvarian, N; Sotudeh, S, 2020
)
0.56
"Administration of oral hyoscine in an outpatient setting was found to ripen the cervix with no clinically significant adverse drug reaction."( Efficacy and safety of oral hyoscine used for outpatient cervical ripening among primiparous women with term pregnancy.
Mirzamoradi, M; Moridi, A; Naeiji, Z; Naghshvarian, N; Sotudeh, S, 2020
)
0.56
" Trial findings will contribute to the evidence base regarding the cholinergic hypothesis of mood disorders and specifically might result in an additional safe therapeutic option for the management of depressive episodes in bipolar disorder."( Efficacy and safety of scopolamine compared to placebo in individuals with bipolar disorder who are experiencing a depressive episode (SCOPE-BD): study protocol for a randomised double-blind placebo-controlled trial.
Cannon, DM; Hallahan, B; Kane, R; McDonald, C; McMahon, E; Miravalles, C, 2022
)
0.72
" Hemodynamic changes, adverse events, and discomfort levels of patients were similar between the two groups."( Antiperistaltic effect and safety of L-menthol for esophagogastroduodenoscopy in the elderly with contraindication to hyoscine-N-butylbromide.
Chen, LK; Chen, PH; Hou, MC; Huang, YH; Lin, MH; Peng, LN; Yang, TC, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
"Plasma hyoscine and morphine levels and various pharmacodynamic responses have been examined in seven patients scheduled for a coronary-artery bypass graft."( Pharmacokinetics and clinical response of hyoscine plus morphine premedication in connection with cardiopulmonary bypass surgery.
Arola, M; Kaila, T; Kanto, J; Kentala, E; Mattila, M, 1991
)
0.28
"Several specific and sensitive new methods for determining atropine and its metabolites in biological fluids have increased the possibility to characterise the pharmacokinetic properties of this antimuscarinic agent."( Pharmacokinetic implications for the clinical use of atropine, scopolamine and glycopyrrolate.
Kanto, J; Klotz, U, 1988
)
0.27
" After intravenous (N = 4) the drug fast disappeared from the circulation with a half-life of about 5 min."( Pharmacokinetics and clinical effects of scopolamine in caesarean section patients.
Kanto, JH; Oksman-Caldentey, KM; Pihlajamäki, KK, 1986
)
0.27
" Pharmacokinetic studies indicate that this new method for administering hyoscine controls the absorption process and the rate of drug entry into the systemic circulation over an extended period (72 hours), providing a means of delivery which is similar to a slow intravenous infusion."( Transdermal hyoscine (Scopolamine). A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Clissold, SP; Heel, RC, 1985
)
0.27
"The pharmacokinetics and some pharmacodynamic properties of atropine, glycopyrrolate and scopolamine are reviewed."( Pharmacokinetics and related pharmacodynamics of anticholinergic drugs.
Ali-Melkkilä, T; Iisalo, E; Kanto, J, 1993
)
0.29
"The effects of subcutaneously administered scopolamine on quantitative electroencephalogram (qEEG) and cognitive performance were evaluated and correlated with pharmacokinetic parameters in a randomized, double-blind placebo-controlled crossover study of 10 healthy male volunteers."( Pharmacokinetics and pharmacodynamics of scopolamine after subcutaneous administration.
Ebert, U; Kirch, W; Oertel, R; Siepmann, M; Wesnes, KA, 1998
)
0.3
" The Cmax value (6."( Influence of grapefruit juice on scopolamine pharmacokinetics and pharmacodynamics in healthy male and female subjects.
Ebert, U; Kirch, W; Oertel, R, 2000
)
0.31
" The objective of the study was to relate pharmacodynamic electroencephalogram (EEG) changes and scopolamine serum concentration using pharmacokinetic-pharmacodynamic (PK-PD) modeling techniques."( Pharmacokinetic-pharmacodynamic modeling of the electroencephalogram effects of scopolamine in healthy volunteers.
Ebert, U; Gramatté, T; Grossmann, M; Kirch, W; Oertel, R, 2001
)
0.31
" Characterization of the pharmacokinetic and/or pharmacodynamic behavior of operationally critical medications is crucial for their effective use in flight; as a first step, we sought to determine whether drugs administered in space actually reach the site of action at concentrations sufficient to elicit the therapeutic response."( Pharmacokinetic consequences of spaceflight.
Cintrón, NM; Putcha, L, 1991
)
0.28
" The plasma drug concentration versus time data were linked to the response versus time data using a signal transduction pharmacodynamic model that was fitted simultaneously to all four experimental data sets."( A signal transduction pharmacodynamic model of the kinetics of the parasympathomimetic activity of low-dose scopolamine and atropine in rats.
Hoffman, A; Krzyzanski, W; Perlstein, I; Stepensky, D, 2002
)
0.31
"High inter-individual variability was observed in all pharmacokinetic parameters."( Pharmacokinetics of scopolamine in serum and subcutaneous adipose tissue in healthy volunteers.
Joukhadar, C; Kirch, W; Kulemann, V; Madai, B; Stetina, PM, 2005
)
0.33
" Recently, pharmacokinetic data on scopolamine in different biozlogic matrices were obtained most efficiently using liquid chromatographic-tandem mass spectrometric (LC-MS/MS) or gas chromatography online coupled to mass spectrometry."( Pharmacokinetics and pharmacodynamics in clinical use of scopolamine.
Kirch, W; Oertel, R; Renner, UD, 2005
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The pharmacodynamic performances of the nanoparticles (NPs) were evaluated for brain targeting and memory improvement in scopolamine-induced amnesic mice using Morris Water Maze Test."( Rivastigmine-loaded PLGA and PBCA nanoparticles: preparation, optimization, characterization, in vitro and pharmacodynamic studies.
Chavhan, SS; Joshi, SA; Sawant, KK, 2010
)
0.36
"Drug development is a high-risk and high failure enterprise, and studies that provide an early read on the pharmacodynamic activity of novel compounds could save time and money, increasing the efficiency of the drug development process."( The scopolamine model as a pharmacodynamic marker in early drug development.
Abi-Saab, W; Baker, JD; Lenz, RA; Locke, C; Mohler, EG; Rueter, LE; Saltarelli, MD; Wesnes, K, 2012
)
0.38
"Preclinical and clinical experiments were designed to examine the utility of the scopolamine-induced cognitive impairment model in predicting pharmacodynamic signals of putatively procognitive compounds, utilizing the acetylcholinesterase inhibitor donepezil for illustration."( The scopolamine model as a pharmacodynamic marker in early drug development.
Abi-Saab, W; Baker, JD; Lenz, RA; Locke, C; Mohler, EG; Rueter, LE; Saltarelli, MD; Wesnes, K, 2012
)
0.38
"These findings suggest that reversal of scopolamine-induced cognitive impairment is a viable model for predicting pharmacodynamic signals of procognitive compounds in both animals and humans."( The scopolamine model as a pharmacodynamic marker in early drug development.
Abi-Saab, W; Baker, JD; Lenz, RA; Locke, C; Mohler, EG; Rueter, LE; Saltarelli, MD; Wesnes, K, 2012
)
0.38
" Plasma concentration of scopolamine hydrobromide was determined by LC-MS/MS and pharmacokinetic parameters were calculated."( [Pharmacokinetics of scopolamine hydrobromide oral disintegrative microencapsule tablets in Beagle dogs determined with LC-MS/MS].
Hu, JH; Liu, DD; Shi, LF; Xia, T, 2011
)
0.37
" Clinical phenomena suggested that the changes of substituent group were related to the pharmacokinetic and pharmacodynamic characteristics of the agents."( Comparative study on pharmacokinetics of a series of anticholinergics, atropine, anisodamine, anisodine, scopolamine and tiotropium in rats.
Chen, X; Li, C; Li, N; Liu, Q; Lu, Y; Ren, S; Tian, F; Wang, X; Zhao, D; Zhou, S, 2015
)
0.42
"The purpose of this study was to investigate the microdialysis pharmacokinetic of scopolamine in plasma, olfactory bulb and vestibule after intranasal administration."( Microdialysis pharmacokinetic study of scopolamine in plasma, olfactory bulb and vestibule after intranasal administration.
Cao, S; Jiang, X; Wang, F; Wang, Y; Wei, Y; Xu, S; Ying, M; Zou, A, 2016
)
0.43
" The pharmacokinetic parameters revealed areas under the curve of 22."( Simultaneous determination of atropine, scopolamine, and anisodamine from Hyoscyamus niger L. in rat plasma by high-performance liquid chromatography with tandem mass spectrometry and its application to a pharmacokinetics study.
Deng, X; Li, Y; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P; Zhou, Y, 2014
)
0.4
" Results indicate dose-linear pharmacokinetics of scopolamine with linear increases in Cmax and AUC within the dose range tested."( Dose escalation pharmacokinetics of intranasal scopolamine gel formulation.
Boyd, JL; Chow, DS; Daniels, V; Putcha, L; Wang, Z; Wu, L, 2015
)
0.42
" The elimination half-life (T1/2) was 14."( Pharmacokinetics and pharmacodynamics of a novel Acetylcholinesterase Inhibitor, DMNG-3.
Guo-Di, M; Kou, F; Tang, P; Xin-Guo, Z; Zhong-Duo, Y, 2016
)
0.43
"The present investigation was carried out to improve the galantamine bioavailability in brain by intranasal drug delivery through thiolated chitosan nanoparticles and compared to nasal and oral delivery of its solution using pharmacodynamic activity as well as biochemical estimation."( Nose to Brain Delivery of Galantamine Loaded Nanoparticles: In-vivo Pharmacodynamic and Biochemical Study in Mice.
Mishra, DN; Singh, SK, 2019
)
0.51
"05) as compared to oral and nasal administration of its solution, by pharmacodynamic study and biochemical estimation of acetylcholinesterase activity in Swiss albino mice brain."( Nose to Brain Delivery of Galantamine Loaded Nanoparticles: In-vivo Pharmacodynamic and Biochemical Study in Mice.
Mishra, DN; Singh, SK, 2019
)
0.51
" In the pharmacokinetic analysis, a pattern recognition analysis method was used to investigate the pharmacokinetics of the absorbed compounds in blood."( Neuroprotective Effects of Red Ginseng Saponins in Scopolamine-Treated Rats and Activity Screening Based on Pharmacokinetics.
Chen, J; Li, M; Qu, D; Sun, Y, 2019
)
0.51
" Therefore, the present study attempts to evaluate the pharmacokinetic and pharmacodynamic properties of nasal liposomal and PLGA nanoparticle formulations of rivastigmine in acute scopolamine-induced amnesia and chronic colchicine induced cognitive dysfunction animal models, and validate the best formulation by employing pharmacokinetic and pharmacodynamic (PK-PD) modeling."( Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer's disease.
Arumugam, K; Bojja, SL; Kumar, N; Rao, CM; Rompicherla, SKL, 2021
)
0.62
" Commercially available transdermal patches, such as Scopoderm (Novartis Consumer Health UK), offer an opportunity to test these experimental approaches as systemic pharmacokinetic data are available with which to validate a predictive model."( Skin Pharmacokinetics of Transdermal Scopolamine: Measurements and Modeling.
Bunge, AL; Delgado-Charro, MB; Guy, RH; Hattam, L; McGrogan, A; Pensado, A; White, KAJ, 2021
)
0.62
" However, the usual transdermal injection of bee venom poses many pharmacokinetic disadvantages."( Pharmacokinetic improvement provided by microneedle patch in delivering bee venom, a case study in combating scopolamine-induced neurodegeneration in mouse model.
An, EJ; Jeong, DH; Kim, JH; Lee, G; Nguyen, CD; Park, SY; Sung, CY; Yoo, J, 2022
)
0.72
" In pharmacodynamic studies, the efficacy of NE administered via the IN route was higher when compared with other groups in neurobehavioral, biochemical estimation, and gene expression studies."( Simultaneous Intranasal Codelivery of Donepezil and Memantine in a Nanocolloidal Carrier: Optimization, Pharmacokinetics, and Pharmacodynamics Studies.
Bhatta, RS; Handa, M; Palkhade, R; Patil, GP; Sanap, SN; Shukla, R; Singh, DP, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"3 mg) alone or combined with ephedrine (25 mg) was tested for its effectiveness in the prevention of seasickness during 24 h at sea and of motion sickness in rotating chair tests in a laboratory."( Drug treatment of motion sickness: scopolamine alone and combined with ephedrine in real and simulated situations.
Aho, J; Gothoni, G; Laitinen, LA; Tokola, O; Vapaatalo, H, 1984
)
0.27
" Scopolamine alone or in combination with ephedrine proved useful in the prevention of seasickness in young healthy male volunteers."( Scopolamine alone or combined with ephedrine in seasickness: a double-blind, placebo-controlled study.
Gothoni, G; Laitinen, LA; Tokola, O; Vapaatalo, H, 1981
)
0.26
" The present study compared behavioral sensitization and drug conditioning between treatments with M combined with scopolamine (S) and M alone with respect to a reciprocal balance between the dopaminergic and inhibitory cholinergic systems in rats."( Behavioral responses induced by repeated treatment with methamphetamine alone and in combination with scopolamine in rats.
Miura, T; Yui, K, 1996
)
0.29
" The antiemetic efficacy of NK1 receptor antagonists against chemotherapy-induced emesis is, however, enhanced when combined with a 5-HT3 receptor antagonist."( Comparison of the neurokinin-1 antagonist GR205171, alone and in combination with the 5-HT3 antagonist ondansetron, hyoscine and placebo in the prevention of motion-induced nausea in man.
Clemes, SA; House, F; Palmer, JL; Reid, K; Somal, HS; Stott, JR; Troakes, C; Wright, RJ, 2000
)
0.31
"The enhancement of NK1 receptor antagonist antiemetic activity through combination with a 5-HT3 receptor antagonist is not replicated in motion-induced nausea."( Comparison of the neurokinin-1 antagonist GR205171, alone and in combination with the 5-HT3 antagonist ondansetron, hyoscine and placebo in the prevention of motion-induced nausea in man.
Clemes, SA; House, F; Palmer, JL; Reid, K; Somal, HS; Stott, JR; Troakes, C; Wright, RJ, 2000
)
0.31
"32-10 mg/kg) was administered with scopolamine (0."( Effects of the cannabinoid ligand SR 141716A alone or in combination with delta9-tetrahydrocannabinol or scopolamine on learning in squirrel monkeys.
Moerschbaecher, JM; Nakamura-Palacios, EM; Winsauer, PJ, 2000
)
0.31

Bioavailability

ExcerptReferenceRelevance
"005 mg/kg intramuscular injection (deltoid muscle), a very fast rate of absorption was found with mean peak serum concentrations occurring after only 10 min (n = 6)."( Pharmacokinetics of scopolamine during caesarean section: relationship between serum concentration and effect.
Kaila, T; Kanto, J; Kentala, E; Pihlajamäki, K, 1989
)
0.28
" Compared to the oral route, losses in bioavailability due to first-pass liver metabolism are reduced."( Transdermal delivery of drugs.
Brown, L; Langer, R, 1988
)
0.27
" or oral atropine administration, typical anticholinergic effects coincide quite well with the absorption rate of the drug, indicating that the premedication should be given about 1 and 2 h before induction of anaesthesia."( Pharmacokinetic implications for the clinical use of atropine, scopolamine and glycopyrrolate.
Kanto, J; Klotz, U, 1988
)
0.27
"6 beta,7 beta-Epoxy-3a(1aH,5aH)-tropanyl-(S)-tropate (scopolamine) has proved to be a very effective drug in the prevention of motion sickness, however, the drug has a small therapeutic window, a low bioavailability and a short half-life."( Development and application of a radioreceptor assay for scopolamine.
de Zeeuw, RA; Ensing, GJ; Ensing, K; Halma, P; in 't Hout, WG; Klinkers, HM, 1988
)
0.27
"The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers."( Bioavailability of intranasal scopolamine in normal subjects.
Bourne, DW; Cintrón, NM; Hunter, RP; Parise, CM; Putcha, L; Tietze, KJ, 1996
)
0.29
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"To investigate the effects of grapefruit juice on absolute bioavailability of scopolamine in healthy subjects and to evaluate differences in pharmacokinetics and pharmacodynamics between genders."( Influence of grapefruit juice on scopolamine pharmacokinetics and pharmacodynamics in healthy male and female subjects.
Ebert, U; Kirch, W; Oertel, R, 2000
)
0.31
"Pretreatment with grapefruit juice delayed the absorption and increased the bioavailability of scopolamine, whereas elimination was not significantly affected."( Influence of grapefruit juice on scopolamine pharmacokinetics and pharmacodynamics in healthy male and female subjects.
Ebert, U; Kirch, W; Oertel, R, 2000
)
0.31
" That spaceflight may alter bioavailability was proposed when drugs prescribed to alleviate space motion sickness (SMS) had little therapeutic effect."( Pharmacokinetic consequences of spaceflight.
Cintrón, NM; Putcha, L, 1991
)
0.28
" Scopolamine has a limited bioavailability if orally administered."( Pharmacokinetics and pharmacodynamics in clinical use of scopolamine.
Kirch, W; Oertel, R; Renner, UD, 2005
)
0.33
" Despite previous evidence to the contrary, a recent bioavailability study demonstrated similar intraindividual absorption and sustained clinical efficacy with long-term use of the drug."( Transdermal scopolamine for prevention of motion sickness : clinical pharmacokinetics and therapeutic applications.
Gordon, CR; Nachum, Z; Shupak, A, 2006
)
0.33
" 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 purpose of this study was to develop a sublingual drug delivery spray formulation of scopolamine hydrobromide (L-(-)-hyoscine hydrobromide) and to determine the absolute bioavailability of scopolamine hydrobromide following sublingual delivery and to investigate the effect of a bioadhesive on the pharmacokinetic parameters of this drug in a rabbit model."( Scopolamine sublingual spray: an alternative route of delivery for the treatment of motion sickness.
Al-Ghananeem, AM; Crooks, PA; Malkawi, AH, 2007
)
0.34
" We estimated bioavailability of four different oral formulations used by the NASA RGO physicians for the treatment of motion sickness."( Relative bioavailability of scopolamine dosage forms and interaction with dextroamphetamine.
Boyd, JL; Du, B; Locke, JP; Putcha, L; Vaksman, Z, 2007
)
0.34
" These results suggest that the n-3 LC-PUFA carrier may play a role in these fatty acids bioavailability and their impact on specific cognitive processes."( n-3 phosphatidylserine attenuated scopolamine-induced amnesia in middle-aged rats.
Pelled, D; Vaisman, N, 2009
)
0.35
" Memogain has more than 15-fold higher bioavailability in the brain than the same doses of galantamine."( Memogain is a galantamine pro-drug having dramatically reduced adverse effects and enhanced efficacy.
Hoeffle-Maas, A; Jordis, U; Koepke, AK; Ludwig, J; Maelicke, A; Maus, A; Samochocki, M, 2010
)
0.36
"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 presence of AG in the KXS formula led to increases in the initial absorption rate and extent of Rg1 and Re in terms of Cmax1 and AUC(0-3h) compared to KXS without AG."( The effect of Acorus gramineus on the bioavailabilities and brain concentrations of ginsenosides Rg1, Re and Rb1 after oral administration of Kai-Xin-San preparations in rats.
Chang, Q; Liao, QP; Liao, YH; Liu, CY; Liu, XM; Quan, LH; Wang, W, 2010
)
0.36
" The absorption rate and AUC of test tablet is different from that of reference tablet."( [Pharmacokinetics of scopolamine hydrobromide oral disintegrative microencapsule tablets in Beagle dogs determined with LC-MS/MS].
Hu, JH; Liu, DD; Shi, LF; Xia, T, 2011
)
0.37
" Because of their partial solubility, Atr, Ani, AT3, and Sco had different bioavailability in rats of 21."( Comparative study on pharmacokinetics of a series of anticholinergics, atropine, anisodamine, anisodine, scopolamine and tiotropium in rats.
Chen, X; Li, C; Li, N; Liu, Q; Lu, Y; Ren, S; Tian, F; Wang, X; Zhao, D; Zhou, S, 2015
)
0.42
" The relative bioavailability of intranasal administrations was 51."( Microdialysis pharmacokinetic study of scopolamine in plasma, olfactory bulb and vestibule after intranasal administration.
Cao, S; Jiang, X; Wang, F; Wang, Y; Wei, Y; Xu, S; Ying, M; Zou, A, 2016
)
0.43
" Bioavailability after oral administration of scopolamine is low and variable, and absorption form transdermal patch is slow and prolonged."( Dose escalation pharmacokinetics of intranasal scopolamine gel formulation.
Boyd, JL; Chow, DS; Daniels, V; Putcha, L; Wang, Z; Wu, L, 2015
)
0.42
" Moreover, ipriflavone is a non-peptidomimetic small molecule AChE inhibitor with an improved bioavailability after systemic administration, due to its efficient blood-brain barrier permeability in comparison with peptidomimetic inhibitors."( Neuroprotective effect of ipriflavone against scopolamine-induced memory impairment in rats.
Abady, MM; Abdel-Monem, N; El Demellawy, MA; Ghareeb, DA; Hafez, HS; Hussien, H; Saleh, SR, 2017
)
0.46
"The present investigation was carried out to improve the galantamine bioavailability in brain by intranasal drug delivery through thiolated chitosan nanoparticles and compared to nasal and oral delivery of its solution using pharmacodynamic activity as well as biochemical estimation."( Nose to Brain Delivery of Galantamine Loaded Nanoparticles: In-vivo Pharmacodynamic and Biochemical Study in Mice.
Mishra, DN; Singh, SK, 2019
)
0.51
"B to mice showed enhanced bioavailability and dose-dependent repression of the behavioral/cognitive impairment by regulating the cholinergic function, restoring the antioxidant status, attenuating the inflammatory cytokines/mediators and actively enriching neurotropic proteins in the hippocampal regions of the scopolamine-administered mice."( Cognitive-enhancing and ameliorative effects of acanthoside B in a scopolamine-induced amnesic mouse model through regulation of oxidative/inflammatory/cholinergic systems and activation of the TrkB/CREB/BDNF pathway.
Choi, DK; Ganesan, P; Karthivashan, G; Kim, DH; Kim, JS; Kweon, MH; Park, SY, 2019
)
0.51
" Among them, the steady intestinal and liver metabolism of curcumin by a curcumin adjuvant (enzyme inhibitor/inducer) is an important and less engrossed strategy for improving the overall systemic bioavailability of curcumin."( Potentiation of anti-Alzheimer activity of curcumin by probiotic Lactobacillus rhamnosus UBLR-58 against scopolamine-induced memory impairment in mice.
Acharya, S; Pande, S; Patel, C, 2020
)
0.56
" In conclusion, this study indicates that the bioavailability of OST was improved by using the OST-NE via the nasal route."( Osthole-Loaded Nanoemulsion Enhances Brain Target in the Treatment of Alzheimer's Disease via Intranasal Administration.
Hao, J; Hao, Q; Hou, X; Song, Y; Wang, J; Wang, X, 2021
)
0.62
"71), enhanced systemic bioavailability (F = 118."( Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer's disease.
Arumugam, K; Bojja, SL; Kumar, N; Rao, CM; Rompicherla, SKL, 2021
)
0.62
"Prediction of skin absorption and local bioavailability from topical formulations remains a difficult task."( Skin Pharmacokinetics of Transdermal Scopolamine: Measurements and Modeling.
Bunge, AL; Delgado-Charro, MB; Guy, RH; Hattam, L; McGrogan, A; Pensado, A; White, KAJ, 2021
)
0.62
"The purpose of the study is to assess the bioavailability and neuroprotective effect of hesperetin (Hesp)-loaded nanofibers."( Hesperetin-loaded polymeric nanofibers: assessment of bioavailability and neuroprotective effect.
Pattnaik, S; Yadav, YC, 2023
)
0.91
" Because of the greatly improved bioavailability of Hesp, the Hesp-loaded nanofibers significantly protected rats from scopolamine-induced amnesia."( Hesperetin-loaded polymeric nanofibers: assessment of bioavailability and neuroprotective effect.
Pattnaik, S; Yadav, YC, 2023
)
0.91
"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

Dosage Studied

ExcerptRelevanceReference
" The choice of a suitable counter-ion can also drastically improve the detection limit, permitting the determination of drug substances in low dosage and possibly of by-products or breakdown products."( High-speed ion-pair partition chromatography in pharmaceutical analysis.
Frei, RW; Huen, JM; Santi, W, 1975
)
0.25
" A more potent dosage of human leukocyte interferon might provide better results."( Interferon in treatment of dendritic keratitis in humans: a preliminary report.
Manthey, KF; Müller, O; Neumann-Haefelin, D; Sundmacher, R, 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
" The incidence of tracheal soiling was lower than that with other intravenous techniques and could be attributed to the use of the semisupine position or the baseline concept of narcotic dosage in the Jorgensen technique."( The efficacy of the laryngeal reflex in conscious sedation.
Allen, GD; Jorgensen, NB; Ricks, CS, 1977
)
0.26
" Management of adverse reactions produced by either methapyrilene or pyrilamine consists of dosage reduction or discontinuation."( Sleep aids and sedatives.
Thornton, WE, 1977
)
0.26
" A comparison of dose-response functions for dopamine using solution injections in VAS and posterior striatum (PS) confirmed that only VAS was responsive."( Identification of a subregion within rat neostriatum for the dopaminergic modulation of lateral hypothalamic self-stimulation.
Gold, MS; Neill, DB; Peay, LA, 1978
)
0.26
" A comparison of dose-response functions for injections of dopamine in solution into ventral anterior, central and posterior striatum confirmed that only injections into ventral anterior striatum (VAS) decreased response efficiency on the DRL schedule."( Anatomical specificity within rat striatum for the dopaminergic modulation of DRL responding and activity.
Herndon, JG; Neill, DB, 1978
)
0.26
" Neither the effective dosage nor the drug's effect on the operant task could be easily generalized to aggressive responses."( Comparing the effects of scopolamine on operant and aggressive responses in squirrel monkeys.
Gore, W; Mollenauer, S; Plotnik, R; Popov, A,
)
0.13
", circling behavior) in a spherical "rotometer" and dose-response relationships were generated using d-amphetamine, apomorphine, L-Dopa, haloperidol, and scopolamine."( Drug-induced rotation in rats without lesions: behavioral and neurochemical indices of a normal asymmetry in nigro-striatal function.
Glick, SD; Jerussi, TP, 1976
)
0.26
"5 mg/70 kg scopolamine produced a virtually linear dose-response curve for amnesia."( Amnesic actions of diazepam and scopolamine in man.
Frumin, MJ; Herekar, VR; Jarvik, ME, 1976
)
0.26
" By utilizing the drugs discussed and titrating the dosage to the needs of the patient, intravenous sedation will last long enough to complete the selected periodontal surgical procedure."( Intravenous sedation of the periodontal surgical patient.
Ruggerio, AC, 1975
)
0.25
" Comparison if single injections of MSB and atropine in normal subjects also demonstrated a more reliable dose-response relationship with MSB."( Cardiac rate and rhythm changes with atropine and methscopolamine.
Allen, AT; Coleman, E; Frederickson, EL; Goldberg, LI; Neeld, JB, 1975
)
0.25
" The same dosage did not affect the threshold for wheen running induced by electrical brain stimulation (EBS)."( Attenuation of "acute" habituation by scopolamine in the black-tailed prairie dog (Cynomys ludovicianus).
Carlson, RH; Sanders, MG; Tal, A; Wood, WG, 1975
)
0.25
" Both At and Sc in a wide range of dosage protect against the tonic phase of convulsions produced by electroshock."( Central action of drugs acting on the cholinergic muscarinic receptor. III. Influence of atropine and scopolamine injected intraventricularly on behavior and levels of biogenic amines in the rat brain.
Kleinrok, Z; Poddubiuk, Z; Zebrowska-Lupina, I, 1975
)
0.25
" Scopolamine produced an inverted U dose-response curve for ambulation, an increase in rearing but no effect on grooming."( Dose-response effects of scopolamine on activity in an open field.
Blain, S; Stewart, WJ, 1975
)
0.25
" The value of low dosage of pyridostigmine (30 mg three times daily) in preventing peripheral anti-muscarinic side effects of a transdermal controlled-release formulation of hyoscine, was tested in a double-blind placebo-controlled study, involving 47 healthy subjects."( Prevention of peripheral side-effects of transdermal hyoscine by adjunctive therapy with low dosage of pyridostigmine.
Alhalel, A; Alkalay, M; Almog, S; Izraeli, S; Menahem, S; Ruach, M; Tochner, Z; Versano, D; Ziv, I, 1992
)
0.28
" The conditioning train produced a displacement to the right of the dose-response curve for C6."( Long-term potentiation of nicotinic transmission by a heterosynaptic mechanism in the stellate ganglion of the cat.
Bachoo, M; Polosa, C, 1991
)
0.28
" 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
"01-1 mg/kg) increased the number of penile erections with bell-shaped dose-response curves."( Septohippocampal cholinergic pathway and penile erections induced by dopaminergic and cholinergic stimulants.
Maeda, N; Matsuoka, N; Yamaguchi, I, 1990
)
0.28
" Scopolamine hydrobromide reinstated contralateral placing errors in infarcted rats at a dosage that did not affect neurologically intact rats."( Ionic channels, cholinergic mechanisms, and recovery of sensorimotor function after neocortical infarcts in rats.
De Ryck, M; Duytschaever, H; Janssen, PA; Pauwels, PJ, 1990
)
0.28
" The effects of scopolamine in this study and others are considered in terms of a model which implies that magnitude of performance deficit depends on performance type (cognitive, motor, self-report) and dosage level."( Differential effects of scopolamine and amphetamine on microcomputer-based performance tests.
Baltzley, DR; Dunlap, WP; Kennedy, RS; Odenheimer, RC; Wood, CD, 1990
)
0.28
" The use of these TTS products has resulted in controlled plasma concentration of drug and reduced side effects by the use of TTS(scopolamine) and more physiologic estradiol to estrone ratio with the transdermal dosage form of estradiol."( Transdermal therapeutic systems and rate controlled drug delivery.
Yum, SI, 1989
)
0.28
" Anisocoria and narrow angle glaucoma were involved in four cases; in one case, the use of a strong dosage resulted in a bilateral mydriasis in a child."( [Transdermal scopolamine and mydriasis].
Cottin, C; Jouglard, J; Rodor, F,
)
0.13
" The dose-response curves for these compounds were bell-shaped."( Effects of N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide (DM-9384) on learning and memory in rats.
Akashi, A; Kojima, H; Ojima, H; Sakurai, T; Yamasaki, T, 1989
)
0.28
" Dose-response curves to carbachol, muscarine and oxotremorine were shifted to the right by gallamine and pirenzepine in a parallel manner with no change in maximal response ostensibly indicating simple competitive inhibition."( Pharmacologic discrimination between receptor heterogeneity and allosteric interaction: resultant analysis of gallamine and pirenzepine antagonism of muscarinic responses in rat trachea.
Boselli, C; Kenakin, T, 1989
)
0.28
" All three antihistaminics, at some dosage levels, enhanced morphine-induced hyperactivity, but did not change or even reduce locomotor stimulation induced by amphetamine and scopolamine."( Antihistaminics enhance morphine-, but not amphetamine- and scopolamine-induced hyperactivity in mice.
D'Udine, B; Renzi, P; Sansone, M; Vetulani, J, 1987
)
0.27
" 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
)
0.28
" H1-agonists (2-methylHi and 2-thiazolylethylamine) also depressed the avoidance response; their dose-response lines run parallel to that of Hi."( The effects of histamine and some related compounds on conditioned avoidance response in rats.
Akahori, H; Kamei, C; Kitazumi, K; Tasaka, K, 1985
)
0.27
" In an apparently all-or-none manner, both caused a sinistral shift in dose-response curves for the phasic component of the contractile response to histamine at H1 receptors on the ileum."( Metronidazole and 5-aminosalicylic acid enhance the contractile activity of histaminergic agonists on the guinea-pig isolated ileum.
Barker, LA; Winbery, SL, 1986
)
0.27
" Methods also have been developed to determine the skin irritation potential of a drug substance during the preclinical stages of transdermal dosage form development."( Testing of controlled-release transdermal dosage forms. Product development and clinical trials.
Amkraut, AA; Prevo, ME; Shaw, JE, 1987
)
0.27
" The differential effect of delay value on delta-arm scores was also eliminated in a dosage dependent manner with scopolamine."( Effects of selection delays on radial maze performance: acquisition and effects of scopolamine.
Baron, SP; Peele, DB, 1988
)
0.27
" With the same drug dosing method, the effects of ScHBr also were tested in clinical dental examination procedures in two dental student groups."( Oral scopolamine hydrobromide solution as an antisialagogic agent in dentistry.
Markkanen, YJ; Pihlajamäki, K, 1987
)
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
" This latter method transfers knowledge about the dose-response pattern of an agonist to subsequent interaction experiments involving the agonist and putative antagonists."( On the use of some multivariate statistical methods in pharmacological research.
Ståhle, L; Wold, S, 1986
)
0.27
"1-30 mg/kg) elicited yawning that began 15-20 min after injection and lasted for 60 min, and the dose-response curve showed a bell-shaped form."( Desipramine induces yawning behaviour in rats.
Czyrak, A; Klimek, V; Mogilnicka, E; Wedzony, K, 1986
)
0.27
" The present experiments extend these findings by providing dose-response data on the effects of scopolamine and Ditran on neocortical activity in relation to behavior in the rat."( Joint cholinergic-serotonergic control of neocortical and hippocampal electrical activity in relation to behavior: effects of scopolamine, ditran, trifluoperazine and amphetamine.
Stewart, DJ; Vanderwolf, CH, 1986
)
0.27
" In hexamethonium, pirenzepine shifted the acetylcholine dose-response curve to the right with an equilibrium dissociation constant of 200 nM, indicating an interaction with a m2-type of muscarinic receptor."( Acetylcholine acts on m2-muscarinic receptors to excite rat locus coeruleus neurones.
Egan, TM; North, RA, 1985
)
0.27
" No dose-response relationship was found between the urinary excretion of scopolamine and alleviation of nausea."( Transdermally administered scopolamine vs. dimenhydrinate. I. Effect on nausea and vertigo in experimentally induced motion sickness.
Jäntti, V; Pyykkö, I; Schalén, L,
)
0.13
"Moderate improvement of cognitive function has been reported in many clinical studies of Hydergine (HYD) but in only a few controlled dose-response studies in animals."( Hydergine enhances memory in mice.
Cherkin, A; Flood, JF; Smith, GE, 1985
)
0.27
" The log dose-response curve for depolarization was sigmoid with a mean ED(50) of 12."( Depolarizing actions of gamma-aminobutyric acid and related compounds on rat superior cervical ganglia in vitro.
Bowery, NG; Brown, DA, 1974
)
0.25
" Hexamethonium and hyoscine did not affect the dose-response relationship for NA."( Studies of the interaction of 5-hydroxytryptamine and the perivascular innervation of the guinea-pig caecum.
Drakontide, AB; Gershon, MD, 1972
)
0.25
" However, the dose-response curve for pilocarpine was steeper than that for apomorphine."( Apomorphine-induced and pilocarpine-induced hypothermia in mice: drug interactions and changes in drug sensitivity after caudate nucleus lesions.
Glick, SD; Marsanico, RG, 1974
)
0.25
" Supersensitivity was observed, after daily oral dosing with hyoscine, in the increased salivation of mice in response to pilocarpine injected at least 66 h after withdrawing hyoscine."( Supersensitivity of salivation in response to pilocarpine after withdrawal of chronically administered hyoscine in the mouse.
Parkes, MW; Parks, JC, 1972
)
0.25
"Scopolamine induced blockade of play fighting in juvenile rats and the rapid induction of behavioral tolerance to an initially effective dosage suggested a rebound in social play following chronic scopolamine exposure."( Social play in juvenile rats during scopolamine withdrawal.
Holloway, WR; Thor, DH, 1984
)
0.27
" For example, M-methyl-4-piperidinol benzylate applied in a wide dosage range induced motor hyperactivity without affecting the short-term memory, whereas tropine phenylcyclopentylglycolate provoked motor hyperactivity and memory disorders at equal doses."( [Comparative study of the effect of 3 M-cholinergic blockaders on memory and motor activity in rats].
Sprints, AM; Vinogradov, VV; Zhirova, ND,
)
0.13
" Following completion of the dose-response determination for the effect of desipramine or water intake, rats were divided into three groups for repeated administration."( The effect of repeated desipramine administration on water intake in rats.
O'Donnell, JM; Rider, DP; Seiden, LS; Somani, S, 1982
)
0.26
" Generally, the dose-response curves were bell-shaped."( Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents.
Bandle, EF; Cumin, R; Gamzu, E; Haefely, WE, 1982
)
0.26
" These side effects could result from the unpredictable blood levels attained with oral dosage (pulse delivery)."( Transdermal scopolamine in motion sickness.
Cronin, CM; Sallan, SE; Wolfe, L,
)
0.13
" Adverse effects are often related to dosage or other factors."( Mydriatic and cycloplegic drugs: a review of ocular and systemic complications.
Doughty, CB; Rengstorff, RH, 1982
)
0.26
" Ten of the studies are dose-response evaluations."( Sleep spindles: pharmacological effects in humans.
Hirshkowitz, M; Karacan, I; Thornby, JI, 1982
)
0.26
"High-performance liquid chromatographic separations are described for the analysis of hyoscyamine-atropine and scopolamine in combination pharmaceutical dosage forms containing phenobarbital."( Belladonna alkaloids and phenobarbital combination pharmaceuticals analysis I: High-performance liquid chromatographic determinations of hyoscyamine-atropine and scopolamine.
Pennington, LJ; Schmidt, WF, 1982
)
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
" In a dose-response experiment it was demonstrated that 50 mg kg-1 was the lowest oral dose of aniracetam to significantly ameliorate scopolamine-induced amnesia."( Aniracetam reverses memory impairment in rats.
Jenck, F; Martin, JR; Moreau, JL, 1995
)
0.29
" Dose-response curves performed in 12 dogs at high (n = 6) and low (n = 6) risk showed that scopolamine at 3 micrograms/kg exerts the greatest effect on HRV."( Do increases in markers of vagal activity imply protection from sudden death? The case of scopolamine.
Adamson, PB; De Ferrari, GM; Foreman, RD; Hull, SS; Schwartz, PJ; Vanoli, E, 1995
)
0.29
" There was not a significant scopolamine x pilocarpine interaction, suggesting that pretreatment with scopolamine produced an apparent parallel shift in the pilocarpine dose-response curve."( Repeated scopolamine injections sensitize rats to pilocarpine-induced vacuous jaw movements and enhance striatal muscarinic receptor binding.
Baskin, PP; Gianutsos, G; Salamone, JD, 1994
)
0.29
" Of these latter, the most serious was that in 1982 he published a scientific journal, spurious results relating to laboratory experiments on pregnant rabbits dosed with scopolamine."( Scientific fraud: the McBride case--judgment.
Humphrey, GF, 1994
)
0.29
"01-1 mg/kg) induced penile erection in rats with bell-shaped dose-response curves."( Role of the dopaminergic, serotonergic and cholinergic link in the expression of penile erection in rats.
Maeda, N; Matsuoka, N; Yamaguchi, I, 1994
)
0.29
" However, in 22MO rats, the behavioral dose-response curve for scopolamine was shifted towards greater sensitivity."( Cholinergic manipulations in the medial septal area: age-related effects on working memory and hippocampal electrophysiology.
Givens, B; Markowska, AL; Olton, DS, 1995
)
0.29
") antagonized this deficit induced by scopolamine, with a bell-shaped dose-response curve."( DAU 6215, a novel 5-HT3-receptor antagonist, selectively antagonizes scopolamine-induced deficit in a passive-avoidance task, but not scopolamine-induced hypermotility in rats.
Borsini, F; Brambilla, A; Ghiorzi, A; Pitsikas, N, 1993
)
0.29
" No significant differences were found in the contribution to the improvement in diagnostic efficacy between the two dosage groups, the use and nonuse of parasympathetic blockers, or patients with and without fasting."( Large scale clinical evaluation of bowel contrast agent containing ferric ammonium citrate in MRI.
Fujita, N; Hirohashi, S; Kawamura, Y; Matsui, O; Ohtomo, K; Uchida, H; Yoshikawa, K; Yuasa, Y, 1994
)
0.29
" The compound facilitated penile erection in naive rats, and it ameliorated scopolamine-induced amnesia of rats in passive avoidance tasks with bell-shaped dose-response curves, while it dose-dependently reduced body weight gain in Zucker fatty rats."( A screening concept based on a hypothesis led to the development of a putative cognitive enhancer that stimulates penile erection.
Arakawa, H; Maeda, N; Matsuoka, N; Ohkubo, Y; Yamaguchi, I; Yamazaki, M, 1994
)
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
)
0.29
" Results show that as the dosage of SCP increased, the mean toxicity scores decreased."( Efficacy comparison of scopolamine and diazepam against soman-induced debilitation in guinea pigs.
Anderson, DR; Bowersox, SL; Carter, WH; Gennings, C; Harris, LW; Lennox, WJ; Solana, RP, 1994
)
0.29
"Diazepam (DZ) and scopolamine (SCP) are known to be beneficial when each is used in combination with atropine (AT) + oxime therapy against intoxication by soman, but the efficacy of each might be expected to vary with the dosage of AT."( Efficacy comparison of scopolamine (SCP) and diazepam (DZ) against soman-induced lethality in guinea pigs.
Anderson, DR; Bowersox, SL; Carter, WH; Gennings, C; Harris, LW; Lennox, WJ; Solana, RP, 1994
)
0.29
" The inhibition was associated with a bell-shaped dose-response curve."( Effects of vasoactive intestinal peptide (VIP) on scopolamine-induced amnesia in the rat.
Kobayashi, H; Yamaguchi, Y, 1994
)
0.29
"3 and 1 mg/kg ip for most compounds), the presence of a bell-shaped dose-response curve and, generally, a reduction of biological activity after po administration."( Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
Banfi, S; Biagetti, R; Cerri, A; Dorigotti, L; Farina, C; Magnani, M; Pfeiffer, U; Pinza, M; Pozzi, O; Riccaboni, MT, 1993
)
0.29
"8 mg/kg as free TRH) produced a sustained increase in immunoreactive plasma TRH levels up to about 2 weeks after dosing in rats."( Effects of sustained release formulation of thyrotropin-releasing hormone on learning impairments caused by scopolamine and AF64A in rodents.
Hirai, K; Kato, K; Miyamoto, M; Nagaoka, A; Nishiyama, M; Okada, H; Takahashi, H, 1993
)
0.29
" The dosage of 10 microM Glu-induced [Ca2+]i accumulation was inhibited by several different types of Ca antagonists and scopolamine."( Relation between long-lasting amounts of excitatory amino acid and its neuronal uptake system in cultured cerebellar granule cells under hypoglycemia.
Hayashi, H; Shibuya, T; Watanabe, Y, 1993
)
0.29
" Therefore, a dose-response curve of posttraining injection (intraperitoneal) of fluoxetine was carried out in an associative learning task (auto-shaping)."( Effect of fluoxetine on learning and memory involves multiple 5-HT systems.
Hong, E; Meneses, A, 1995
)
0.29
" The inhibition of the reduction in initial correct responses was associated with a bell-shaped dose-response curve for Rg1."( Effects of ginsenosides on impaired performance induced in the rat by scopolamine in a radial-arm maze.
Haruta, K; Kobayashi, H; Yamaguchi, Y, 1995
)
0.29
" Four chemicals, using three different routes of exposure (in utero [accomplished by feeding the dam dosed feed], dosed feed, and gavage) were used to 1) evaluate the effect of diet restriction on the sensitivity of the bioassay toward chemically-induced chronic toxicity and carcinogenicity; and 2) evaluate the effect of weight-matched control groups on the sensitivity of the bioassays."( The sensitivity of the NTP bioassay for carcinogen hazard evaluation can be modulated by dietary restriction.
Abdo, KM; Kari, FW, 1996
)
0.29
" The cholinergic antagonists exerted complex changes in the ONR-ON component depending on dosage and adaptation."( Cholinergic effects on cat retina In vitro: changes in rod- and cone-driven b-wave and optic nerve response.
Jurklies, B; Kaelin-Lang, A; Niemeyer, G, 1996
)
0.29
" 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
)
0.29
"The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers."( Bioavailability of intranasal scopolamine in normal subjects.
Bourne, DW; Cintrón, NM; Hunter, RP; Parise, CM; Putcha, L; Tietze, KJ, 1996
)
0.29
") inhibited a decrease in ACh content in the frontal cortex, and with the same dosage of HJ increased CAT activity in the frontal cortex and AChE activity in the hippocampus."( Effect of Hachimi-jio-gan on scopolamine-induced memory impairment and on acetylcholine content in rat brain.
Amagaya, S; Hirokawa, S; Ishige, A; Nose, M; Ogihara, Y; Oyama, T, 1996
)
0.29
" Although anaesthesia was not standardized, there was no difference in anaesthesia techniques, drug dosage or perioperative management."( [Transdermal scopolamine for prevention of postoperative nausea and vomiting. No clinically relevant result in spite of reduced postoperative vomiting in general surgical and gynecologic patients].
Eberhart, LH; Holzrichter, P; Roscher, R, 1996
)
0.29
" Dosage of the separate drugs in ophthalmic preparations is also presented."( Development and validation of a capillary zone electrophoresis method for the determination of atropine, homatropine and scopolamine in ophthalmic solutions.
Cherkaoui, S; Christen, P; Mateus, L; Veuthey, JL, 1997
)
0.3
" Study results indicate that fetal behavioural states can be altered pharmacologically and in a manner similar to that seen in the adult but with notable differences that may relate to species, developmental or dose-response issues."( The effects of 'sleep promoting agents' on behavioural state in the ovine fetus.
Carmichael, L; Homan, J; Morrison, JL; Richardson, BS, 1997
)
0.3
" (-)-Rolipram produced a biphasic dose-response and (+/-)-rolipram produced a broad dose-response."( Rolipram and its optical isomers, phosphodiesterase 4 inhibitors, attenuated the scopolamine-induced impairments of learning and memory in rats.
Egawa, T; Fujiwara, M; Iwasaki, K; Matsumoto, Y; Mishima, K, 1997
)
0.3
" The peripheral cholinergic antagonist, SCOPMB, generally produced small to moderate depressions in all measures with the exception of patterning of arm entries and pellets earned, but there were no clear dose-response relationships evident in the data."( Scopolamine-induced impairment in concurrent fixed-interval responding in a radial maze task.
Elsmore, TF; Pilcher, JJ; Sessions, GR, 1998
)
0.3
" The reversal of scopolamine-induced impairment was characterized by an inverted U-shaped dose-response curve."( Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268).
Braida, D; Colibretti, L; Griffini, P; Lamperti, M; Paladini, E; Sala, M, 1998
)
0.3
" Unilateral microinjection of these substances produced changes mainly only on the day of dosage and had no effect on subsequent behavior, while bilateral microinjection altered the established motor behavior for a longer period of time."( Increasing the activity of the neostriatum cholinergic system alters an established type of motor behavior in animals.
Shapovalova, KB,
)
0.13
" Methysergide counteracted the effect of thioperamide in the open-field test only at a high dosage (50 mg/kg)."( Combined action of thioperamide plus scopolamine, diphenhydramine, or methysergide on memory in mice.
Di Carlo, G; Ghi, P; Molinengo, L, 1999
)
0.3
" The scopolamine-induced abolishment of rCBF response was restored by the administration of FK960 at relatively wide dosing range from 1 to 1000 microg/kg (i."( FK960 [N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide monohydrate], a novel potential antidementia drug, restores the regional cerebral blood flow response abolished by scopolamine but not by HA-966: a positron emission tomography study with unanesthetized
Inoue, T; Kakiuchi, T; Matsuoka, N; Nishimura, S; Nishiyama, S; Noda, A; Tsukada, H; Yamazaki, S, 1999
)
0.3
" An inverted U-shaped unit dose-response curve was seen with the contingent mice."( Intravenous scopolamine is potently self-administered in drug-naive mice.
Fink-Jensen, A; Rasmussen, T, 2000
)
0.31
" The NGT could be removed in all 10 home care and in 3 hospitalized patients without changing the dosage of the drugs."( Role of octreotide, scopolamine butylbromide, and hydration in symptom control of patients with inoperable bowel obstruction and nasogastric tubes: a prospective randomized trial.
Casuccio, A; De Conno, F; Groff, L; Mercadante, S; Ripamonti, C; Zecca, E, 2000
)
0.31
" Rats were dosed with chlorpyrifos (0 or 25 mg/kg orally)."( Chlorpyrifos-induced hypothermia and vasodilation in the tail of the rat: blockade by scopolamine.
Gordon, CJ; Yang, YL, 2000
)
0.31
" Acute and repeated oral dosing of TC-2559 enhances performance in a radial arm maze task."( TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors.
Bane, AJ; Bencherif, M; Dull, GM; Gatto, GJ; Miller, CH, 2000
)
0.31
" However, there never appeared a nasal dosage form."( Scopolamine nasal spray in motion sickness: a randomised, controlled, and crossover study for the comparison of two scopolamine nasal sprays with oral dimenhydrinate and placebo.
Hanschke, W; Klöcker, N; Toussaint, S; Verse, T, 2001
)
0.31
" The observations made using different doses indicate that these learning-facilitating and/or memory-consolidating effects by the agents follow inverse U-shaped dose-response curves in dose ranges lower than (for hyperforin) or equal to (for Hypericum extract) their effective dose in the behavioral despair test for antidepressants."( Hypericum extract and hyperforin: memory-enhancing properties in rodents.
Chatterjee, SS; Germane, S; Klusa, V; Nöldner, M, 2001
)
0.31
" The specific objectives of research are to identify physiologic, pharmacokinetic, and pharmacodynamic changes in space; to develop simple, reliable, non-invasive, safe and effective acute and sustained-release dosage forms and regimens for pharmacological interventions in space; and to create and maintain a comprehensive space PK-PD and therapeutics database."( Pharmacotherapeutics in space.
Putcha, L, 1999
)
0.3
" Results indicate that GRP at this dose improved memory only when the dosage of scopolamine was relatively low (1 mg/kg)."( Posttraining administration of gastrin-releasing peptide improves memory loss in scopolamine- and hypoxia-induced amnesic mice.
Santo-Yamada, Y; Wada, K; Yamada, K,
)
0.13
" The improving effects of huperzine A exhibited a bell-shaped dose-response curve."( Huperzine A reverses scopolamine- and muscimol-induced memory deficits in chick.
Gao, Y; Guan, LC; Kuang, PZ; Tang, XC, 2000
)
0.31
" The common currency for this quantitation is the dose-response curve."( Quantitation in receptor pharmacology.
Kenakin, TP, 2001
)
0.31
" The three doses of DCS reduced this increase significantly and resulted in a U-shaped dose-response curve, where 15 mg/kg had a stronger compensatory effect than both 5 and 50 mg/kg."( Effects of scopolamine and D-cycloserine on non-spatial reference memory in rats.
Andersen, JM; Lindberg, V; Myhrer, T, 2002
)
0.31
"0 min after the intravenous administration of each drug and at all dosages except the lowest dosage of atropine."( Ultrasonographic evaluation of reticular motility in cows after administration of atropine, scopolamine and xylazine.
Braun, U; Gansohr, B; Haessig, M, 2002
)
0.31
" Demerol in small dosage is safe and effective."( An evaluation of obstetrical analgesia.
FIST, HS, 1954
)
0.23
" These data indicate that some of the pronounced neurobehavioral changes observed following fenamiphos dosing may be centrally mediated (blocked by SCO only), despite the small amount of inhibition of brain ChE."( Differential profiles of cholinesterase inhibition and neurobehavioral effects in rats exposed to fenamiphos or profenofos.
McDaniel, KL; Moser, VC,
)
0.13
" Such a hyposensitivity did not develop after a single or multiple (at short intervals) dosing with oxotremorine (OXO), a direct muscarinic agonist, which suggests that it was not mediated by muscarinic receptors."( Behavioral sensitivity to amphetamine or scopolamine after acute administration of nicotine in the rat.
Gralewicz, S; Lutz, P, 2005
)
0.33
"Attempts to increase scopolamine levels in plasma by increasing the drug dosage or improving transdermal absorption should be considered for the treatment of "non-responders"."( Scopolamine patch to prevent seasickness: clinical response vs. plasma concentration in sailors.
Adir, Y; Chapman, S; Dachir, S; Gil, A; Levy, A; Nachum, Z; Shupak, A; Tal, D, 2005
)
0.33
" Pharmacokinetic parameters are dependent on the dosage form (oral dose, tablets; parenteral application; IV infusion; SC and IM injection)."( Pharmacokinetics and pharmacodynamics in clinical use of scopolamine.
Kirch, W; Oertel, R; Renner, UD, 2005
)
0.33
" To reveal any effect of cholinergic dysfunction on APP processing in vivo, 11-month-old transgenic Tg2576 mice with Abeta plaque pathology received intraperitoneal injections of scopolamine at a daily dosage of 2mg/kg body weight for 14 days in order to suppress cortical cholinergic transmission by chronic inhibition of muscarinic acetylcholine receptors."( Muscarinic acetylcholine receptor inhibition in transgenic Alzheimer-like Tg2576 mice by scopolamine favours the amyloidogenic route of processing of amyloid precursor protein.
Liskowsky, W; Schliebs, R,
)
0.13
") could reverse scopolamine-induced memory retrieval deficits in mice, and displayed a typical bell-shaped dose-response relationship."( Pharmacological profile of PMS777, a new AChE inhibitor with PAF antagonistic activity.
Chen, HZ; Dong, CZ; Gao, XL; Heymans, F; Huang, H; Li, J; Massicot, F; Miezan Ezoulin, JM, 2007
)
0.34
" Dose-response curves for carbachol revealed a lower peak response in new-born bladders compared with adults."( Developmental regulation of nerve and receptor mediated contractions of mammalian urinary bladder smooth muscle.
Andersson, KE; Arner, A; Ekman, M, 2006
)
0.33
" The absence of atropine in hair is consistent with its very low dosage in the flower of Datura inoxia."( Testing for atropine and scopolamine in hair by LC-MS-MS after Datura inoxia abuse.
Barguil, Y; Charlot, JY; Cirimele, V; Kintz, P; Villain, M, 2006
)
0.33
" 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
" For caffeine and scopolamine, even the lowest dosage tested (5 mg/horse/day and 2 mg/horse/day respectively) induced detectable concentrations of the molecule in urine."( Urinary excretion of dietary contaminants in horses.
Bonnaire, Y; Julliand, V; Lallemand, A; Respondek, F, 2006
)
0.33
" Considering the limitations of delivering scopolamine orally or transdermally to patients who experience motion sickness, the sublingual route of administration using a spray delivery dosage form, is a potential alternative modality for the prevention of nausea and vomiting associated with motion sickness."( Scopolamine sublingual spray: an alternative route of delivery for the treatment of motion sickness.
Al-Ghananeem, AM; Crooks, PA; Malkawi, AH, 2007
)
0.34
" A representative quinazolinimine (MD212) showed attenuation of cognitive deficits at a low dosage (0."( In vivo investigations on the cholinesterase-inhibiting effects of tricyclic quinazolinimines: scopolamine-induced cognitive impairments in rats are attenuated at low dosage and reinforced at higher dosage.
Appenroth, D; Decker, M; Fleck, C; Lehmann, J; Mohr, K; Tränkle, C, 2008
)
0.35
" The medications are sometimes dispensed as custom dosage forms in gelatin capsules for convenience."( Relative bioavailability of scopolamine dosage forms and interaction with dextroamphetamine.
Boyd, JL; Du, B; Locke, JP; Putcha, L; Vaksman, Z, 2007
)
0.34
" Although feasible to consent and study this population in a way that respects autonomy and dignity even in the terminal hours of life, this pilot study suggests reconsideration of the pharmacological interventions (choice of agents, dosing, timing of dosing and pharmacokinetic profiles), standardizing of non-pharmacological care; and ways to measure directly family distress before further randomized studies for this symptom."( A pilot phase II randomized, cross-over, double-blinded, controlled efficacy study of octreotide versus hyoscine hydrobromide for control of noisy breathing at the end-of-life.
Abernethy, AP; Agar, M; Clark, K; Currow, DC; Fazekas, BS, 2008
)
0.35
" After equimolar dosage compared to the reference drug rivastigmine (CAS 123441-03-2), two of the new substances slightly improved cognition in rats, but only to a significantly lower degree compared to the irreversible inhibitor rivastigmine."( A new way of data interpretation for cognition tests in rats used to characterise six choline esterase inhibitors with heterocyclic nitrogen bridgehead structure. Application in Alzheimer therapy.
Appenroth, D; Decker, M; Fleck, C; Lehmann, J, 2008
)
0.35
" However, the dosage dependency of scopolamine's effect across different studies and the lack of antidepressant effects with other anticholinergic drugs suggest that a specific muscarinic receptor subtype might be most relevant to the potential antidepressant mechanism of action of anticholinergic drugs."( The antidepressant effects of anticholinergic drugs.
Howland, RH, 2009
)
0.35
" Anticonvulsant effective doses (ED(50)) were determined using an up-down dosing procedure over successive animals."( Protection against sarin-induced seizures in rats by direct brain microinjection of scopolamine, midazolam or MK-801.
McDonough, JH; Shih, TM; Skovira, JW, 2010
)
0.36
" Examination of the dose-response curve of systemically administered scopolamine indicates that sensory discrimination and attention are most sensitive to disruption."( The validity of scopolamine as a pharmacological model for cognitive impairment: a review of animal behavioral studies.
Blokland, A; Klinkenberg, I, 2010
)
0.36
" Acute injection of scopolamine shifted the morphine dose-response curved leftward and downward and acute injection of morphine shifted the scopolamine and nicotine dose-response curves leftward and downward."( Interactions between morphine, scopolamine and nicotine: schedule-controlled responding in rats.
France, CP; Li, JX; Li, X, 2010
)
0.36
" The preparation method of SH-NiMS is stable and reliable to use, which provide a new way to develop new dosage form."( [Preparation of scopolamine hydrobromide nanoparticles-in-microsphere system].
Hu, JH; Li, FQ; Lü, WL; Zhu, QG, 2010
)
0.36
" The dosage and duration of the treatment should be taken into account if GNPs are used in the future as vehicles to carry therapeutic agents into the brain."( Size-dependent impairment of cognition in mice caused by the injection of gold nanoparticles.
Chen, YS; Hong, MY; Huang, GS; Hung, YC; Liau, I; Lin, LW, 2010
)
0.36
" A group of male and female rats was treated with one of these compounds for 15 days, after which a single dosage of scopolamine was administered."( Comparative protective action of curcumin, memantine and diclofenac against scopolamine-induced memory dysfunction.
Ali, EH; Arafa, NM, 2011
)
0.37
" In the experimental dry eye model, application of 1% MIM-D3 to rat eyes for either 1 or 17 consecutive days, followed by 1 week of no dosing produced a statistically significant decrease in corneal staining (p < 0."( An NGF mimetic, MIM-D3, stimulates conjunctival cell glycoconjugate secretion and demonstrates therapeutic efficacy in a rat model of dry eye.
Cumberlidge, G; Jain, P; Lama, T; Li, R; Meerovitch, K; Saragovi, HU, 2011
)
0.37
" Compounds were dosed 30 min before the learning trial of the task."( Phosphodiesterase type 5 (PDE5) inhibition improves object recognition memory: indications for central and peripheral mechanisms.
Akkerman, S; Blokland, A; Menniti, FS; Prickaerts, J; Reneerkens, OA; Rutten, K; Shaffer, CL; Steinbusch, HW, 2012
)
0.38
" For each drug treatment in each brain area, anticonvulsant ED₅₀ values were calculated using an up-down dosing procedure over successive animals."( Neuropharmacological specificity of brain structures involved in soman-induced seizures.
McDonough, JH; Shih, TM; Skovira, JW, 2012
)
0.38
" Furthermore, subcutaneous administration of Bis-Mep (10, 100 or 1000 ng/kg) significantly reversed the scopolamine-induced memory deficits in a typical bell-shaped dose-response manner."( Bis(9)-(-)-nor-meptazinol as a novel dual-binding AChEI potently ameliorates scopolamine-induced cognitive deficits in mice.
Chen, HZ; Cui, Y; Ge, XX; Li, J; Liu, T; Qiu, ZB; Wang, H; Xia, Z; Xie, Q; Xu, J; Xu, JR; Zhang, WW, 2013
)
0.39
"Low and high doses of NIC, cytisine (CYT), CC4 and CC26 respectively improved and worsened the mean running time, showing an inverted U dose-response function."( Role of neuronal nicotinic acetylcholine receptors (nAChRs) on learning and memory in zebrafish.
Braida, D; Gotti, C; Martucci, R; Ponzoni, L; Sala, M; Sparatore, F, 2014
)
0.4
" Serial blood samples and total urine voids were collected after dosing and drug concentrations were determined using a modified LC-MS-MS method."( Dose escalation pharmacokinetics of intranasal scopolamine gel formulation.
Boyd, JL; Chow, DS; Daniels, V; Putcha, L; Wang, Z; Wu, L, 2015
)
0.42
" However, PHA-543613 had lower efficacy in the MK-801 induced transient amnesia model, as the pharmacologically induced memory deficit was only partially reversed and an inverted U-shaped dose-response was found."( Differential effects of α7 nicotinic receptor agonist PHA-543613 on spatial memory performance of rats in two distinct pharmacological dementia models.
Bali, ZK; Bruszt, N; Csurgyók, R; Hernádi, I; Horváth, H; Inkeller, J, 2015
)
0.42
" Scopolamine is metabolized primarily in the liver and excreted by the kidneys, so renal and hepatic impairment should be considered when initiating and dosing this medication."( An unusual case of nonsustained ventricular tachycardia.
Brandt, JC; Harman, E; Winchester, D, 2015
)
0.42
" We found that PO vardenafil restored a scopolamine-induced memory impairment when dosed within 2 min after the learning trial while ICV vardenafil was able to restore memory when injected within 4 min after learning."( PDE5 inhibition improves acquisition processes after learning via a central mechanism.
Akkerman, S; Blokland, A; Cremers, P; Osgood, SM; Prickaerts, J; Shaffer, CL; Steinbusch, HW; van Goethem, NP, 2015
)
0.42
" This suggests that researchers should fully explore dose-response relationships in their strain of choice and use care in the interpretation of reversal of cognitive impairment."( Cross-site strain comparison of pharmacological deficits in the touchscreen visual discrimination test.
Chapin, D; Ding, Z; Kozak, R; Mohler, EG; Rueter, LE; Young, D, 2015
)
0.42
", by reaching the high end of a nicotinic receptor activation inverted-U dose-response function."( Attenuation in rats of impairments of memory by scopolamine, a muscarinic receptor antagonist, by mecamylamine, a nicotinic receptor antagonist.
Gold, PE; Newman, LA, 2016
)
0.43
" However, according to current clinical dosage and treatment period, its direct effect on memory is unclear."( Vinpocetine Improves Scopolamine Induced Learning and Memory Dysfunction in C57 BL/6J Mice.
Gu, PF; Li, Y; Shang, Y; Wang, L, 2016
)
0.43
" These data suggest that vortioxetine has some effects on memory that could be mediated through cholinergic neurotransmission, however these effects are modest and only seen under acute dosing conditions."( Task- and Treatment Length-Dependent Effects of Vortioxetine on Scopolamine-Induced Cognitive Dysfunction and Hippocampal Extracellular Acetylcholine in Rats.
Budac, D; Cajina, M; Haddjeri, N; Hillhouse, TM; Mørk, A; Pehrson, AL; Porter, JH; Rovera, R; Sanchez, C; Smagin, G; Song, D, 2016
)
0.43
"This study revealed the effectiveness of SCOP, PCP, and BIP as tools to induce amnesia, with the PCP model being the most efficacious and SCOP being the only model that demonstrates a clear dose-response relationship."( Comparison of pro-amnesic efficacy of scopolamine, biperiden, and phencyclidine by using passive avoidance task in CD-1 mice.
Malikowska, N; Podkowa, A; Sałat, K, 2017
)
0.46
"The AChE activity was significantly decreased and the content of neurotransmitter acetylcholine (ACh) was significantly increased in normal mice cortex and hippocampus by treatment with donepezil at dosage of 8mg/kg, EXT at dosages of 183, 550, 1650mg/kg and ALK at dosages of 10, 30, 90mg/kg (P<0."( Anti-amnesic effect of extract and alkaloid fraction from aerial parts of Peganum harmala on scopolamine-induced memory deficits in mice.
Cheng, X; Jiang, B; Li, S; Liu, W; Ma, C; Qi, S; Wang, C; Wang, Y; Wang, Z; Xuan, Z; Zhu, Y, 2017
)
0.46
" To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task."( Co-modulation of an allosteric modulator of nicotinic receptor-cholinesterase inhibitor (galantamine) and a 5-HT4 receptor agonist (RS-67333): effect on scopolamine-induced memory deficit in the mouse.
Boulouard, M; Dauphin, F; Freret, T; Hamidouche, K; Lecouflet, P; Lelong-Boulouard, V, 2017
)
0.46
" WHY SHOULD AN EMERGENCY PHYSICIAN BE AWARE OF THIS?: Although therapeutically dosed scopolamine transdermal patches rarely cause complications, incomplete toxidromes can be insidiously common in polypharmacy settings."( Postoperative Anticholinergic Poisoning: Concealed Complications of a Commonly Used Medication.
Farrell, N; Hack, J; Haronian, T; Zhang, XC, 2017
)
0.46
" Expression levels of Arc and Fos mRNA in the hippocampus and amygdala were also evaluated on the second day of dosing by fluorescent in situ hybridization (FISH) and reverse transcriptase-quantitative polymerase chain reaction (RT-qPCR)."( Gene expression analysis of Arc mRNA as a neuronal cell activity marker in the hippocampus and amygdala in two-way active avoidance test in rats.
Igarashi, I; Iguchi, T; Kai, K; Mori, K; Takahashi, E; Tsuchiya, Y; Yasuno, K,
)
0.13
" However, several parameters of scopolamine's potential antidepressant effect remain unknown, such as its dose-response profile and its washout period."( A randomised, double-blind, active placebo-controlled, parallel groups, dose-response study of scopolamine hydrobromide (4-6 μg/kg) in patients with major depressive disorder.
Ayeni, HA; Campbell, D; Chen, JCC; Hoeh, N; Krishnamurthy Naga, V; Muthukumaraswamy, S; Singh, V; Sumner, RL; Sundram, F, 2020
)
0.56
" Determining the dose-response profile and washout period of scopolamine's antidepressant effect will also provide important information for designing and conducting crossover trials."( A randomised, double-blind, active placebo-controlled, parallel groups, dose-response study of scopolamine hydrobromide (4-6 μg/kg) in patients with major depressive disorder.
Ayeni, HA; Campbell, D; Chen, JCC; Hoeh, N; Krishnamurthy Naga, V; Muthukumaraswamy, S; Singh, V; Sumner, RL; Sundram, F, 2020
)
0.56
" This is a complicating factor in the prediction of efficacy in the human situation, largely because atropine dosing also influences therapeutic efficacy of oximes and anticonvulsants generally part of the treatment administered."( Comparative physiology and efficacy of atropine and scopolamine in sarin nerve agent poisoning.
Bohnert, S; Cornelissen, AS; Joosen, MJA; Klaassen, SD; van Groningen, T, 2020
)
0.56
" pharmacokinetic analyses with the goal of scientifically supporting a single and robust method for use across the dosage form and ultimately facilitate the development of more consistent and clinically meaningful labeling."( Determination of Rate and Extent of Scopolamine Release from Transderm Scōp® Transdermal Drug Delivery Systems in Healthy Human Adults.
Brogden, NK; Carr, J; Fisher, J; Ghosh, P; Kandimalla, KK; Kelchen, M; Rajagopal, S; Strasinger, C; Swaminathan, SK; Ueda, K; Wokovich, A; Ye, W, 2020
)
0.56
" First, in silico pharmacokinetic modeling was used to select a dosing protocol by which M-receptor inhibitory brain levels of scopolamine are maintained during prolonged treatment."( Scopolamine prevents aberrant mossy fiber sprouting and facilitates remission of epilepsy after brain injury.
Brandt, C; Gailus, B; Käufer, C; Löscher, W; Meller, S, 2021
)
0.62
" Skin conductance response to conditional stimulus (SCR-to-CS) termination suggested a dose-response relationship for enhanced HPC functioning individuals, wherein individuals receiving scopolamine demonstrated less fear at CX."( Pre-treatment hippocampal functioning impacts context renewal for cholinergic modulated exposure therapy.
Craske, M; Fanselow, M; McGlade, A; Sewart, A; Treanor, M, 2021
)
0.62
" In the case of ineffectiveness, the dosage of drug responsive of sialorrhea can be adjusted according to the patient's response and his/her medical history (i."( [Treatment options for drug-induced sialorrhea: Prescribing guidelines].
Amad, A; Cuvelier, E; Décaudin, B; Fovet, T; Gressier, B; Simon, N, 2022
)
0.72
"In the case of drug-induced hypersalivation, after failure of non-drug therapies and dosage optimization of the causative treatment, an anticholinergic drug can be initiated."( [Treatment options for drug-induced sialorrhea: Prescribing guidelines].
Amad, A; Cuvelier, E; Décaudin, B; Fovet, T; Gressier, B; Simon, N, 2022
)
0.72
"This work focuses on developing nanoemulsions using a low-energy emulsification method for the codelivery of donepezil and memantine in one dosage form intended to be administered via the intranasal route for enhanced brain delivery."( Simultaneous Intranasal Codelivery of Donepezil and Memantine in a Nanocolloidal Carrier: Optimization, Pharmacokinetics, and Pharmacodynamics Studies.
Bhatta, RS; Handa, M; Palkhade, R; Patil, GP; Sanap, SN; Shukla, R; Singh, DP, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency54.95030.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.05310.006038.004119,952.5996AID1159521
GLI family zinc finger 3Homo sapiens (human)Potency5.95570.000714.592883.7951AID1259392
AR proteinHomo sapiens (human)Potency7.49780.000221.22318,912.5098AID1259243
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.00860.00000.690210.0000AID1185256; AID1185257; AID1185258; AID1185259; AID1185260; AID723608
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC50 (µMol)0.00300.00001.15467.5858AID1167257; AID1167263; AID1167267; AID1479898; AID1479900
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.03690.00000.79519.1201AID723606
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.00600.00052.773925.1700AID141667; AID141669; AID141681
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.00050.00010.579710.0000AID141707
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)0.00600.00052.891925.1700AID141667; AID141669; AID141681
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.00600.00052.747825.1700AID141667; AID141669; AID141681
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.00060.00011.753610.0000AID1479900
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)0.00600.00052.780225.1700AID141667; AID141669; AID141681
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.00940.00000.72926.9183AID1185261; AID723848
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)0.00600.00053.314249.5000AID141667; AID141669; AID141681
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.00460.00010.58908.2600AID142941
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)0.00260.00001.403910.0000AID1167235; AID1167243; AID1167251; AID1479893; AID1479895
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.00750.00000.59729.1201AID723849
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.00650.00000.54057.7600AID723607
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Kd0.00300.00021.38829.1000AID142933
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (79)

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)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

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)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

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)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (207)

Assay IDTitleYearJournalArticle
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
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.
AID1479898Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins 2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
AID1167257Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID131433Nootropic effect on mouse passive Avoidance test, using Scopolamine as Amnesic drug on 2 nd day2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID723847Selectivity index, ratio of Ki for human M1 muscarinic receptor to Ki for human M5 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID723602Orthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 100 uM oxotremorine-evoked [3H]DA release2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
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.
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.
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID131434Nootropic effect of the compound, when administered subcutaneously, on mouse passive Avoidance test, using Scopolamine as Amnesic drug on 1 st day2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity.
AID1167251Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID1167236Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID77632In vitro functional studies in guinea pig left atrium1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
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.
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.
AID176600In vitro activity against oxotremorine induced tumors in rat (iv)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID141669Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1148060Anti-tremorine activity against sc dosed albino mouse assessed as normalized dose for reversal of tremorine-induced spontaneous activity depression1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 1. Glycolates.
AID723601Orthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 10 uM oxotremorine-evoked [3H]DA release2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID128205Induction of mydriasis in mice following s.c. administration.1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 2. Non-glycolates.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID26355pKa value was determined1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID419688Antagonist activity at muscarinic receptor2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
3D-QSAR study of 8-azabicyclo[3.2.1] octane analogs antagonists of cholinergic receptor.
AID723600Orthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 100 uM oxotremorine-evoked [3H]DA release at 1 uM2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID1185259Displacement of [3H]-NMS from human muscarinic M2 Y177Q/T423H mutant expressed in Flp-In-CHO cells by liquid scintillation counting2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID142898Inhibition of (-)-[3H]-QNB muscarinic acetylcholine receptor binding on rat/ dog ventricular muscle1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Analogues of 3-quinuclidinyl benzilate.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID135107Anti-tremorine effect in mice following s.c. administration.1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 2. Non-glycolates.
AID140726Minimal effective dose to reverse Scopolamine induced amnesia, when given ip in mouse passive avoidance test2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Design, synthesis, and preliminary pharmacological evaluation of 1, 4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents.
AID723603Selectivity index, ratio of Ki for human M4 muscarinic receptor to Ki for human M5 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
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.
AID190634Tested for running time in radial maze test in rat on the day after treatment at 1 mg/kg sc along with Scopolamine at 50 ug/kg sc1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID142933In vitro receptor binding against Muscarinic acetylcholine receptor M2 in rat heart was determined using [3H]pirenzepine1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID723608Displacement of [3H]NMS from human M2 muscarinic receptor expressed in CHO-K1 cells2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID227699Virtual screen for compounds with anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID1185256Displacement of [3H]-NMS from wild-type human muscarinic M2 receptor expressed in Flp-In-CHO cells by liquid scintillation counting2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
AID1185258Displacement of [3H]-NMS from human muscarinic M2 Y177Q mutant expressed in Flp-In-CHO cells by liquid scintillation counting2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
AID141696In vitro receptor binding against Muscarinic acetylcholine receptor M1 in rat cerebral cortex was determined using [3H]pirenzepine1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID361985Lipophilicity, log D of compound at pH 7.4 by microfluidic liquid-liquid extraction method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID127476Binding affinity against human monoclonal antibody (mAb) 2E2 relative to cocaine by ELISA method.2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Three-dimensional quantitative structure-activity relationship modeling of cocaine binding by a novel human monoclonal antibody.
AID1479900Antagonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured afte2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID190636Tested for running time in radial maze test in rat on the day of treatment at 1 mg/kg sc along with Scopolamine at 50 ug/kg sc1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID129946Change in the latency time on day 1 to that of day 22000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Design, synthesis, and preliminary pharmacological evaluation of 1, 4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents.
AID176598In vitro activity against carbachol-induced colonic spasms in rat (iv)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
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.
AID1167243Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
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.
AID1185260Displacement of [3H]-NMS from human muscarinic M2 W422A mutant expressed in Flp-In-CHO cells by liquid scintillation counting2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
AID723846Orthosteric antagonist activity at human M1 muscarinic receptor expressed in CHO-K1 cells assessed as inhibition of [3H]NMS binding at saturation concentration relative to untreated control2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID1167267Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID679755TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Scopolamine: 100 uM) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID1167252Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1330794Hepatotoxicity in Kunming mouse assessed as area of necrosis in hepatocytes at 3 mg/kg, po for 6 days by hematoxylin and eosin-staining based microscopic analysis2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
AID1479893Antagonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins 2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
AID138626Latency time on 2nd (post-treatment) day of mouse passive-avoidance test.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Design, synthesis, and preliminary pharmacological evaluation of 1, 4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents.
AID1148061Toxicity in iv dosed mouse1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 1. Glycolates.
AID190498Effect on increase in reflex latent time after administration of 1 mg/kg of the compound2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Design of new cognition enhancers: from computer prediction to synthesis and biological evaluation.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID141667Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the absence of Zn1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID377491Anxiolytic activity against CF1 mouse assessed as suppression of oxotremorine-treated tremors at 3 mg/kg2005Journal of natural products, Mar, Volume: 68, Issue:3
Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator.
AID723849Displacement of [3H]NMS from human M1 muscarinic receptor expressed in CHO-K1 cells2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1330793Hepatotoxicity in Kunming mouse assessed as distinct fatty degeneration in hepatocytes at 3 mg/kg, po for 6 days by hematoxylin and eosin-staining based microscopic analysis2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID131283Cognition enhancing activity was evaluated by mouse passive-avoidance test using Scopolamine as amnesing drug after 1st day2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs.
AID77631In vitro functional studies in guinea pig ileum1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1185257Displacement of [3H]-NMS from human muscarinic M2 Y104A mutant expressed in Flp-In-CHO cells by liquid scintillation counting2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
AID187332Effect on number of animal not entering dark chamber after administration of 1 mg/kg of the compound2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Design of new cognition enhancers: from computer prediction to synthesis and biological evaluation.
AID1167264Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID723606Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID226399Muscarinic receptor binding comparison to QNB, Relative binding index(RBI)1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Analogues of 3-quinuclidinyl benzilate.
AID361986Lipophilicity, log D of compound at pH 7.4 by shake flask method2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Determination of log D via automated microfluidic liquid-liquid extraction.
AID131284Cognition enhancing activity was evaluated by mouse passive-avoidance test using Scopolamine as amnesing drug after 2nd day2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs.
AID62885The ability to displace [3H]spiroperidol from Dopamine receptor in striatum of rat brain membrane was determined; Not tested1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID141707Binding affinity towards rat Muscarinic acetylcholine receptor M1 was determined1997Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways.
AID127581Change in entry latency expressed as [(latency on day 2)-(latency on day 1)]2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity.
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.
AID723605Selectivity index, ratio of Ki for human M2 muscarinic receptor to Ki for human M5 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID1185261Displacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation counting2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
AID204449Inhibitory activity against sigma receptor isolated from guinea pig brain cortex membrane using [3H]DTG as radioligand; Inactive1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID179848Tested for efficiency in responding in radial maze test in rat on the day after treatment at 1 mg/kg sc along with Scopolamine at 50 ug/kg sc1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1167244Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID133093Minimum effective dose administered intraperitoneally in mouse passive avoidance test2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Molecular simplification of 1,4-diazabicyclo[4.3.0]nonan-9-ones gives piperazine derivatives that maintain high nootropic activity.
AID1167263Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID138625Latency time on 1st day of mouse passive-avoidance test.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Design, synthesis, and preliminary pharmacological evaluation of 1, 4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents.
AID142922Binding affinity towards Muscarinic acetylcholine receptor M1 was determined in calf brain membrane1997Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways.
AID196039Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation; Not tested1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1330792Hepatotoxicity in Kunming mouse assessed as increase in number of inflammatory cells in portal fields of liver at 3 mg/kg, po for 6 days by hematoxylin and eosin-staining based microscopic analysis2016European journal of medicinal chemistry, Nov-10, Volume: 123Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
AID141681Displacement of [3H]QNB from Muscarinic acetylcholine receptor of rat brain membrane1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
AID723607Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
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.
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.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID179850Tested for efficiency in responding in radial maze test in rat on the day of treatment at 1 mg/kg sc along with Scopolamine at 50 ug/kg sc1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1479895Antagonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by carbachol induction measured afte2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
AID224355Ability to reverse scopolamine-induced amnesia in a passive avoidance test to assess memory impairment administered perorally 1 mg/kg (no. of mice)1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
(R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment.
AID723848Displacement of [3H]NMS from human M5 muscarinic receptor expressed in CHO-K1 cells2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID176599In vitro activity against oxotremorine induced salivation in rat (iv)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID118785Compound was tested for cognitive activity by measuring retention for passive avoidance learning in mice at dose 0.63 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID1167258Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID232627Ratio of inhibitory activity against [3H]quinuclidinyl benzilate (QNB) binding in the absence of Zn to in the presence of Zn1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1167268Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID133185Tested for physostigmine lethality at a dose of 1 mg/kg after oral administration in mice1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID118796Compound was tested for cognitive activity by measuring retention for passive avoidance learning in mice at dose 1.25 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID134595LD50 in mice following i.v. administration.1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 2. Non-glycolates.
AID1148059Toxicity in sc dosed albino mouse assessed as mydriasis1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 1. Glycolates.
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.
AID142941Binding affinity towards rat Muscarinic acetylcholine receptor M2 was determined1997Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways.
AID190635Tested for running time in radial maze test in rat on the day before treatment at 1 mg/kg sc along with Scopolamine at 50 ug/kg sc1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID1167235Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID268587Antiamnesic effect in passive avoidance step-down task paradigm in rat assessed as number of mistakes at 0.4 mg/kg, ip2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
Synthesis and efficacy of 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives for acetylcholinesterase inhibition, as a stimulant of central cholinergic neurotransmission in Alzheimer's disease.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID511767Antidementia against scopolamine-induced cognitive impairment in Swiss albino mouse assessed as improvement in latency to transfer from bright to dark compartment at 20 umol/kg, po by passive avoidance 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.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID114184Effective dose against, administration in mice; Not tested1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID131285Difference between entry latency of cognition enhancing activity between 2nd day and 1st day2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs.
AID134633Cognition enhancing activity was evaluated by mouse passive-avoidance test using Scopolamine as amnesing drug administered intraperitoneally2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs.
AID141614In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID32094Inhibitory activity against acetylcholinesterase in rat striatal preparation1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID179849Tested for efficiency in responding in radial maze test in rat on the day before treatment at 1 mg/kg sc along with Scopolamine at 50 ug/kg sc1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
Synthesis and pharmacological activity of a series of dihydro-1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-diones, a novel class of potent cognition enhancers.
AID723845Orthosteric antagonist activity at human M5 muscarinic receptor expressed in CHO-K1 cells assessed as inhibition of [3H]NMS binding at saturation concentration relative to untreated control2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID723604Selectivity index, ratio of Ki for human M3 muscarinic receptor to Ki for human M5 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
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.
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.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7,114)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903113 (43.76)18.7374
1990's1428 (20.07)18.2507
2000's1048 (14.73)29.6817
2010's1146 (16.11)24.3611
2020's379 (5.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials563 (7.46%)5.53%
Trials0 (0.00%)5.53%
Reviews224 (2.97%)6.00%
Reviews1 (6.67%)6.00%
Case Studies262 (3.47%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other6,499 (86.10%)84.16%
Other14 (93.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]