Page last updated: 2024-11-05

benactyzine

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

Description

Benactyzine is an anticholinergic drug with anxiolytic and sedative properties. It was initially synthesized in the 1950s and has been used to treat anxiety disorders, but its use has declined due to concerns about its side effects. Benactyzine is a noncompetitive antagonist of the muscarinic acetylcholine receptors, particularly the M1 and M2 subtypes. Its effects are attributed to its ability to block acetylcholine transmission in the central nervous system, leading to a reduction in anxiety and a calming effect. It is studied for its potential to treat anxiety, insomnia, and other neurological disorders, however, due to its complex pharmacological profile and side effects, it is not widely used in clinical practice.'

Benactyzine: A centrally acting muscarinic antagonist. Benactyzine has been used in the treatment of depression and is used in research to investigate the role of cholinergic systems on behavior. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9330
CHEMBL ID70352
CHEBI ID94775
SCHEMBL ID49077
MeSH IDM0002303

Synonyms (68)

Synonym
benzeneacetic acid, .alpha.-hydroxy-.alpha.-phenyl-, 2-(diethylamino)ethyl ester
benzilic acid, 2-(diethylamino)ethyl ester
benactyzine
302-40-9
2-(diethylamino)ethyl hydroxy(diphenyl)acetate
benactyzin
alpha-hydroxy-alpha-phenylbenzeneacetic acid 2-(diethylamino)ethyl ester
brn 2156821
benacticina [inn-spanish]
benactyzinum [inn-latin]
diphenylglycolic acid 2-(diethylamino)ethyl ester
einecs 206-123-8
benzactyzine
2-(diethylamino)ethyl diphenylglycolate
2-diethylaminoethyl benzilate
2-(diethylamino)ethyl benzilate
benactizina [italian]
hsdb 3292
benactyzine [inn:ban]
benzeneacetic acid, alpha-hydroxy-alpha-phenyl-, 2-(diethylamino)ethyl ester
benactizina [dcit]
benzilic acid beta-diethylaminoethyl ester
diethylaminoethyl benzilate
benactyzine (inn)
D07498
NCGC00159434-02
NCGC00159434-03
hydroxy-diphenyl-acetic acid 2-diethylamino-ethyl ester(benactyzine)
bdbm50144504
hydroxy-diphenyl-acetic acid 2-diethylamino-ethyl ester
CHEMBL70352 ,
NCGC00159434-04
benactizina
unii-595eg71r3f
benactyzinum
595eg71r3f ,
benacticina
4-10-00-01263 (beilstein handbook reference)
cas-302-40-9
dtxcid202644
dtxsid0022644 ,
tox21_111665
benactyzine [inn]
benactyzine [vandf]
benactyzine [who-dd]
benactyzine [mi]
benactyzine [hsdb]
SCHEMBL49077
tox21_111665_1
2-(diethylamino)ethyl hydroxy(diphenyl)acetate #
benzilic acid .beta.-diethylaminoethyl ester
2-diethylaminoethyl benizilate
.alpha.-hydroxy-.alpha.-phenylbenzeneacetic acid 2-(diethylamino)ethyl ester
.beta.-diethylaminoethyl benzilate
diethyl(2-hydroxyethyl)amine benzilate
IVQOFBKHQCTVQV-UHFFFAOYSA-N
DB09023
CHEBI:94775
2-hydroxy-2,2-diphenylacetic acid 2-(diethylamino)ethyl ester
STL509562
Q4083674
2-(diethylamino)ethyl 2-hydroxy-2,2-diphenylacetate
diazil; diethylaminoethyl benzilate; beta-diethylaminoethyl benzilate
fortran
AKOS037490135
diazil; diethylaminoethyl benzilate; -diethylaminoethyl benzilate
EN300-22905669
Z242331154

Research Excerpts

Overview

Benactyzine is a combined anticholinergic, anti-NMDA compound. It has been used in past years in psychiatry, but is little used today.

ExcerptReferenceRelevance
"Benactyzine is a combined anticholinergic, anti-NMDA compound."( Synthesis and preliminary biological evaluation of gabactyzine, a benactyzine-GABA mutual prodrug, as an organophosphate antidote.
Daniels, D; Eisenkraft, A; Guez, D; Krivoy, A; Last, D; Makarovsky, I; Mardor, Y; Nudelman, A; Shneor, R; TaShma, Z; Weitman, M, 2022
)
1.68
"Benactyzine is an anticholinergic agent which has been used in past years in psychiatry, but is little used today. "( Effects of an anticholinergic drug, benactyzine hyrochloride, on vision and vision performance.
Adams, AJ; Brown, B; Haegerstrom-Portnoy, G; Jampolsky, A; Jones, RT, 1982
)
1.98

Toxicity

The LD50 was determined by a shift of the LD50 for the two OP agents. Maximum protection was observed with the cholinolytic benactyzine. An additive toxic effect of atropine was suggested with its combinations with TMB4, mecamylamine, and diazepam.

ExcerptReferenceRelevance
" Maximum protection, as determined by a shift of the LD50 for the two OP agents, was observed with the cholinolytic benactyzine."( Actions and interactions of cholinolytics and cholinesterase reactivators in the treatment of acute organophosphorus toxicity.
Asthana, SN; Batra, BS; Chowdhri, BL; Das Gupta, S; Ghosh, AK, 1991
)
0.49
" An additive toxic effect of atropine was suggested with its combinations with TMB4, mecamylamine, and diazepam, whereas no additive toxicity occurred with combinations involving hexamethonium or benactyzine (i."( Efficacy and toxicity of drug combinations in treatment of physostigmine toxicosis.
Klemm, WR, 1983
)
0.45
"A computer program (Q-test) was used to evaluate the combined toxic effects of nerve agent GF and its combined form with sarin (GB/GF) in mice."( Evaluation of combined toxic effects of GB/GF and efficacy of jielin injection against combined poisoning in mice.
Liang, J; Luo, C, 1997
)
0.3
" The results from these studies are far from unambiguous, since pyridostigmine may produce adverse effects on behavior in animals in relatively high doses, but not in a consistent way."( Pretreatment and prophylaxis against nerve agent poisoning: Are undesirable behavioral side effects unavoidable?
Aas, P; Myhrer, T, 2016
)
0.43
" We further evaluated the efficacy of two different antidotal regimens, one comprising a single and the other repeated administration of antidotes, in countering the toxic effects of the exposure."( Repetitive antidotal treatment is crucial in eliminating eye pathology, respiratory toxicity and death following whole-body VX vapor exposure in freely moving rats.
Bloch-Shilderman, E; Cohen, L; Egoz, I; Gez, R; Gutman, H; Nili, U; Rabinovitz, I; Yacov, G, 2019
)
0.51

Compound-Compound Interactions

Methoxime combined with atropine, benactyzine and natrium thiosulphate was studied in tabun-poisoned mice. In the experiments performed in rats, under effect of ethinyl estradiol and norethisteron acetate, the first signs of overmaturation are revealed in oocytes situating in the follicular cavity. PANPAL pretreatment did not improve the efficacy of HI-6 in combination with benactzine on soman-induced anticholinesterase and stressogenic effects.

ExcerptReferenceRelevance
" In the experiments performed in rats, under effect of ethinyl estradiol and norethisteron acetate, and especially at their combination with benactyzine, the first signs of overmaturation are revealed in oocytes situating in the follicular cavity."( [Effect of an estrogen-progestin preparation alone and in combination with amizil on the structure and electrophoretic parameters of oocytes and early rat embryos].
Kitaev, EM; Lupanova, GE; Makusheva, VP; Snetkova, MG, 1987
)
0.47
"Atropine, in combination with 1 of 6 other drugs, was tested in mice for the ability to prevent death by an otherwise lethal dose of the cholinesterase inhibitor, physostigmine."( Efficacy and toxicity of drug combinations in treatment of physostigmine toxicosis.
Klemm, WR, 1983
)
0.27
"In male rat experiments, the therapeutic effect of oxime HI-6 and its derivatives (HI-6 ester and amide) in combination with benactyzine on the cholinergic and stressogenic effects of a sublethal dose of soman was compared."( [Comparison of the effect of HI-6 oxime and its derivatives in combination with benactyzine on cholinergic and stress effects of soman in rats].
Kassa, J, 1996
)
0.73
" PANPAL pretreatment did not improve the efficacy of HI-6 in combination with benactyzine on soman-induced anticholinesterase and stressogenic effects."( The influence of pharmacological pretreatment on efficacy of HI-6 oxime in combination with benactyzine in soman poisoning in rats.
Bajgar, J; Kassa, J, 1996
)
0.74
"The effect of methoxime combined with a) atropine, b) benactyzine, c) atropine and natrium thiosulphate, d) atropine and diazepam on antidotal treatment effectiveness was studied in tabun-poisoned mice."( Effect of methoxime combined with anticholinergic, anticonvulsant or anti-HCN drugs in tabun-poisoned mice.
Sevelová, L; Vachek, J, 2003
)
0.57

Bioavailability

ExcerptReferenceRelevance
"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
" Best therapeutic efficiency was shown by HGG-42 in a dosage of 30 muMol/kg."( Therapeutic effects of the bis-pyridinium salts HGG-12, HGG-42, and atropine, benactyzine in organophosphate poisoning of dogs.
Hauser, W; Weger, N, 1979
)
0.49
" With increase of antidepressants dosage received by a subordinate rat its competing ability becomes enhanced too; this may cause a change in domination."( [Effect of pharmacologic substances on the dominance-submission relationship in a pair of rats].
Kampov-Polevoi, AB, 1978
)
0.26
" Pharmacological evaluation using dose-response experiments on isolated rat ileum tissue demonstrated that these compounds noncompetitively inhibited acetylcholine-induced ileum contractions."( Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine.
Bhargava, HN; Flavin, MT; Lu, MC; Thompson, EB, 1987
)
0.48
" In contrast, benactyzine and trihexyphenidyl showed a third profile of activity: There was a smaller increase in drug dosage required for anticonvulsant activity as seizure duration increased, and both drugs could terminate seizures that had progressed for 40 min."( Pharmacological modulation of soman-induced seizures.
McDonough, JH; Shih, TM, 1993
)
0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency12.95180.006038.004119,952.5996AID1159521; AID1159523
TDP1 proteinHomo sapiens (human)Potency9.84750.000811.382244.6684AID686978; AID686979
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.48710.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency5.81720.000214.376460.0339AID720691; AID720692
cytochrome P450 2D6Homo sapiens (human)Potency5.49500.00108.379861.1304AID1645840
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency15.84890.01789.637444.6684AID588834
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.00290.005612.367736.1254AID624032
[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)
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki1.00000.00000.490110.0000AID204635
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
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.
AID1508628Confirmatory 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.
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.
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.
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.
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.
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.
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.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID204635Binding affinity for Sigma receptor type 1,using [3H](+)-pentazocine as radioligand2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Thioxanthene-derived analogs as sigma(1) receptor ligands.
AID77620Antimuscarinic activity was assayed for its ability to block the acetyl-choline induced contraction of the guinea pig ileum1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
AID197429Antimuscarinic potency is measured as its ability to block ACh-induced contractions of the rat ileum.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Molecular modification of anticholinergics as probes for muscarinic receptors. 3. Conformationally restricted analogues of benactyzine.
AID79352Antimuscarinic activity was assayed for its ability to block the acetyl-choline induced contraction of the guinea pig ileum1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
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.
AID204767Binding affinity of compound was measured towards Sigma receptor type 2 by using [3H]ditolylguanidine as radioligand2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Thioxanthene-derived analogs as sigma(1) receptor ligands.
AID157520Inhibition of carbachol-induced release of alpha-amylase from pancreatic acini from rat was determined1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (461)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990402 (87.20)18.7374
1990's27 (5.86)18.2507
2000's17 (3.69)29.6817
2010's8 (1.74)24.3611
2020's7 (1.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.87

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.87 (24.57)
Research Supply Index6.53 (2.92)
Research Growth Index4.22 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (3.46%)5.53%
Reviews10 (1.51%)6.00%
Case Studies2 (0.30%)4.05%
Observational0 (0.00%)0.25%
Other629 (94.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]