Page last updated: 2024-12-08

dironyl

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

Description

dironyl: pronounced antifertility agent in rats; lactation suppressor in other species; serotonin antagonist; RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID443951
CHEMBL ID73151
CHEBI ID32193
SCHEMBL ID147259
MeSH IDM0048502

Synonyms (77)

Synonym
CHEMBL73151 ,
3-[(6ar,9s,10ar)-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinoline-9-yl]-1,1-diethylurea
gtpl56
sh-406
zk-31224
MLS000069833 ,
transdihydrolisuride
vufb-6638
smr000058934
mysalfon
teluron
trans-dihydrolisuride
terguride
BSPBIO_000834
PRESTWICK2_000945
AB00514698
teluron (tn)
37686-84-3
D01348
terguride (jan/inn)
BPBIO1_000918
(+)-terguride
brn 0766582
6-methyl-8alpha-(diethylcarbamoylamino)ergoline
zk 31224
terguridum [latin]
einecs 253-624-2
1-((5r,8s,10r)-6-methyl-8-ergolinyl)-3,3-diethylurea
(+)-(5r,8s,10r)-terguride
terguride [inn]
(5r,8s,10r)-terguride
9,10-alpha-dihydrolisuride
dironyl
1,1-diethyl-3-(6-methylergolin-8alpha-yl)urea
n,n-diethyl-n'-(d-6-methyl-10alpha-isoergolin-8-yl)urea
tergurida [spanish]
urea, n,n-diethyl-n'-((8-alpha)-6-methylergolin-8-yl)-
SPBIO_003069
PRESTWICK0_000945
PRESTWICK1_000945
PRESTWICK3_000927
HMS1570N12
s(+)-terguride
1,1-diethyl-3-(7-methyl-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-yl)-urea
bdbm50017519
NCGC00179409-02
dtxsid3045809 ,
dtxcid1025809
tox21_111283
HMS2232H10
tergurida
terguridum
unii-21ojt43q88
21ojt43q88 ,
trans-dihydro lisuride
tdhl
1,1-diethyl-3-(6-methylergolin-8.alpha.-yl)urea
terguride [mart.]
terguride [jan]
terguride [who-dd]
terguride [mi]
SCHEMBL147259
JOAHPSVPXZTVEP-YXJHDRRASA-N
1,1-diethyl-3-(6-methyl-8alpha-ergolinyl)urea
8alpha-(3,3-diethylureido)-6-methylergoline
s(+)-n,n-diethyl-n'([8alpha]-6-methylergolin-8-yl)urea
OPERA_ID_1172
J-523241
n,n-dethyl-n'-[(8alpha)-6-methylergoln-8-yl]urea
CHEBI:32193
3-[(6ar,9s,10ar)-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinolin-9-yl]-1,1-diethylurea
s(+)-n,n-diethyl-n([8alpha]-6-methylergolin-8-yl)urea
DB13399
KS-1464
Q7702355
tergurid; terguride; trans-dihydrolisuride
AKOS037653997

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Only those adverse events already known to be side effects of terguride were observed."( Evaluation of the efficacy and safety of terguride in patients with fibromyalgia syndrome: results of a twelve-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.
Bendszus, M; Distler, O; Dokoupilova, E; Dvorak, Z; Eich, W; Fleck, M; Gaubitz, M; Hechler, M; Jansen, JP; Krause, A; Müller-Ladner, U; Pache, L; Reiter, R, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
" injection, the concentration of TDHL declined with a half-life of 37 +/- 19 min."( Pharmacokinetics and pharmacodynamics of the ergot derivative, transdihydrolisuride, in man.
Dorow, R; Hasan, SH; Krause, W; Nieuweboer, B, 1984
)
0.27

Bioavailability

ExcerptReferenceRelevance
" The bioavailability was around 20%."( Pharmacokinetics of 3H-terguride in elderly volunteers.
Krause, W; Kühne, G; Seifert, W, 1991
)
0.28
" The oral bioavailability of terguride over all doses was about 20%."( Pharmacokinetics and endocrine effects of terguride in healthy subjects.
Dorow, R; Gräf, KJ; Krause, W; Kühne, G; Sauerbrey, N; Träger, H, 1990
)
0.28
" The bioavailability of terguride was 79% in the rat and 15% in the monkey."( Pharmacokinetics of the dopamine partial agonist, terguride, in the rat and rhesus monkey.
Hümpel, M; Krause, W,
)
0.13
" The bioavailability of oral TDHL was proportional to the dose; after 200, 400 and 800 micrograms the bioavailability was 20 +/- 25%, 31 +/- 24% and 48 +/- 26%."( Pharmacokinetics and pharmacodynamics of the ergot derivative, transdihydrolisuride, in man.
Dorow, R; Hasan, SH; Krause, W; Nieuweboer, B, 1984
)
0.27
"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
"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 neuroleptic dosage was kept constant."( Treatment of extrapyramidal side effects with terguride.
Filip, V; Hálková, E; Karen, P; Marsálek, M, 1992
)
0.28
" In no case the antagonism was competitive: the control dose-response curves were not shifted in a parallel and dose-dependent manner."( [Effects of the partial dopamine receptor agonist, terguride, on the field-stimulated vas deferens in the mouse].
Carratù, MR; Conte-Camerino, D; De Serio, A; Ferrari, E; Lagioia, R; Mitolo-Chieppa, D, 1990
)
0.28
" Throughout the treatment terguride was well tolerated without any side effects up to a maximal daily dosage of 3 mg given orally."( Rapid regression of macroprolactinomas by the new dopamine partial agonist terguride.
Dorow, R; Gräf, KJ; Horowski, R; Köhler, D, 1986
)
0.27
" The dissociation constant (K(B)) and relative intrinsic efficacy (E(r)) for each partial agonist were calculated using a partial agonist interaction null model in which the effects of fixed concentrations of each partial agonist on the dopamine dose-response curve were evaluated."( Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells.
Abell, C; Avalos, M; Kwan, SW; Mak, C; Randall, PK; Trzeciakowski, JP; Wilcox, RE,
)
0.13
" Although this model could be improved, it could explain the long duration of the antihyperprolactinemic activity of terguride and might be useful for designing its rational dosage regimen."( [Pharmacokinetic/pharmacodynamic analysis of anti-hyperprolactinemic effect of terguride based on dopamine D2 receptor occupancy].
Iga, T; Irizuki, N; Sawada, Y; Takayanagi, R; Yamada, Y; Yamamoto, K, 2003
)
0.32
" Over 21 days, the dosage was titrated to a maximum daily dose of 3 mg of terguride or placebo, and this fixed dosage was continued over 9 weeks."( Evaluation of the efficacy and safety of terguride in patients with fibromyalgia syndrome: results of a twelve-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.
Bendszus, M; Distler, O; Dokoupilova, E; Dvorak, Z; Eich, W; Fleck, M; Gaubitz, M; Hechler, M; Jansen, JP; Krause, A; Müller-Ladner, U; Pache, L; Reiter, R, 2010
)
0.36
" Here we use these as case studies to emphasize the importance of informed drug target selection, the early evaluation of dose-response relationships in human studies, and the value of the deep phenotyping of patients in clinical studies to better understand inter-individual variation in patient response."( Why drugs fail in clinical trials in pulmonary arterial hypertension, and strategies to succeed in the future.
Attard, M; Ghataorhe, P; Lythgoe, MP; Rhodes, CJ; Wharton, J; Wilkins, MR, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.12510.631035.7641100.0000AID504339
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686979
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency4.46680.707912.194339.8107AID720542
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.78280.01237.983543.2770AID1346984
pregnane X nuclear receptorHomo sapiens (human)Potency25.11890.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency21.13170.000229.305416,493.5996AID743079
aryl hydrocarbon receptorHomo sapiens (human)Potency31.03990.000723.06741,258.9301AID743085; AID743122
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency27.48220.000323.4451159.6830AID743065; AID743067
importin subunit beta-1 isoform 1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency35.48130.425612.059128.1838AID504891
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.43280.050127.073689.1251AID588590
DNA polymerase kappa isoform 1Homo sapiens (human)Potency100.00000.031622.3146100.0000AID588579
VprHuman immunodeficiency virus 1Potency14.12541.584919.626463.0957AID651644
D(3) dopamine receptor isoform eHomo sapiens (human)Potency0.00790.02009.148539.8107AID720506
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[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)
DRattus norvegicus (Norway rat)IC50 (µMol)0.06900.00030.50267.7625AID61177
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.02500.00031.38338.4000AID3753
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00400.00010.54948.4000AID64292
[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)
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC50 (µMol)92.50700.13203.30049.5690AID624499
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC50 (µMol)0.00380.00381.36218.3930AID624503
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1345788Human D2 receptor (Dopamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1345833Human D3 receptor (Dopamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1345814Human D4 receptor (Dopamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID624218Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID624235Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A2002The Journal of pharmacology and experimental therapeutics, Nov, Volume: 303, Issue:2
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID3753In vitro binding activity against 5-hydroxytryptamine 1A receptor from homogenized rat brain, using [3H]-8-OH-DPAT as the radioligand1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.
AID250135Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID64292In vitro binding activity against dopamine receptor D2 from homogenized rat brain, using [3H]spiperone as the radioligand1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.
AID61177In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (149)

TimeframeStudies, This Drug (%)All Drugs %
pre-199047 (31.54)18.7374
1990's45 (30.20)18.2507
2000's34 (22.82)29.6817
2010's21 (14.09)24.3611
2020's2 (1.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.13

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

MetricThis Compound (vs All)
Research Demand Index9.13 (24.57)
Research Supply Index5.17 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials18 (11.46%)5.53%
Reviews8 (5.10%)6.00%
Case Studies6 (3.82%)4.05%
Observational0 (0.00%)0.25%
Other125 (79.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]