Page last updated: 2024-11-04

talipexole

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

Description

talipexole: dopamine receptor agonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5374
CHEMBL ID279085
CHEBI ID93327
SCHEMBL ID49817
MeSH IDM0083316

Synonyms (50)

Synonym
BRD-K75615183-001-01-7
talipexole
BPBIO1_001257
BIOMOL-NT_000038
NCGC00163160-01
bht920
talipexole [inn]
6-allyl-2-amino-5,6,7,8-tetrahydro-4h-thiazolo(4,5-d)azepine
talipexol [spanish]
talipexolum [latin]
NCGC00163160-02
CHEMBL279085 ,
L001140
101626-70-4
talipexole (inn)
D08558
6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine
NCGC00163160-03
unii-7am2j46z1y
7am2j46z1y ,
talipexol
talipexolum
cas-101626-70-4
tox21_112020
dtxcid6026321
dtxsid8046321 ,
cid_5374
cas_101626-70-4
nsc_104870
bdbm86053
SR-01000722008-2
sr-01000722008
FT-0631016
b-ht920
gtpl5442
6-(prop-2-en-1-yl)-4h,5h,6h,7h,8h-[1,3]thiazolo[4,5-d]azepin-2-amine
talipexole [mi]
talipexole [who-dd]
HY-A0040
SCHEMBL49817
NCGC00163160-04
tox21_112020_1
AKOS030526065
6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine
CHEBI:93327
6-allyl-5,6,7,8-tetrahydro-4h-thiazolo[4,5-d]azepin-2-amine
Q7679540
C13994
p-tolylacetylchloride
4h-thiazolo[4,5-d]azepin-2-amine, 5,6,7,8-tetrahydro-6-(2-propen-1-yl)-

Research Excerpts

Overview

Talipexole is a non-ergot dopamine (DA) agonist that has been used in the treatment of Parkinson's disease. It has putative preferential activity on presynaptic dopamine receptors.

ExcerptReferenceRelevance
"Talipexole is a non-ergot dopamine (DA) agonist that has been used in the treatment of Parkinson's disease. "( The neuroprotective effect of talipexole from paraquat-induced cell death in dopaminergic neuronal cells.
Bravo-San Pedro, JM; Fuentes, JM; Gómez-Sánchez, R; González-Polo, RA; Niso-Santano, M; Soler, G, 2010
)
2.09
"Talipexole is a new dopamine autoagonist with putative preferential activity on presynaptic dopamine receptors. "( Talipexole and adult Gilles de la Tourette's syndrome: double-blind, placebo-controlled clinical trial.
Goetz, CG; Stebbins, GT; Thelen, JA, 1994
)
3.17

Effects

ExcerptReferenceRelevance
"Talipexole hydrochloride has been on market in Japan recently, but MAO-B inhibitors and COMT inhibitors are in final stages to wait evaluations by the governmental committee."( [Clinical characteristics and trends in research of Parkinson's disease and parkinsonism in Japan].
Yanagisawa, N, 1997
)
1.02

Actions

ExcerptReferenceRelevance
"Talipexole did also not produce an inhibition when tritium overflow was evoked by NMDA in the presence of omega-conotoxin GVIA 0.1 mumol/l; the latter, by itself, decreased the response to NMDA by about 55%.(ABSTRACT TRUNCATED AT 250 WORDS)"( Modulation of N-methyl-D-aspartate (NMDA)-stimulated noradrenaline release in rat brain cortex by presynaptic alpha 2-adrenoceptors.
Fink, K; Göthert, M, 1993
)
1.01

Treatment

Talipexole pretreatment prevents the reduction in the anti-apoptotic Bcl-x(L) protein and increases in the pro-APoptotic form of Bak and p-Bad, both induced by PQ. The talipexoles had no effect on levels of proapoptotics Bax, Bak, and Bad.

ExcerptReferenceRelevance
"Talipexole pretreatment prevents the reduction in the anti-apoptotic Bcl-x(L) protein and increases in the pro-apoptotic form of Bak and p-Bad, both induced by PQ."( The neuroprotective effect of talipexole from paraquat-induced cell death in dopaminergic neuronal cells.
Bravo-San Pedro, JM; Fuentes, JM; Gómez-Sánchez, R; González-Polo, RA; Niso-Santano, M; Soler, G, 2010
)
1.37
"The talipexole pretreatment induced an increase in antiapoptotic Bcl-2 protein level but had no effect on levels of proapoptotic Bax, Bak, and Bad."( Protective effects of the antiparkinsonian drugs talipexole and pramipexole against 1-methyl-4-phenylpyridinium-induced apoptotic death in human neuroblastoma SH-SY5Y cells.
Kakimura, JI; Kitamura, Y; Kohno, Y; Kosaka, T; Matsuoka, Y; Nomura, Y; Taniguchi, T, 1998
)
1.04

Pharmacokinetics

ExcerptReferenceRelevance
" Doxazosin has a longer terminal elimination half-life than prazosin."( Pharmacokinetic and pharmacodynamic studies with two alpha-adrenoceptor antagonists, doxazosin and prazosin in the rabbit.
Hamilton, CA; Reid, JL; Vincent, J, 1985
)
0.27
" Pharmacokinetic parameters C(max), t(max), t(1/2z), mean residence time (MRT), AUC(0-tau), AUC(0-infinity), CL(z)/F and V(z)/F were determined under the non-compartmental model."( Pharmacokinetic profile of talipexole in healthy volunteers is not altered when it is co-administered with Madopar (co-beneldopa).
Hang, TJ; Jia, L; Song, M; Wen, AD; Xu, XF; Yang, L; Zhang, TT, 2009
)
0.65
" For talipexole hydrochloride, there were no significant differences in the pharmacokinetic values between the two administrations."( Pharmacokinetic profile of talipexole in healthy volunteers is not altered when it is co-administered with Madopar (co-beneldopa).
Hang, TJ; Jia, L; Song, M; Wen, AD; Xu, XF; Yang, L; Zhang, TT, 2009
)
1.16

Compound-Compound Interactions

ExcerptReferenceRelevance
"The present experiments were performed to investigate the effects of dopamine D1 receptor agonists given alone or in combination with dopamine D2 receptor agonists on body temperature in rats."( Hyperthermia induced by the dopamine D1 receptor agonist SK&F38393 in combination with the dopamine D2 receptor agonist talipexole in the rat.
Furukawa, T; Kimura, H; Matsumoto, S; Nagashima, M; Yamada, K, 1992
)
0.49
"We examined whether or not the antiparkinsonian activity of talipexole (B-HT 920, 6-allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]-azepine) could be optimised by combination with L-3,4-dihydroxyphenylalanine (L-dopa)."( Antiparkinsonian activity of talipexole in MPTP-treated monkeys: in combination with L-dopa and as chronic treatment.
Fukuda, T; Irifune, M; Nomoto, M, 1994
)
0.82

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
" CEC treatment had little effect on the pressor dose-response curve of either phenylephrine or BHT 920."( Effect of chlorethylclonidine on arterial blood pressure and heart rate in the conscious rat.
Piascik, MT; Pruitt, TA; Sparks, MS, 1992
)
0.28
" Treatment with captopril was found to attenuate pressor responses produced by the administration of either alpha 1- or alpha 2-adrenoceptor agonists, resulting in the displacement to the right of the agonist dose-response curves and significantly increasing the calculated ED50 values."( The interrelationship between the effects of captopril and nifedipine on pressor responses elicited by selective alpha-adrenoceptor agonists in the pithed rat preparation.
Tabrizchi, R; Triggle, CR, 1992
)
0.28
" Since the behavioural effects of B-HT 920 vary according to the dosage employed, discussion centres on what receptors might conceivably underly these effects and on their preclinical relevance."( Effects of B-HT 920 in the tail-suspension test.
Cassinadri, M; Ferrari, F; Tampieri, A; Tartoni, PL, 1991
)
0.28
" The ED50 value for the dose-response curves to B-HT 920 and St587 were found to be significantly increased after the administration of staurosporine."( Effects of staurosporine on the pressor responses to alpha-adrenoceptor agonists in pithed rats: a comparison with nifedipine.
Tabrizchi, R; Triggle, CR, 1991
)
0.28
" Both milrinone and pertussis toxin shifted the blood pressure dose-response curves of B-HT 920 to the right, but the responses to angiotensin II were decreased after milrinone pretreatment only."( Cardiovascular responses to milrinone in pertussis toxin-pretreated pithed rats.
De Wildt, DJ; Porsius, AJ; Van Rooij, HH; Verrijk, R; Wemer, J, 1990
)
0.28
" Similarly, increased plasma renin activity induced by chronic salt depletion (0% NaCl) in pithed rats provoked a shift to the right of the dose-response curves to Ang II and ET-1 but not to MTX."( Cross-desensitization between angiotensin II and endothelin-1 in the pithed rat.
Auguet, M; Braquet, P; Chabrier, PE; Etiemble, E; Guillon, JM; Roubert, P, 1991
)
0.28
" In all rings, cooling caused an increase in the slope of the dose-response curve and a significant increase in the concentration of agonist required to evoke contractions, as assessed by that concentration of NE required to evoke a contraction equal to 10% of maximal (EC10)."( Cooling augments alpha 2-adrenoceptor-mediated contractions in rat tail artery.
Bowman, CJ; Harker, CT; Ousley, PJ; Porter, JM, 1991
)
0.28
" Both vasodilators depressed the pressor dose-response curves to BHT 920, while sparing those to methoxamine."( Calcium entry blockade and alpha-adrenergic responsiveness in vivo.
Pedrinelli, R; Tarazi, RC, 1985
)
0.27
" Bay K 8644 (10(-8) M) markedly potentiated B-HT-958-mediated vasoconstrictor responses with a leftward shift and an increase in the maximum response of the logarithmic dose-response curve."( Sensitivity of alpha-adrenoceptor agonists to the calcium channel activator, Bay K 8644, in canine saphenous vein.
Eskinder, H; Gross, GJ, 1987
)
0.27
" Dose-response curves were generated for epinephrine, and were then repeated in the presence of either prazosin (alpha 1 antagonist), yohimbine (alpha 2 antagonist) or SK&F-86466 (alpha 2 antagonist)."( An in vivo evaluation of alpha adrenergic receptors in canine prostate.
Chernesky, CE; Chou, TC; Felsen, D; Marion, DN; Somers, WJ; Vaughan, ED, 1989
)
0.28
" Dose-response curves were generated for the relatively selective alpha 1-receptor agonist phenylephrine, the alpha 2-receptor agonist BHT-920, and the alpha 1- and alpha 2-receptor agonist norepinephrine."( Differences in alpha-adrenergic responsiveness between human internal mammary arteries and saphenous veins.
Grossman, W; Johnson, RG; Morgan, KG; Thurer, RL; Weinstein, JS; Weintraub, RM, 1989
)
0.28
" The absence of a depression of the maximum of the dose-response curve of ST 587 and the very moderate attenuation of the maximal B-HT 920-induced increase in diastolic blood pressure (BP) confirms the lack of major calcium entry blocking properties of R 56865 for alpha-adrenoceptor-activated calcium channels in vitro."( Interaction between R 56865 and alpha-adrenoceptors in the pithed rat.
Fruh, C; Koch, P; Peters, T; Schneider, J; Wilffert, B; Wilhelm, D,
)
0.13
" Its dose-response curve was bell-shaped with maximal effects at a dose of 100 micrograms/kg."( Occurrence of yawning and decrease of prolactin levels via stimulation of dopamine D2-receptors after administration of SND 919 in rats.
Domae, M; Furukawa, T; Matsumoto, S; Nagashima, M; Shirakawa, K; Yamada, K, 1989
)
0.28
" Dose-response curves to the dopaminergic agonist BHT920 showed that, during the infusion of 10(-7) M neurotensin, dopaminergic autoreceptors of some neurones were less sensitive than in control conditions."( Electrophysiological effects of neurotensin on dopaminergic neurones of the ventral tegmental area of the rat in vitro.
Dresse, A; Massotte, L; Seutin, V, 1989
)
0.28
" At 24 h post reserpine the dose-response curve of B-HT 920 (0."( Locomotor behaviour of selective dopamine agonists in mice: is endogenous dopamine the only catecholamine involved?
Pichler, L; Pifl, C, 1989
)
0.28
" In the rat tail artery, there were no differences in the dose-response relationships to noradrenaline, methoxamine, and KCl whether the agonists were applied as single or cumulative doses."( Desensitization of the vascular contractile response to cumulative doses of alpha 2-adrenoceptor agonists.
Cheung, DW, 1986
)
0.27
" Although administered in a dosage range 100 to 1000 times that of alpha-1 agonists, the alpha-2 agonists (B-HT 920, UK 14,304 and guanabenz) produced only minimal renal vasoconstriction before systemic pressor effects."( In vivo assessment of rat renal alpha adrenoceptors.
Gesek, FA; Strandhoy, JW; Wolff, DW, 1987
)
0.27
" Its dose-response curve was shifted to the right at 23 degrees C/0."( B-HT 920 and B-HT 958: presynaptic effects on electrically evoked 3H-dopamine release from slices of rat nucleus accumbens.
Cichini, G; Placheta, P; Singer, EA, 1987
)
0.27
" For remoxipride, the dose-response curve for antagonism of GBL-reversal was superimposable over that for antagonism of apomorphine-induced stereotypies, with an ED50 value about 12 times higher than that for antagonism of apomorphine-induced hyperactivity."( Comparison of the effects of haloperidol, remoxipride and raclopride on "pre"- and postsynaptic dopamine receptors in the rat brain.
Fowler, CJ; Magnusson, O; Mohringe, B; Ogren, SO; Wijkström, A, 1988
)
0.27
" B-HT920 was found to produce a dose-response profile qualitatively similar to, but weaker than, clonidine: low doses impaired memory and began to lower blood pressure and produce sedation, while high doses improved memory."( The alpha-2 adrenergic agonist guanfacine improves memory in aged monkeys without sedative or hypotensive side effects: evidence for alpha-2 receptor subtypes.
Arnsten, AF; Cai, JX; Goldman-Rakic, PS, 1988
)
0.27
" Coronary flow resistance increased in a dose-response fashion with a maximum increase of 22."( The differential effects of alpha 2-adrenergic stimulation on the myocardium and coronary vessels in the isolated rat heart.
Fouad-Tarazi, FM; Hirakata, H, 1988
)
0.27
"3 mg/kg) in presence of prazosin shifted the norepinephrine pressor dose-response curves to the right whereas it was ineffective in yohimbine-pretreated animals."( Calcium entry blockade by nitrendipine and alpha adrenergic responsiveness in vivo: comparison with noncalcium entry blocker vasodilators in absence and presence of phenoxybenzamine pretreatment.
Pedrinelli, R; Tarazi, RC, 1985
)
0.27
"In rat isolated perfused tail arteries, dose-response curves were established for the vasopressor effects of phenylephrine (alpha 1-adrenoceptor agonist), clonidine (alpha 1- and alpha 2-adrenoceptor agonist), clonidine in the presence of 10(-7) mol/l prazosin (alpha 2-agonist), and BHT-920 (alpha 2-agonist)."( Investigations into the nature of alpha 2-adrenoceptors in rat tail arteries.
Armsworth, SJ; Chapman, KL; Marwood, JF; Stokes, GS,
)
0.13
" Dose-response curves were constructed to noradrenaline (alpha 1/alpha 2), methoxamine (alpha 1-selective) and B-HT 920 (alpha 2-selective)."( Characterization of post-junctional alpha-adrenoceptors in the rat isolated perfused femoral artery.
Dyke, AC; Widdop, RE, 1987
)
0.27
" The log dose-response curve to methoxamine, an alpha 1-agonist, was shifted to the right whereas the vasopressor responses to BHT-920, an alpha 2-agonist, were unaffected by trifluoperazine."( Trifluoperazine antagonizes postsynaptic alpha 1-but not alpha 2-adrenoceptor-mediated pressor responses in the rat.
Mainguy, Y; Pruneau, D; Roy, F, 1984
)
0.27
" Hypotensive potency after intravenous administration to anesthetized, normotensive rats was determined as a measure of central alpha-adrenergic activity and expressed as pC25, obtained from log dose-response curves."( Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
de Jonge, A; Lam, E; Slothorst-Grisdijk, FP; Timmermans, PB; van Meel, JC; van Zwieten, PA, 1981
)
0.26
" Dose-response curves were generated for para-aminoclonidine in the presence of vehicle alone, yohimbine (alpha-2 antagonist), idazoxan (alpha-2/I1/I2 antagonist) and prazosin (alpha-1 antagonist)."( Identification, localization and functional analysis of imidazoline and alpha adrenergic receptors in canine prostate.
Breslin, DS; Ernsberger, P; Felsen, D; Marion, DN; May, M; Nejat, RJ; Nguyen, P; Sutaria, PM; Vaughan, ED, 1994
)
0.29
" Nifedipine (100 micrograms/kg, 300 micrograms/kg, and 1000 micrograms/kg) inhibited in a dose-dependent manner the pressor responses to the alpha 1- and alpha 2-adrenoceptor agonists, the dose-response curves to the alpha 2-adrenoceptor agonists being shifted further to the right."( A comparison of the effects of TMB-8 and nifedipine on pressor responses to alpha 1- and alpha 2-adrenoceptor agonists in pithed rats.
Aleixandre, MA; Pintado, A; Puerro, M, 1995
)
0.29
" The measured reduction in dopamine D2 receptor density after EEDQ was of the same magnitude as the reduction in receptor number predicted from the EEDQ induced shift in the dose-response curve of the full dopamine D2 receptor agonist NPA."( A high dose of EEDQ reduces pituitary dopamine D2 receptor density and the prolactin suppressive potency of agonists.
Ekman, A; Eriksson, E, 1993
)
0.29
" Dosage of concurrent neuroleptics was fixed at least 3 weeks prior to the trial and was unchanged throughout the study period."( B-HT 920, a dopamine D2 agonist, in the treatment of negative symptoms of chronic schizophrenia.
Inoue, T; Koyama, T; Matsubara, S; Ohmori, T; Yamashita, I, 1993
)
0.29
" The dosage of talipexole was gradually reduced and the drug was ultimately discontinued since incomplete neuroleptic malignant syndrome was suspected."( [Increase in serum creatine phosphokinase following administration of talipexole hydrochloride].
Imai, T; Osumi, E, 2000
)
0.89
" 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
") caused dose-dependent rightward shift in the pressor dose-response curve induced by B-HT 920."( alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator.
Hashimoto, A; Imaizumi, T; Kambe, T; Kishi, M; Mori, T; Nakazawa, T; Orito, K, 2001
)
0.31
" In the dose-response curves to ACh, maximum relaxation and ED50 were similar between FFR and CNT."( Impaired endothelial alpha-2 adrenergic receptor-mediated vascular relaxation in the fructose-fed rat.
Berger, ME; Golub, MS; Takagawa, Y; Tuck, ML, 2002
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
azepine
[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 (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
phosphopantetheinyl transferaseBacillus subtilisPotency94.00150.141337.9142100.0000AID1490; AID2701; AID2707
GLS proteinHomo sapiens (human)Potency15.84890.35487.935539.8107AID624170
Microtubule-associated protein tauHomo sapiens (human)Potency19.95260.180013.557439.8107AID1460
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.39140.000214.376460.0339AID720691
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.60320.000229.305416,493.5996AID743091
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.84890.035520.977089.1251AID504332
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency44.66840.354828.065989.1251AID504847
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.70790.009610.525035.4813AID1479145
[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)
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki1.35290.00000.437510.0000AID65737; AID65738
[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)92.47000.13203.30049.5690AID720642
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC50 (µMol)76.08300.00381.36218.3930AID720643
[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 (50)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID197167Hypotensive activity (25% decrease in arterial pressure) after i.v. administration to anesthetized normotensive rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID65738In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the antagonist [3H]spiperone + GTP to label the low affinity state (D2 low)1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
AID23716Partition coefficient (logD7.4)1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID65737In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the agonist [3H]quinpirole to label the high affinity state (D2 high)1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID33250Central hypotensive activity in anesthetized normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID33252Peripheral hypertensive activity in pithed normotensive rats.1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Characterization of alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral alpha-adrenoceptors.
AID73720Concentration-related inhibition of response to sympathetic nerve stimulation in isolated guinea pig atrium mediated by alpha-2 receptors1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of alpha 2-adrenoceptors.
AID36788Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 2.5*10e-81984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36721Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]-prazosin binding (0.2 nM) to rat isolated brain membranes by 50% was reported; 5*10e-41984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID230928Ratio of the binding affinity to low affinity state (D2 low) to high affinity state (D2 high)1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
AID23715Apparent partion coefficient of compound was evaluated in octanol/buffer at pH of 7.4 at 37 degree Centigrade1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (401)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990196 (48.88)18.7374
1990's157 (39.15)18.2507
2000's32 (7.98)29.6817
2010's10 (2.49)24.3611
2020's6 (1.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.75

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 Index19.75 (24.57)
Research Supply Index6.06 (2.92)
Research Growth Index4.17 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (0.47%)5.53%
Reviews7 (1.64%)6.00%
Case Studies4 (0.94%)4.05%
Observational0 (0.00%)0.25%
Other413 (96.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]