Page last updated: 2024-11-04

mazindol

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Description

Mazindol is a non-amphetamine, non-catecholamine, sympathomimetic drug with anorectic properties. It was synthesized in the 1960s and was initially marketed as an appetite suppressant. Mazindol is believed to exert its anorectic effects by stimulating the release of norepinephrine and dopamine in the central nervous system, which can lead to reduced appetite and increased energy expenditure. While mazindol was once widely prescribed for weight loss, its use has declined due to concerns about its potential for abuse and adverse effects. However, research continues to explore its potential therapeutic uses, including the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Mazindol's mechanisms of action, particularly its influence on neurotransmitter release and its potential interactions with other medications, remain areas of active investigation. Mazindol is also studied for its potential effects on cognitive function and mood regulation. While further research is needed, mazindol holds promise as a potential therapeutic agent in a variety of settings.'

Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4020
CHEMBL ID781
CHEBI ID6702
SCHEMBL ID27849
MeSH IDM0013149

Synonyms (96)

Synonym
HY-15279
mazindol
3h-imidazo[2,1-a]isoindol-5-ol, 5-(4-chlorophenyl)-2,5-dihydro-
5-(4-chlorophenyl)-2,5-dihydro-3h-imidazo[2,1-a]isoindol-5-ol
an-448 ,
dea no. 1605
hsdb 3112
mazindole
5h-imidazo(2,1-a)isoindol-5-ol, 5-(4-chlorophenyl)-2,3-dihydro
teronac
3h-imidazo(2,1-a)isoindol-5-ol, 5-(4-chlorophenyl)-2,5-dihydro-
3h-imidazo(2,1-a)isoindol-5-ol, 5-(4-chlorophenyl)-2,5-dihydro-, (+-)-
dimagrir
einecs 244-857-0
sanorex
5-p-chlorophenyl-2,3-dihydro-5h-imidazo(2,1-a)isoindol-5-ol
mazildene
s 42548
3h-imidazo(2,1-a)isoindol-5-ol, 5-(p-chlorophenyl)-2,5-dihydro-
3h-imidazo(2,1-a)isoindol-5-ol, 2,5-dihydro-5-(4-chlorophenyl)-
5-(4-chlorophenyl)-2,3-dihydro-5-hydroxy-5h-imidazo(2,1-a)isoindole
sah 42548
(+-)-5-(p-chlorophenyl)-2,5-dihydro-3h-imidazo(2,1-a)isoindol-5-ol
magrilon
mazanor
sa 42-548
an 448
mazindolum [inn-latin]
ccris 3152
brn 0546547
5-(p-chlorophenyl)-2,5-dihydro-3h-imidazo(2,1-a)isoindol-5-ol
mazindol, >=98% (tlc), powder
DB00579
22232-71-9
mazindol (jan/usp/inn)
D00367
sanorex (tn)
mazindol civ
terenac
sah-42548
CHEMBL781 ,
5-(4-chlorophenyl)-2,3-dihydro-5-hydroxy-5h-imidazo[2,1-a]isoindole
bdbm50005536
5-(4-chloro-phenyl)-2,5-dihydro-3h-imidazo[2,1-a]isoindol-5-ol
5-(4-chlorophenyl)-3,5-dihydro-2h-imidazo[2,1-a]isoindol-5-ol
5-thiophen-2-yl-2,3,5,6-tetrahydro-imidazo[2,1-a]isoquinolin-5-ol
5-(4-chlorophenyl)-2,3-dihydroimidazo[1,2-b]isoindol-5-ol
A816031
unii-c56709m5nh
mazindol [usan:usp:inn:ban]
c56709m5nh ,
mazindolum
smr000238174
MLS003899228
AKOS015895573
gtpl4591
[3h]-mazindol
[3h]mazindol
gtpl4797
5-(4-chlorophenyl)-2h,3h,5h-imidazo[2,1-a]isoindol-5-ol
SCHEMBL27849
mazindol [usan]
mazindol [inn]
mazindol [who-dd]
mazindol [jan]
mazindol [hsdb]
mazindol [orange book]
(+/-)-5-(p-chlorophenyl)-2,5-dihydro-3h-imidazo(2,1-a)isoindol-5-ol
mazindol [vandf]
mazindol [mi]
mazindol [mart.]
mazindol [usp impurity]
3h-imidazo(2,1-a)isoindol-5-ol, 5-(4-chlorophenyl)-2,5-dihydro-, (+/-)-
5-(4-chlorophenyl)-2,3-dihydro-5h-imidazo [2,1-a]isoindol-5-ol
5-(4-chlorophenyl)-2,3-dihydro-5h-imidazo[2,1-a]isoindol-5-ol
5h-imidazo(2,1-a)isoindol-5-ol, 5-(4-chlorophenyl)-2,3-dihydro-
5-(4-chlorophenyl)-2,5-dihydro-3h-imidazo[2,1-a]isoindol-5-ol #
3h-imidazo[2,1-a]isoindol-5-ol, 5-(p-chlorophenyl)-2,5-dihydro-
5-(p-chlorophenyl)-2,5-dihydro-3h-imidazo[2,1-a]isoindol-5-ol
DTXSID1023237 ,
mazindol, united states pharmacopeia (usp) reference standard
CHEBI:6702
NCGC00378886-01
FT-0670955
Q255680
mazindolo
a08aa05
5-(4-chlorophenyl)-2,5-dihydro-3h-imidazo
5-(4-chlorophenyl)-2,3-dihydro-5-hydroxy-5h-imidazo
mazindol (usp impurity)
mazindol (mart.)
mazindol (usan:usp:inn:ban)
dtxcid403237
mazindolum (inn-latin)
mazindol, 1mg/ml in dmf
mazindol; 5-(4-chlorophenyl)-2,5-dihydro-3h-imidazol[2,1-a]isoindol-5-ol; 5-(4-chlorophenyl)-2,3-dihydroimidazo[1,2-b]isoindol-5-ol

Research Excerpts

Overview

Mazindol is an imidazo-isoindole derivative, a tricyclic compound and a non-amphetamine central nervous system stimulant that blocks dopamine and norepinephrine reuptake. It is an attractive scaffold for both understanding the molecular determinants of serotonin/dopamine transporter selectivity and for the development of novel drug abuse treatments.

ExcerptReferenceRelevance
"Mazindol is an imidazo-isoindole derivative, a tricyclic compound and a non-amphetamine central nervous system stimulant that blocks dopamine and norepinephrine reuptake. "( Mazindol: a risk factor for pulmonary arterial hypertension?
Benzouid, C; Delclaux, C; Hussey, E; Konofal, E; Lecendreux, M, 2017
)
3.34
"Mazindol, therefore, is an attractive scaffold for both understanding the molecular determinants of serotonin/dopamine transporter selectivity and for the development of novel drug abuse treatments."( Binding of mazindol and analogs to the human serotonin and dopamine transporters.
Jensen, HH; Koldsø, H; Møller, PT; Schiøtt, B; Schjøth-Eskesen, C; Severinsen, K; Sinning, S; Thorup, KA; Wiborg, O, 2014
)
1.51
"Mazindol is a sympathomimetic amine, widely used as an anorectic agent in the treatment of obesity. "( Effects of acute administration of mazindol on brain energy metabolism in adult mice.
Bez, GD; Daufenbach, JF; Ferreira, GK; Gomes, LM; Gonçalves, CL; Jeremias, IC; Rezin, GT; Scaini, G; Streck, EL; Zugno, AI, 2014
)
2.12
"Mazindol is a tricyclic, anorectic, non-amphetamine stimulant used in narcolepsy and obesity since 1970. "( Mazindol in narcolepsy and idiopathic and symptomatic hypersomnia refractory to stimulants: a long-term chart review.
Arnulf, I; Bayard, S; Cock, VC; Dauvilliers, Y; Franco, P; Inocente, CO; Konofal, E; Lecendreux, M; Leu-Semenescu, S; Nittur, N; Scholtz, S, 2013
)
3.28
"Mazindol is a catecholamine reuptake inhibitor that blocks binding of cocaine at the dopamine reuptake site. "( Effects of cocaine alone and in combination with mazindol in human cocaine abusers.
Berger, P; Bigelow, GE; Preston, KL; Sullivan, JT, 1993
)
1.98
"1 Mazindol is a new anorexigenic agent which possesses a different chemical structure from that of phenylethylamines, but shows a pharmacological profile similar to that of (+)-amphetamine. "( Effects of mazindol, a non-phenylethylamine anorexigenic agent, on biogenic amine levels and turnover rate.
Carruba, MO; Groppetti, A; Mantegazza, P; Vicentini, L; Zambotti, F, 1976
)
1.37
"Mazindol is a potent inhibitor of neuronal dopamine (DA) and norepinephrine (NE) uptake. "( Differential visualization of dopamine and norepinephrine uptake sites in rat brain using [3H]mazindol autoradiography.
Javitch, JA; Snyder, SH; Strittmatter, SM, 1985
)
1.93

Effects

Mazindol has a long-term, favorable benefit/risk ratio in 60% of drug-resistant hypersomniacs. It has an indirect sympathomimetic action and is known to cause urogenital side effects such as urinary retention and testicular pain.

Mazindol has been shown to produce anorexia in several animal species including humans. Its pharmacological effects may be elicited by blockade of neuronal reuptake of dopamine and norepinephrine. Mazindol is known to cause urogenital side effects such as urinary retention and testicular pain.

ExcerptReferenceRelevance
"Mazindol has a long-term, favorable benefit/risk ratio in 60% of drug-resistant hypersomniacs, including a clear benefit on cataplexy."( Mazindol in narcolepsy and idiopathic and symptomatic hypersomnia refractory to stimulants: a long-term chart review.
Arnulf, I; Bayard, S; Cock, VC; Dauvilliers, Y; Franco, P; Inocente, CO; Konofal, E; Lecendreux, M; Leu-Semenescu, S; Nittur, N; Scholtz, S, 2013
)
3.28
"Mazindol has an indirect sympathomimetic action and is known to cause urogenital side effects such as urinary retention and testicular pain."( Semen-like urethral discharge during the use of mazindol.
Meyboom, RH; van Puijenbroek, EP, 1998
)
1.28
"Mazindol has been explored as a possible agent in cocaine addiction pharmacotherapy. "( Binding of mazindol and analogs to the human serotonin and dopamine transporters.
Jensen, HH; Koldsø, H; Møller, PT; Schiøtt, B; Schjøth-Eskesen, C; Severinsen, K; Sinning, S; Thorup, KA; Wiborg, O, 2014
)
2.23
"Mazindol has been proposed as a potential treatment of children with attention deficit/hyperactivity disorder (ADHD). "( Pilot Phase II study of mazindol in children with attention deficit/hyperactivity disorder.
Benadjaoud, L; Jacqz-Aigrain, E; Kaguelidou, F; Konofal, E; Laouénan, C; Lecendreux, M; Mentré, F; Zhao, W, 2014
)
2.15
"Mazindol has a long-term, favorable benefit/risk ratio in 60% of drug-resistant hypersomniacs, including a clear benefit on cataplexy."( Mazindol in narcolepsy and idiopathic and symptomatic hypersomnia refractory to stimulants: a long-term chart review.
Arnulf, I; Bayard, S; Cock, VC; Dauvilliers, Y; Franco, P; Inocente, CO; Konofal, E; Lecendreux, M; Leu-Semenescu, S; Nittur, N; Scholtz, S, 2013
)
3.28
"Mazindol has not only hunger (appetite) suppressing properties, but it probably affects the metabolism of energy substrates as well."( Endocrine studies with mazindol in obese patients.
Dolecek, R, 1980
)
1.29
"Mazindol has an indirect sympathomimetic action and is known to cause urogenital side effects such as urinary retention and testicular pain."( Semen-like urethral discharge during the use of mazindol.
Meyboom, RH; van Puijenbroek, EP, 1998
)
1.28
"Mazindol has been shown to produce anorexia in several animal species including humans, and its pharmacological effects may be elicited by blockade of neuronal reuptake of dopamine and norepinephrine. "( Effect of mazindol administration on (3H)-N-methylscopolamine binding to rat cerebral cortex.
Marinho, MM; Sousa, FC; Viana, GS, 1992
)
2.13
"1. Mazindol, which has been proposed as a therapy for muscular dystrophy because of a suppression of growth hormone release was administered orally (0.1 mg/kg body wt/day) for approximately six weeks to healthy young rats and dystrophic mice. "( Effect of mazindol on dystrophic mice and on growth in young rats.
Coakley, JH; Edwards, RH; Ensor, D; Jackson, MJ; Wagenmakers, AJ, 1989
)
1.3
"Mazindol has been reported to improve muscle function in Duchenne muscular dystrophy (DMD) by virtue of its growth hormone (GH) suppression. "( The effect of mazindol on growth hormone secretion in boys with Duchenne muscular dystrophy.
Coakley, JH; Edwards, RH; Griffiths, RD; Hipkin, LJ; Moorcraft, J; Smith, CS, 1988
)
2.08

Treatment

Treatment with mazindol showed greater short-term weight loss than that with placebo. Mazindol prevented the decrease in MAP and the increase in plasma renin activity (PRA) following 2DG infusions without modifying increased thirst or AVP responses to glucoprivation.

ExcerptReferenceRelevance
"3. Mazindol treated rats had reduced wt gain, but this effect was due to appetite suppression not growth hormone inhibition."( Effect of mazindol on dystrophic mice and on growth in young rats.
Coakley, JH; Edwards, RH; Ensor, D; Jackson, MJ; Wagenmakers, AJ, 1989
)
1.19
"Treatment with mazindol showed greater short-term weight loss than that with placebo (MD -1.721 kg; p<0.05; I2: 0.9%; p=0.388)."( Systematic review and meta-analysis of the efficacy and safety of amfepramone and mazindol as a monotherapy for the treatment of obese or overweight patients.
Correr, CJ; Fernandez-Llimos, F; Lucchetta, RC; Otuki, MF; Pontarolo, R; Radominski, RB; Riveros, BS, 2017
)
1.02
"Pretreatment with mazindol prevented the decrease in MAP and the increase in plasma renin activity (PRA) following 2DG infusions without modifying increased thirst, water intake, or AVP responses to glucoprivation."( Increased thirst and plasma arginine vasopressin levels during 2-deoxy-D-glucose-induced glucoprivation in humans.
Campbell, RG; Lilavivat, U; Robertson, GL; Thompson, DA; Welle, SL, 1981
)
0.59

Toxicity

ExcerptReferenceRelevance
" Accordingly, we tested the ability of both fetal neural (striatum) and fetal non-neural (liver) tissue implants to protect the rat striatum against the toxic effects of a subsequent intrastriatal injection of 6-OHDA."( Sham transplantation protects against 6-hydroxydopamine-induced dopaminergic toxicity in rats: behavioral and morphological evidence.
Cadet, JL; Dollison, A; Fahn, S; Gash, DM; Jackson-Lewis, V; Kostic, V; Levivier, M; Przedborski, S, 1991
)
0.28
" L-DOPA was toxic for both DA and non-DA neurons."( Toxic effects of L-DOPA on mesencephalic cell cultures: protection with antioxidants.
Casarejos, MJ; De Yébenes, JG; Mena, MA; Paíno, CL; Pardo, B, 1995
)
0.29
"Data extracted from each report included key study characteristics, clinical information, co-interventions, and outcomes, including dropouts due to either adverse drug effects or perceived lack of effect."( An overview of the efficacy and safety of fenfluramine and mazindol in the treatment of obesity.
Imperiale, TF; Stahl, KA, 1993
)
0.53
" Dropouts due to adverse drug effects were more common in the treatment group (7% vs 2%; P < ."( An overview of the efficacy and safety of fenfluramine and mazindol in the treatment of obesity.
Imperiale, TF; Stahl, KA, 1993
)
0.53
"The apparent short-term efficacy of these appetite-suppressant drugs and the lack of severe adverse drug effects or addiction suggest that they may be useful in the treatment of obesity."( An overview of the efficacy and safety of fenfluramine and mazindol in the treatment of obesity.
Imperiale, TF; Stahl, KA, 1993
)
0.53
" To verify this hypothesis, we investigated the influence of hypothermia on the toxic activity of both neurotoxins."( Apparent opposite effects of tetrabenazine and reserpine on the toxic effects of 1-methyl-4-phenylpyridinium or 6-hydroxydopamine on nigro-striatal dopaminergic neurons.
Cleren, C; Costentin, J; Naudin, B, 2003
)
0.32

Compound-Compound Interactions

ExcerptReferenceRelevance
") was administered in combination with mazindol (0, 1 and 2 mg given orally 2 hr before the cocaine injection)."( Effects of cocaine alone and in combination with mazindol in human cocaine abusers.
Berger, P; Bigelow, GE; Preston, KL; Sullivan, JT, 1993
)
0.81
" In the present study, we examined tissues from normal macaque monkeys treated for 13 weeks with high doses of L-DOPA (in combination with the peripheral decarboxylase inhibitor, carbidopa) and/or the COMT inhibitor, entacapone."( Chronic high dose L-DOPA alone or in combination with the COMT inhibitor entacapone does not increase oxidative damage or impair the function of the nigro-striatal pathway in normal cynomologus monkeys.
Halliwell, B; Jenner, P; Lyras, L; McKenzie, G; Pearce, RK; Zeng, BY, 2002
)
0.31

Bioavailability

ExcerptReferenceRelevance
" On the contrary, the [3H]mazindol tracer dose induced a marked labelling of the noradrenaline uptake complex in cerebellum; its prevention by desipramine (5 mg/kg) increased simultaneously the cerebral bioavailability and thereby the striatal labelling of the dopamine transporter."( Pharmacological modifications of dopamine transmission do not influence the striatal in vivo binding of [3H]mazindol or [3H]cocaine in mice.
Bonnet, JJ; Costentin, J; Thibaut, F; Vaugeois, JM, 1996
)
0.81
"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

Mazindol leftwardly shifted the dose-response curve to norepinephrine in a dose-dependent manner. Meal patterns were monitored in adult male rats after Mazindol dosing during the first three hours of the dark cycle using automated feeding chambers (BioDAQ) Side effects included decreased appetite (36%), dry mouth (10%), behavioral change (22%), and gastrointestinal symptoms.

ExcerptRelevanceReference
" Dose-response relationships and time course of this effect for the various drugs were determined."( Effects of mazindol, fenfluramine and chlorimipramine on the 5-hydroxytryptamine uptake and storage mechanisms in rat brain: similarities and differences.
Carruba, MO; Mantegazza, P; Picotti, GB; Zambotti, F, 1977
)
0.65
" dosage per injection, of 50 and 100 mug/kg resulted in self-administration rates significantly greater than that which occurred with saline."( Mazindol self-administration in the rhesus monkey.
Schuster, CR; Wilson, MC, 1976
)
1.7
" Side effects attributable to mazindol included decreased appetite (36%), dry mouth (10%), behavioral change (22%), and gastrointestinal symptoms (18%); mazindol dosage was reduced in 43% of patients."( Randomized, double-blind trial of mazindol in Duchenne dystrophy.
Brooke, MH; Fenichel, GM; Florence, J; Griggs, RC; Kaiser, KK; Mandel, S; Mendell, JR; Miller, PJ; Moxley, RT; Schierbecker, J, 1990
)
0.85
" Furthermore, CHP led to a dose-dependent inhibition of [3H]-DA uptake by striatal synaptosomes, reaching to maximal inhibition of uptake (30%) at CHP dosage of 10 nM."( Neuropeptide-dopamine interactions. V. Cyclo(His-Pro) regulation of striatal dopamine transporter complex.
Ikegami, H; Prasad, C,
)
0.13
" The results obtained by dosage of d-amphetamine, fenfluramine or mazindol, on days 5 and 8 after tumor implantation, failed to demonstrate conclusively any predominant modification of a dopaminergic, noradrenergic, or serotonergic system in the anorectic effects of these agents."( Effects of anorectic agents in rats bearing the Walker-256 tumor.
Johnson, K; Kinney, DR; Maickel, RP, 1987
)
0.51
" Mice were dosed daily (25 mg/kg po) for 28 days after which time carcass composition was determined."( The contribution of increased thermogenesis to the effect of anorectic drugs on body composition in mice.
Arch, JR, 1981
)
0.26
" In the present study, a K+ dose-response curve was obtained for the release of both [3H]-DA and endogenous DA from striatal tissue, in the absence and presence of catecholamine uptake blockers."( Mazindol, nomifensine and desmethylimipramine inhibit potassium-induced release of dopamine: effect of stimulus strength.
Dembiec-Cohen, D, 1998
)
1.74
" In an attempt to further clarify the mechanisms underlying these degeneration patterns, autoradiographic studies using a variety of receptor ligands were conducted in animals 21 days after an identical dosage of the continuous phencyclidine administration employed in the previous degeneration studies."( Long-term changes in brain following continuous phencyclidine administration: an autoradiographic study using flunitrazepam, ketanserin, mazindol, quinuclidinyl benzilate, piperidyl-3,4-3H(N)-TCP, and AMPA receptor ligands.
Ellison, G; Keys, A; Noguchi, K, 1999
)
0.51
" In addition, half of each of these groups also received a bolus dosage of CPF in corn oil ("spiked" animals; 60 mg/kg initially and 45 mg/kg thereafter) every 2 months (0+CPF, 1+CPF, 5+CPF)."( Neurochemical effects of chronic dietary and repeated high-level acute exposure to chlorpyrifos in rats.
Hunter, DL; Mailman, RB; Marshall, RS; Moser, VC; Oxendine, S; Padilla, S; Southerland, SB, 2005
)
0.33
" Meal patterns were monitored in adult male rats after mazindol dosing during the first three hours of the dark cycle using automated feeding chambers (BioDAQ)."( Systemic mazindol reduces food intake in rats via suppression of meal size and meal number.
Wellman, PJ, 2008
)
1.01
" 10b was additionally bioavailable following oral dosing and demonstrated efficacy in rat models of acute, inflammatory, and neuropathic pain."( Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
Adedoyin, A; Bray, JA; Deecher, DC; Fensome, A; Goldberg, JA; Harrison, J; Leventhal, L; Mann, C; Mark, L; Nogle, L; O'Neill, DJ; Spangler, TB; Sullivan, NR; Terefenko, EA; Trybulski, EJ; Uveges, AJ; Vu, A; Whiteside, GT; Zhang, P, 2011
)
0.37
[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 (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency2.68370.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency15.09160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
[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)
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.04500.00050.09140.4900AID64377
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)0.00290.00081.541620.0000AID1443747; AID147756
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.01520.00031.465610.0000AID1443758; AID1443759; AID145371; AID147760
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.04540.00070.97749.7000AID64679; AID64680; AID65015; AID65016; AID65018; AID65019; AID65020; AID65022; AID65023
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.03930.00030.37088.1600AID65189; AID65494; AID65495
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)0.07400.00010.86458.7096AID1443750; AID204063
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.07030.00000.70488.1930AID1443760; AID1443761; AID204083; AID204204
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)0.23100.00030.81978.4900AID204359
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.24750.00000.705610.0000AID204534
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)0.02750.00071.841946.0000AID1443745; AID352220; AID410156; AID481499; AID64348; AID64356
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.03790.00021.11158.0280AID1443756; AID1443757; AID431885; AID483450; AID619833; AID64377; AID64524
Sodium-dependent dopamine transporterMus musculus (house mouse)IC50 (µMol)0.01300.01300.10650.2000AID1443752
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki0.40400.40400.68731.0350AID1443755
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.23440.00030.70285.3660AID203852
TransporterRattus norvegicus (Norway rat)Ki0.00080.00010.866710.0000AID147740
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.60000.00010.40364.8000AID88008
Sodium-dependent dopamine transporter Homo sapiens (human)Activity0.02210.02210.02210.0221AID339403
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (104)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
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 (45)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
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 (47)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
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 (114)

Assay IDTitleYearJournalArticle
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID229439Selectivity ratio as ratio of IC50 value against NET to that of DAT2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1443748Enhancing of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID360444Displacement of [3H]RTI82 from DAT in rat striatal membrane2007The Journal of biological chemistry, Mar-23, Volume: 282, Issue:12
Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter.
AID230715Ratio of the IC50 against DAT in HEK hDAT cells to that of rat striatal membranes.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID114488Inhibition of reserpine (5 mg/kg i.p.) induced hypothermia in mice 2 hr after i.p. administration.1983Journal of medicinal chemistry, May, Volume: 26, Issue:5
Antidepressant activity of 5-aryl-2,3,5,6-tetrahydroimidazo[2,1-a]isoquinolin-5-ols.
AID1443742Enhancing of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID446939Displacement of [3H]WIN-35428 from human recombinant DAT expressed in CHO cells at 1 uM2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID65016Inhibition of [3H]BTCP binding to the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID229442Selectivity ratio as ratio of IC50 value against SERT to that of DAT2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID82374Ability to block the uptake of [3H]- 5- HT(serotonin) in HEK-hSERT cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID64836Inhibition of [3H]WIN-35428 binding to the dopamine transporter in rat brain1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID64348Ability to displace [3H]WIN-35428 from dopamine transporter on guinea pig striatal membrane.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID410156Displacement of [3H]WIN-35428 from human recombinant DAT expressed in CHO cells2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
AID64356Inhibition of dopamine uptake in HEK cells expressing human dopamine transporter (hDAT)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID65015Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID3719Binding affinity against 5-hydroxytryptamine 1A receptor (5-HT1A) by displacement of [3H]8-OH-DPAT from rat hippocampus membranes2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
AID65020Inhibition of [3H]WIN-35428 binding to the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID65019Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID1443752Inhibition of mouse DAT expressed in HEK293 cells assessed as reduction in [3H]-DA uptake2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID204083Displacement of [125I]- RTI-55 from Serotonin transporter expressed in HEK cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID232303Discrimination ratio against NET as ratio of IC50 to that of Ki uptake to NET.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID88008Displacement of [3H](-)-trans-H2-PAT from Guinea pig histamine H2 receptors.1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Synthesis, evaluation, and comparative molecular field analysis of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for histamine H(1) receptors.
AID339403Displacement of [3H]WIN-35428 from human recombinant dopamine transporter expressed in CHO cells2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
AID233649Selectivity ratio of IC50 values of Serotonin transporter vs Dopamine transporter1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID64680Ability to displace [3H]WIN-35428 from dopamine transporter on rat striatal membrane.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID1443746Enhancing of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID65034Ability to displace [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter.
AID1443757Inhibition of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID204359Compound was tested for inhibition of [3H]5-HT reuptake at Serotonin transporter1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID147756Inhibition of NE uptake in HEK cells expressing human noradrenaline transporter (hNET)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID232302Discrimination ratio against NET as ratio of IC50 to that of Ki uptake to NET.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID1443755Inhibition of [125I]RTI-55 binding to mouse DAT expressed in HEK293 cells preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID64377Displacement of [125I]- RTI-55 from Dopamine transporter expressed in HEK cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID65495Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID65018Inhibition of [3H]GBR-12935 binding to the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID230721Ratio of the IC50 value of Mazindol to that in guinea pig was determined2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID204204Inhibition of [125I]- RTI -55 binding at the Serotonin transporter sites on HEK-hSERT cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1443745Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID64346Ability to displace [3H]WIN-35428 from Dopamine Transporter in guinea pig striatal membrane2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID1443760Inhibition of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID1597741Half life in human at 1 to 3 mg2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Sleep modulating agents.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1443756Inhibition of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID203852The compound was tested for affinity towards sigma-3 receptor1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.
AID232305Discrimination ratio against SERT as ratio of IC50 to that of Ki uptake to SERT.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID229440Selectivity ratio as ratio of IC50 value against NET to that of DAT2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID230714Ratio of the IC50 against DAT in HEK hDAT cells to that of guinea pig striatal membranes.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID64840Inhibition of [3H]dopamine uptake at the dopamine transporter in rat striatal tissue1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID232304Discrimination ratio against SERT as ratio of IC50 to that of Ki uptake to SERT.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID147760Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1443762Selectivity ratio of Ki for [125I]RTI-55 binding to mouse DAT expressed in HEK293 cells to Ki for [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID64837Compound was tested for inhibition of [3H]WIN-35428 binding at the dopamine transporter in rat striatal membrane1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID65172Binding affinity to a single, sodium-dependent site on the Dopamine transporter in rat striatal membranes2000Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID232300Discrimination ratio against DAT as ratio of IC50 to that of Ki uptake to DAT.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID65022Inhibition of [3H]cocaine binding to the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID1443750Inhibition of recombinant human SERT expressed in HEK293 cell membranes assessed as reduction in [3H]5-HT uptake incubated for 22 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1443758Inhibition of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID145391Compound was tested for inhibition of [3H]DMI binding at the Norepinephrine transporter in rat cortical membranes at (10e-5) M1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID483450Displacement of [3H]WIN-35428 from human recombinant DAT expressed in CHO cells2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).
AID65189Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
AID114489Inhibition of reserpine (5 mg/kg i.p.) induced hypothermia in mice 4 hr after i.p. administration.1983Journal of medicinal chemistry, May, Volume: 26, Issue:5
Antidepressant activity of 5-aryl-2,3,5,6-tetrahydroimidazo[2,1-a]isoquinolin-5-ols.
AID431885Inhibition of [3H]WIN-35428 binding to human recombinant DAT expressed in CHO cells by scintillation counting2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1443747Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID420090Ratio of Ki for [3H]dopamine uptake at rat dopamine transporter expressed in CHO cells to Ki for displacement of [3H]WIN-35428 from rat dopamine transporter expressed in CHO cells2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.
AID145371Inhibition of [125I]- RTI -55 binding at the Norepinephrine transporter sites on HEK-hNET cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID1443759Inhibition of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID1443744Enhancing of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID1443743Enhancing of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID64679Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID1443761Inhibition of [3H]mazindol binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
AID64524Inhibition of [125I]- RTI -55 binding at the Dopamine transporter sites on HEK-hDAT cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID619833Displacement of [3H]-WIN-35428 from human DAT expressed in CHO cells2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
AID82373Ability to block the uptake of [3H]NE (norepinephrine) in HEK-hNET cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID204063Inhibition of 5-HT uptake in HEK cells expressing human serotonin transporter (hSERT)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID233648Selectivity ratio of IC50 values of Norepinephrine transporter vs Dopamine transporter1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID481499Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
AID82372Ability to block the uptake of [3H]- DA(dopamine) in HEK-hDAT cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID230722Ratio of the IC50 value of Mazindol to that of the compound.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID229441Selectivity ratio as ratio of IC50 value against SERT to that of DAT2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID232301Discrimination ratio against DAT as ratio of IC50 to that of Ki uptake to DAT.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID352220Inhibition of [3H]WIN-35428 binding to human recombinant DAT expressed in CHO cells2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors.
AID5476Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID65023Inhibition of [3H]dopamine uptake at the dopamine transporter.1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID230268Ratio of SERT to that of NET2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
AID65630The ratio of uptake/binding at Dopamine transporter1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID147740Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
AID65494Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.
AID230716Ratio of the IC50 against DAT in rat striatal membranes to that of guinea pig striatal membranes.2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID204534Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats2003Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID493017Wombat Data for BeliefDocking1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
AID1346944Rat NET (Monoamine transporter subfamily)2004Naunyn-Schmiedeberg's archives of pharmacology, Jul, Volume: 370, Issue:1
Binding of [3H]mazindol to cardiac norepinephrine transporters: kinetic and equilibrium studies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (609)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990254 (41.71)18.7374
1990's216 (35.47)18.2507
2000's103 (16.91)29.6817
2010's31 (5.09)24.3611
2020's5 (0.82)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 70.43

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

MetricThis Compound (vs All)
Research Demand Index70.43 (24.57)
Research Supply Index6.56 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index124.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (70.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials73 (11.57%)5.53%
Reviews27 (4.28%)6.00%
Case Studies17 (2.69%)4.05%
Observational0 (0.00%)0.25%
Other514 (81.46%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Trial to Evaluate the Efficacy and Safety of NLS-2 (Mazindol Extended-Release) Tablets in the Treatment of Narcolepsy Type 1 [NCT05914194]Phase 348 participants (Anticipated)Interventional2024-01-15Not yet recruiting
A Double-Blind Placebo-Controlled Phase II Study to Determine the Efficacy, Safety, Tolerability and Pharmacokinetics of a Controlled Release (CR) Formulation of Mazindol in Adults With DSM-5 Attention Deficit Hyperactivity Disorder (ADHD) [NCT02808104]Phase 284 participants (Actual)Interventional2016-08-31Completed
Mazindol for Cocaine Abuse [NCT00000277]Phase 20 participants Interventional1994-09-30Completed
A 6-Month Multicenter, Open-Labelled Extension of the Clinical Trial NLS-1021 in Narcoleptic Patients With and Without Cataplexy [NCT05055024]Phase 252 participants (Actual)Interventional2021-10-26Completed
A Four-week, Double-blind, Placebo-controlled, Randomized, Multicenter, Parallel-group Study of the Safety and Efficacy of NLS-2 (Mazindol Extended Release) in Adults for the Treatment of Narcolepsy [NCT04923594]Phase 267 participants (Actual)Interventional2021-09-13Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]