Page last updated: 2024-12-11

pridopidine

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

Description

pridopidine: a dopamine stabilizer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9795739
CHEMBL ID596802
SCHEMBL ID166748
MeSH IDM0464604

Synonyms (37)

Synonym
acr-16
acr16
CHEMBL596802 ,
pridopidine
4-(3-methylsulfonylphenyl)-1-propylpiperidine
4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine
bdbm50308028
346688-38-8
D09953
pridopidine (usan/inn)
acr16 compound
pridopidine [usan:inn]
4-(3-methanesulfonylphenyl)-1-propylpiperidine
unii-hd4tw8s2vk
acr 16
piperidine, 4-(3-(methylsulfonyl)phenyl)-1-propyl-
4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine
4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine
hd4tw8s2vk ,
FT-0672149
AKOS015891431
SCHEMBL166748
pridopidine [inn]
pridopidine [usan]
pridopidine [who-dd]
pridopidine [mi]
DTXSID90188225
NCGC00386586-01
DB11947
4-3-(methylsulfonyl)phenyl-1-propylpiperidine
mfcd09835586
AS-50146
Q7242858
HY-10684
CS-0002733
asp2314
O11067

Research Excerpts

Overview

Pridopidine is an oral drug in clinical development for treatment of Huntington's disease. Pridopidine was found to be a metabolism dependent inhibitor of CYP2D6, the main enzyme catalysing its own metabolism.

ExcerptReferenceRelevance
"Pridopidine is a highly selective and potent S1R agonist in clinical development."( Neuroprotection of retinal ganglion cells by the sigma-1 receptor agonist pridopidine in models of experimental glaucoma.
Gershoni-Emek, N; Geva, M; Hayden, MR; Levin, LA; Ly, P; Mota, S; Naia, L; Rego, AC, 2021
)
1.57
"Pridopidine is a selective and potent sigma-1 receptor (S1R) agonist currently in clinical development for HD."( Pridopidine rescues BDNF/TrkB trafficking dynamics and synapse homeostasis in a Huntington disease brain-on-a-chip model.
Capellano, L; Genoux, A; Gershoni-Emek, N; Geva, M; Hayden, MR; Lahaye, RA; Lenoir, S; Saudou, F; Scaramuzzino, C; Virlogeux, A; Vitet, H, 2022
)
2.89
"Pridopidine is a sigma-1-receptor agonist shown to have beneficial effects in preclinical models of HD."( Effects of Pridopidine on Functional Capacity in Early-Stage Participants from the PRIDE-HD Study.
Geva, M; Hayden, M; Kieburtz, K; Leinonen, M; McGarry, A; Olanow, CW, 2020
)
1.67
"Pridopidine is an oral drug in clinical development for treatment of patients with Huntington's disease. "( Metoprolol-pridopidine drug-drug interaction and food effect assessments of pridopidine, a new drug for treatment of Huntington's disease.
Hallak, H; Muglia, P; Pastino, G; Rabinovich-Guilatt, L; Spiegelstein, O; Steiner, L, 2017
)
2.29
"Pridopidine was found to be a metabolism dependent inhibitor of CYP2D6, the main enzyme catalysing its own metabolism. "( Metoprolol-pridopidine drug-drug interaction and food effect assessments of pridopidine, a new drug for treatment of Huntington's disease.
Hallak, H; Muglia, P; Pastino, G; Rabinovich-Guilatt, L; Spiegelstein, O; Steiner, L, 2017
)
2.29
"As pridopidine is a metabolism-dependent inhibitor of CYP2D6, systemic levels of drugs metabolized by CYP2D6 may increase with chronic coadministration of pridopidine. "( Metoprolol-pridopidine drug-drug interaction and food effect assessments of pridopidine, a new drug for treatment of Huntington's disease.
Hallak, H; Muglia, P; Pastino, G; Rabinovich-Guilatt, L; Spiegelstein, O; Steiner, L, 2017
)
1.47
"Pridopidine is a small molecule in clinical development for the treatment of Huntington's disease. "( Pridopidine Induces Functional Neurorestoration Via the Sigma-1 Receptor in a Mouse Model of Parkinson's Disease.
Bez, F; Cenci, MA; Denis, Q; Francardo, V; Geva, M; Hayden, MR; Steiner, L, 2019
)
3.4
"Pridopidine is a small molecule that has been clinically developed for Huntington disease."( Targeting the Sigma-1 Receptor via Pridopidine Ameliorates Central Features of ALS Pathology in a SOD1
Altman, T; Geva, M; Gradus, T; Hayden, M; Ionescu, A; Maimon, R; Perlson, E; Saraf Avraham, N, 2019
)
1.51
"Pridopidine is a small molecule showing therapeutic potential in HD preclinical and clinical studies."( Pridopidine protects neurons from mutant-huntingtin toxicity via the sigma-1 receptor.
Akimov, S; Arbez, N; Eddings, CR; Geva, M; Hayden, MR; Ross, CA, 2019
)
2.68
"Pridopidine is a new dopaminergic stabilizer, recently developed for the treatment of motor symptoms associated with HD."( Pridopidine, a dopamine stabilizer, improves motor performance and shows neuroprotective effects in Huntington disease R6/2 mouse model.
Amico, E; Di Pardo, A; Favellato, M; Frati, L; Maglione, V; Squitieri, F, 2015
)
2.58
"Pridopidine is a novel agent in the dopidine class believed to have 'state dependent' effects at dopamine receptors, thus show promise in the treatment of these disorders of voluntary movement."( Pridopidine for the treatment of Huntington's disease.
Shannon, KM, 2016
)
2.6

Effects

Pridopidine (90 mg/day) has an acceptable safety profile and is well-tolerated for 1 year. Pridopidine has an additive effect on IKAP levels when used in combination with kinetin or TSA, but not with PS.

ExcerptReferenceRelevance
"Pridopidine has an additive effect on IKAP levels when used in combination with kinetin or TSA, but not with PS; suggesting that PS and pridopidine influence IKBKAP levels through the same mechanism."( Combinatorial treatment increases IKAP levels in human cells generated from Familial Dysautonomia patients.
Ast, G; Donyo, M; Yannai, S; Zonszain, J, 2019
)
1.24
"Pridopidine (≤90 mg/day) has an acceptable safety profile and is well-tolerated for 1 year."( One-year safety and tolerability profile of pridopidine in patients with Huntington disease.
Bright, J; de Yebenes, JG; Ivkovic, J; Landwehrmeyer, B; Prang, A; Reilmann, R; Rembratt, A; Rosser, A; Squitieri, F, 2013
)
2.09
"Pridopidine has been shown to display both functional dopamine D2 receptor antagonist properties and increase in biomarkers associated with NMDA-mediated glutamate transmission in the frontal cortex."( The dopaminergic stabilizer pridopidine increases neuronal activity of pyramidal neurons in the prefrontal cortex.
Gronier, B; Ponten, H; Waters, S, 2013
)
1.41

Treatment

Pridopidine treatment suppressed supranormal ER Ca. SOD1 G93A mice showed genotype-specific effects with the prevention of cachexia.

ExcerptReferenceRelevance
"Pridopidine-treated SOD1 G93A mice showed genotype-specific effects with the prevention of cachexia."( Pridopidine modifies disease phenotype in a SOD1 mouse model of amyotrophic lateral sclerosis.
Estévez-Silva, HM; Giacobbo, BL; Liu, X; Marcellino, DJ; Mediavilla, T; Sultan, FR, 2022
)
2.89
"Pridopidine treatment suppressed supranormal ER Ca"( The sigma-1 receptor mediates the beneficial effects of pridopidine in a mouse model of Huntington disease.
Bezprozvanny, I; Geva, M; Grossman, I; Hayden, M; Kusko, R; Ryskamp, D; Wu, J, 2017
)
1.42

Toxicity

Pridopidine 45 mg BID was generally safe and tolerable in HD subjects over 36 months. Pridopidine remained safe and well tolerated over the 60-month interval.

ExcerptReferenceRelevance
" Any adverse events (AEs) were recorded."( One-year safety and tolerability profile of pridopidine in patients with Huntington disease.
Bright, J; de Yebenes, JG; Ivkovic, J; Landwehrmeyer, B; Prang, A; Reilmann, R; Rembratt, A; Rosser, A; Squitieri, F, 2013
)
0.65
"This study provides Class IV evidence that pridopidine (≤90 mg/day) is generally safe and well-tolerated in patients with Huntington disease for up to 1 year."( One-year safety and tolerability profile of pridopidine in patients with Huntington disease.
Bright, J; de Yebenes, JG; Ivkovic, J; Landwehrmeyer, B; Prang, A; Reilmann, R; Rembratt, A; Rosser, A; Squitieri, F, 2013
)
0.91
" Adverse events (AEs), laboratory values, and electrocardiography were monitored throughout."( Safety and Exploratory Efficacy at 36 Months in Open-HART, an Open-Label Extension Study of Pridopidine in Huntington's Disease.
Abler, V; Auinger, P; Gandhi, S; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Papapetropoulos, S, 2017
)
0.68
"Pridopidine 45 mg BID was generally safe and tolerable in HD subjects over 36 months."( Safety and Exploratory Efficacy at 36 Months in Open-HART, an Open-Label Extension Study of Pridopidine in Huntington's Disease.
Abler, V; Auinger, P; Gandhi, S; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Papapetropoulos, S, 2017
)
2.12
" The most frequent adverse events across all groups were diarrhoea, vomiting, nasopharyngitis, falls, headache, insomnia, and anxiety."( Safety and efficacy of pridopidine in patients with Huntington's disease (PRIDE-HD): a phase 2, randomised, placebo-controlled, multicentre, dose-ranging study.
Borowsky, B; Eyal, E; Grachev, ID; Gross, N; Hayden, M; Kieburtz, K; Landwehrmeyer, GB; Langbehn, D; McGarry, A; Papapetropoulos, S; Reilmann, R; Savola, JM; Schubert, R; Squitieri, F; Wickenberg, AT, 2019
)
0.82
" Adverse events, concomitant medications, vital signs, laboratory values, and ECG data were monitored."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
0.77
" Pridopidine remained safe and well tolerated over the 60-month interval."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
1.68
"The 45 mg BID pridopidine dosage remained safe and tolerable over 60 months."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
1.13

Pharmacokinetics

ExcerptReferenceRelevance
" In vitro studies have shown that pridopidine is a substrate for the P450 cytochrome 2D6 enzyme (CYP2D6), and clinical data show that the half-life of pridopidine is different following single dosing versus at steady state."( Pharmacokinetic and tolerability profile of pridopidine in healthy-volunteer poor and extensive CYP2D6 metabolizers, following single and multiple dosing.
Gundorf Drewes, P; Lindskov Krog, P; Osterberg, O; Rembratt, Å; Schultz, A; Timmer, W, 2013
)
0.93

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

Pridopidine is a substrate for the P450 cytochrome 2D6 enzyme (CYP2D6) In vitro studies have shown that the half-life of pridopidine is different following single dosing versus at steady state. The 45 mg BID pridobidine dosage remained safe and tolerable over 60 months.

ExcerptRelevanceReference
" Results of studies examining the effects of multiple repeat dosing suggest that the CYP2D6 enzyme is at least partly inactivated by pridopidine."( The dopaminergic stabilizer pridopidine is to a major extent N-depropylated by CYP2D6 in humans.
Bertilsson, L; Helldén, A; Johansson, P; Panagiotidis, G; Tedroff, J; Waters, N; Waters, S, 2012
)
0.88
" In vitro studies have shown that pridopidine is a substrate for the P450 cytochrome 2D6 enzyme (CYP2D6), and clinical data show that the half-life of pridopidine is different following single dosing versus at steady state."( Pharmacokinetic and tolerability profile of pridopidine in healthy-volunteer poor and extensive CYP2D6 metabolizers, following single and multiple dosing.
Gundorf Drewes, P; Lindskov Krog, P; Osterberg, O; Rembratt, Å; Schultz, A; Timmer, W, 2013
)
0.93
" The 90 mg/day dosage appears worthy of further study."( A randomized, double-blind, placebo-controlled trial of pridopidine in Huntington's disease.
, 2013
)
0.64
"Drug-interaction experiments, supplemented by dose-response data, examined the effects of these compounds on locomotor activity, on striatal levels of dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC), and on levels of activity-regulated cytoskeleton-associated (Arc) gene expression in the striatum and frontal cortex of male Sprague-Dawley rats."( Co-administration of the Dopaminergic Stabilizer Pridopidine and Tetrabenazine in Rats.
Klamer, D; Ponten, H; Waters, N; Waters, S, 2014
)
0.66
"The 45 mg BID pridopidine dosage remained safe and tolerable over 60 months."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6Homo sapiens (human)Potency8.48660.00108.379861.1304AID1645840
[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 receptorHomo sapiens (human)Ki12.51770.00000.651810.0000AID1718169; AID1718170; AID458632; AID458633
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.08170.00000.490110.0000AID1718135
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (102)

Processvia Protein(s)Taxonomy
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo 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 (10)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo 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 (34)

Processvia Protein(s)Taxonomy
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo 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 (22)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID458641Reduction in spontaneous locomotor activity in Sprague-Dawley rat striatum at 100 umol/kg, sc relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID458632Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID714095Reduction in spontaneous locomotor activity in Sprague-Dawley rat at 300 umol/kg, sc measured after 15 to 60 mins relative to saline-treated control2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID714104Increase in DOPAC level in sc dosed Sprague-Dawley rat striatum by HPLC analysis2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID458633Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID714098Decrease in 5-HIAA level in Sprague-Dawley rat striatum at 300 umol/kg, sc by HPLC analysis relative to saline-treated control2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID736003Displacement of [3H]Ro 41-1049 from rat MAO-A receptor expressed in HEK293 cells2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, pharmacological evaluation and QSAR modeling of mono-substituted 4-phenylpiperidines and 4-phenylpiperazines.
AID458634Selectivity ratio of Ki for human dopamine D2 receptor at low affinity state to Ki for human dopamine D2 receptor at high affinity state2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1718135Inhibition of [3H](+)-pentazocine binding to human sigma1 receptor expressed in HEK293 cells by liquid scintillation spectrometry2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
AID1718170Binding affinity to dopamine D2 (high) receptor (unknown origin)2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
AID1718169Binding affinity to dopamine D2 (low) receptor (unknown origin)2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
AID458635Activity at dopamine D2L receptor expressed in HEK293 cells coexpressing Galphaqi5 assessed as maximal efficacy relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID714099Increase in DOPAC level in Sprague-Dawley rat striatum at 300 umol/kg, sc by HPLC analysis relative to saline-treated control2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID714105Displacement of [3H]Ro 41-1049 from MAO-A in rat cerebral cortex by competition binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID714107Displacement of [3H]imipramine from human SERT expressed in CHO cells by competition binding assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.
AID458636Reduction in 3,4-dihydroxyphenylacetic acid level in Sprague-Dawley rat striatum at 100 umol/kg, sc relative to saline treated control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID458654Reduction in amphetamine-induced locomotor activity in Sprague-Dawley rat striatum at 150 umol/kg, sc relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (67)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (8.96)29.6817
2010's46 (68.66)24.3611
2020's15 (22.39)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.07

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index49.07 (24.57)
Research Supply Index4.41 (2.92)
Research Growth Index5.09 (4.65)
Search Engine Demand Index74.20 (26.88)
Search Engine Supply Index1.97 (0.95)

This Compound (49.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials12 (17.39%)5.53%
Reviews8 (11.59%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other49 (71.01%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]