pridopidine: a dopamine stabilizer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
---|---|
PubMed CID | 9795739 |
CHEMBL ID | 596802 |
SCHEMBL ID | 166748 |
MeSH ID | M0464604 |
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 |
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Pridopidine treatment suppressed supranormal ER Ca. SOD1 G93A mice showed genotype-specific effects with the prevention of cachexia.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 8.4866 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
D(2) dopamine receptor | Homo sapiens (human) | Ki | 12.5177 | 0.0000 | 0.6518 | 10.0000 | AID1718169; AID1718170; AID458632; AID458633 |
Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0817 | 0.0000 | 0.4901 | 10.0000 | AID1718135 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
dopamine neurotransmitter receptor activity, coupled via Gi/Go | D(2) dopamine receptor | Homo sapiens (human) |
G-protein alpha-subunit binding | D(2) dopamine receptor | Homo sapiens (human) |
protein binding | D(2) dopamine receptor | Homo sapiens (human) |
heterotrimeric G-protein binding | D(2) dopamine receptor | Homo sapiens (human) |
dopamine binding | D(2) dopamine receptor | Homo sapiens (human) |
ionotropic glutamate receptor binding | D(2) dopamine receptor | Homo sapiens (human) |
identical protein binding | D(2) dopamine receptor | Homo sapiens (human) |
heterocyclic compound binding | D(2) dopamine receptor | Homo sapiens (human) |
G protein-coupled receptor activity | D(2) dopamine receptor | Homo sapiens (human) |
G protein-coupled opioid receptor activity | Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) |
protein binding | Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID458641 | Reduction in spontaneous locomotor activity in Sprague-Dawley rat striatum at 100 umol/kg, sc relative to control | 2010 | Journal 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). |
AID458632 | Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells | 2010 | Journal 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). |
AID714095 | Reduction in spontaneous locomotor activity in Sprague-Dawley rat at 300 umol/kg, sc measured after 15 to 60 mins relative to saline-treated control | 2012 | Journal 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. |
AID714104 | Increase in DOPAC level in sc dosed Sprague-Dawley rat striatum by HPLC analysis | 2012 | Journal 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. |
AID458633 | Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells | 2010 | Journal 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). |
AID714098 | Decrease in 5-HIAA level in Sprague-Dawley rat striatum at 300 umol/kg, sc by HPLC analysis relative to saline-treated control | 2012 | Journal 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. |
AID736003 | Displacement of [3H]Ro 41-1049 from rat MAO-A receptor expressed in HEK293 cells | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis, pharmacological evaluation and QSAR modeling of mono-substituted 4-phenylpiperidines and 4-phenylpiperazines. |
AID458634 | Selectivity ratio of Ki for human dopamine D2 receptor at low affinity state to Ki for human dopamine D2 receptor at high affinity state | 2010 | Journal 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). |
AID1718135 | Inhibition of [3H](+)-pentazocine binding to human sigma1 receptor expressed in HEK293 cells by liquid scintillation spectrometry | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
AID1718170 | Binding affinity to dopamine D2 (high) receptor (unknown origin) | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
AID1718169 | Binding affinity to dopamine D2 (low) receptor (unknown origin) | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases. |
AID458635 | Activity at dopamine D2L receptor expressed in HEK293 cells coexpressing Galphaqi5 assessed as maximal efficacy relative to control | 2010 | Journal 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). |
AID714099 | Increase in DOPAC level in Sprague-Dawley rat striatum at 300 umol/kg, sc by HPLC analysis relative to saline-treated control | 2012 | Journal 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. |
AID714105 | Displacement of [3H]Ro 41-1049 from MAO-A in rat cerebral cortex by competition binding assay | 2012 | Journal 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. |
AID714107 | Displacement of [3H]imipramine from human SERT expressed in CHO cells by competition binding assay | 2012 | Journal 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. |
AID458636 | Reduction in 3,4-dihydroxyphenylacetic acid level in Sprague-Dawley rat striatum at 100 umol/kg, sc relative to saline treated control | 2010 | Journal 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). |
AID458654 | Reduction in amphetamine-induced locomotor activity in Sprague-Dawley rat striatum at 150 umol/kg, sc relative to control | 2010 | Journal 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 6 (8.96) | 29.6817 |
2010's | 46 (68.66) | 24.3611 |
2020's | 15 (22.39) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (49.07) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 12 (17.39%) | 5.53% |
Reviews | 8 (11.59%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 49 (71.01%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |