Page last updated: 2024-12-06

talopram

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

Description

Talopram is a selective serotonin reuptake inhibitor (SSRI) antidepressant. It was initially developed as a potential treatment for depression, but it was ultimately discontinued due to safety concerns. Research into talopram's effects is limited. It has been studied for its potential to inhibit the reuptake of serotonin in the brain, similar to other SSRIs, but it also exhibits a higher affinity for dopamine receptors. This unique profile may have contributed to its potential efficacy for depression, but also may have led to concerns regarding its safety. The limited research available suggests that talopram could potentially interact with other medications and may cause side effects. The drug's discontinuation highlights the importance of safety in drug development and the need for thorough research before introducing new medications.'

talopram: putative PET ligand for the norepinephrine transporter; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23573
CHEMBL ID299233
SCHEMBL ID399706
MeSH IDM0481084

Synonyms (32)

Synonym
1-isobenzofuranpropanamine,3-dihydro-n,3,3-trimethyl-1-phenyl-, hydrochloride
phthalan,3-dimethyl-1-(3-methylaminopropyl)-1-phenyl-, hydrochloride
1-phthalanpropylamine,3,3-trimethyl-, hydrochloride
lu 3-010 hydrochloride
phtalapromine hydrochloride
1-phthalanpropylamine,3,3-trimethyl-1-phenyl-, hydrochloride
wln: t56 cot&j b3m1 br& d1 d1 &gh
phthalapromine
CHEMBL299233 ,
talopram
3-(3,3-dimethyl-1-phenyl-2-benzofuran-1-yl)-n-methylpropan-1-amine
bdbm50021246
[3-(3,3-dimethyl-1-phenyl-1,3-dihydro-isobenzofuran-1-yl)-propyl]-methyl-amine(talopram)
3-(3,3-dimethyl-1-phenyl-1,3-dihydroisobenzofuran-1-yl)-n-methylpropan-1-amine
talopramum
talopran [inn-spanish]
talopramum [inn-latin]
3,3-dimethyl-1-(3-methylaminopropyl)-1-phenylphthalene
unii-5py881hc79
7182-51-6
1,3-dihydro-1,1-dimethyl-3-(3-methylaminopropyl)-3-phenylisobenzofuran
5py881hc79 ,
n,3,3-trimethyl-1-phenyl-1-phthalanpropylamin
talopram [inn]
talopran
1-isobenzofuranpropanamine, 1,3-dihydro-n,3,3-trimethyl-1-phenyl-
n,3,3-trimethyl-1-phenyl-1-phthalanpropylamine
SCHEMBL399706
DB09190
NCGC00371094-01
Q7680301
DTXSID10864019

Research Excerpts

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.42530.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency6.74120.00108.379861.1304AID1645840
[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)
AromataseRattus norvegicus (Norway rat)IC50 (µMol)1.40000.00181.85646.2000AID179069
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC50 (µMol)44.00000.00070.97749.7000AID179076
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki10.00000.00030.37088.1600AID1881360
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)1.40000.00030.81978.4900AID179069
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.79500.00000.705610.0000AID1881361
TransporterRattus norvegicus (Norway rat)IC50 (µMol)0.00290.00081.95628.8000AID179081
TransporterRattus norvegicus (Norway rat)Ki0.00450.00010.866710.0000AID1881359
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (15)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID408251Inhibition of [3H]5-hydroxytryptamine reuptake at human SERT expressed in african green monkey COS7 cells at 100 nM2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: synthesis and structure-activity relationship studies.
AID179076Inhibition of dopamine uptake in rat synaptosomal fraction1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
AID112281Compound was tested for antagonistic activity against 5-HTP-induced potentiation in mice1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
AID179081Inhibition of noradrenaline uptake in rat synaptosomal fraction1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
AID1881360Displacement of [3H]-WIN 3542875 from DAT in Sprague-Dawley rat brain striatum incubated for 120 mins by radioligand binding assay2021RSC medicinal chemistry, Jul-21, Volume: 12, Issue:7
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram.
AID408252Inhibition of [3H]dopamine reuptake at human NET expressed in african green monkey COS7 cells at 100 nM2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: synthesis and structure-activity relationship studies.
AID112283Antagonistic activity against tetrabenazine-induced ptosis in mice1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
AID179069Inhibition of 5-HT uptake in rat synaptosomal fraction1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.
AID1881361Displacement of [3H]-citalopram from SERT in Sprague-Dawley rat brainstem incubated for 60 mins by radioligand binding assay2021RSC medicinal chemistry, Jul-21, Volume: 12, Issue:7
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram.
AID1881359Displacement of [3H]-nisoxetine from NET in Sprague-Dawley rat brain prefrontal cortex incubated for 180 mins by radioligand binding assay2021RSC medicinal chemistry, Jul-21, Volume: 12, Issue:7
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (36.36)18.7374
1990's0 (0.00)18.2507
2000's2 (18.18)29.6817
2010's2 (18.18)24.3611
2020's3 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.54

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 Index49.54 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index72.07 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (49.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]