Page last updated: 2024-12-07

ta 0910

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

Description

TA 0910: structure given in first source; has central nervous system actions; RN given refers to (S)-isomer; RN for cpd without isomeric designation not available 8/90 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID114750
CHEMBL ID2107016
CHEBI ID135653
SCHEMBL ID194528
SCHEMBL ID21219549
SCHEMBL ID22077031
MeSH IDM0179022

Synonyms (50)

Synonym
(4s)-n-[(2s)-1-[(2s)-2-carbamoylpyrrolidin-1-yl]-3-(3h-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
gtpl2143
taltirelin ,
ta-0910
ceredist
NCGC00181033-01
l-prolinamide, n-((hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl)-l-histidyl-, (s)-
l-prolinamide, n-(((4s)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl)-l-histidyl-
ta 0910
(1-methyl-4,5-dihydroorotyl)-histidyl-prolinamide
(-)-n-(((s)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl)-l-histidyl-l-prolinamide
n-{[(4s)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-l-histidyl-l-prolinamide
taltirelina
CHEBI:135653
taltirelinum
1-methyl-(s)-4,5-dihydroorotyl-l-histidyl-l-prolinamide
taltireline
103300-74-9
(4s)-n-[(2s)-1-[(2s)-2-carbamoylpyrrolidin-1-yl]-3-(1h-imidazol-5-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
dtxsid0043763 ,
dtxcid8023763
cas-103300-74-9
tox21_112682
unii-doz62mv6a5
ccris 8513
taltirelin [inn]
doz62mv6a5 ,
AKOS015920135
CHEMBL2107016
AKOS015969113
BCPP000053
HY-B0596
SCHEMBL194528
taltirelin [mi]
taltirelin [who-dd]
taltirelin [mart.]
taltirelin acetate
n-[[(4s)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-l-histidyl-l-prolinamide
(s)-n-((s)-1-((s)-2-carbamoylpyrrolidin-1-yl)-3-(1h-imidazol-4-yl)-1-oxopropan-2-yl)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxamide
AC-23956
J-000925
(1-methyl-(s)-4,5-dihydroorotyl)-l-histidyl-l-prolinamide
methyl5-(propan-2-yl)-1,2-oxazole-3-carboxylate
SCHEMBL21219549
(s)-n-((s)-1-((s)-2-carbamoylpyrrolidin-1-yl)-3-(1h-imidazol-5-yl)-1-oxopropan-2-yl)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxamide
BCP02001
Q7680336
AMY22588
NCGC00381723-02
SCHEMBL22077031

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" No adverse effects of taltirelin hydrate on reproductive function were detected in any groups."( [Reproductive and developmental toxicity studies of taltirelin hydrate (1) fertility study in rats by oral administration].
Ariyuki, F; Asano, Y; Imado, N; Imahie, H; Inui, T; Kobayashi, T, 1997
)
0.3
" No adverse effect of taltirelin hydrate on the body weight gain, food consumption, water intake, and reproductive performance was observed in this group."( [Reproductive and developmental toxicity studies of taltirelin hydrate (2) teratogenicity study in rats by oral administration].
Asano, Y; Imado, N; Imahie, H; Kobayashi, T; Nishida, A, 1997
)
0.3
" Neither death nor adverse effects on food consumption in dams were found in any dose groups."( [Reproductive and developmental toxicity studies of taltirelin hydrate (3) teratogenicity study in rabbits by oral administration].
Asano, Y; Imado, N; Imahie, H; Nishida, A, 1997
)
0.3
" No adverse effect of taltirelin hydrate on the body weight gain, food consumption and reproductive performance was observed in this group."( [Reproductive and developmental toxicity studies of taltirelin hydrate (4) perinatal and postnatal study in rats by oral administration].
Asano, Y; Imahie, H; Kobayashi, T; Koguchi, A, 1997
)
0.3

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" injection of taltirelin at this dosage produced a significant increase in the dissociation constant (Kd) of specific [3H]MeTRH binding in sham and 2VO-reperfusion groups (33."( Neuroprotective effect and brain receptor binding of taltirelin, a novel thyrotropin-releasing hormone (TRH) analogue, in transient forebrain ischemia of C57BL/6J mice.
Kimura, R; Urayama, A; Watanabe, Y; Yamada, S; Zhang, J, 2002
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
nootropic agentAny compound that improves mental functions such as cognition, memory, intelligence, motivation, attention, and concentration.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
[role 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]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[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 (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
AID1346830Mouse TRH2 receptor (Thyrotropin-releasing hormone receptors)2013Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, May, Volume: 38, Issue:6
Thyrotropin-releasing hormone receptor type 1 (TRH-R1), not TRH-R2, primarily mediates taltirelin actions in the CNS of mice.
AID1346376Human TRH1 receptor (Thyrotropin-releasing hormone receptors)2012Frontiers in endocrinology, , Volume: 3Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (64)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's40 (62.50)18.2507
2000's10 (15.63)29.6817
2010's12 (18.75)24.3611
2020's2 (3.13)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.36

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

MetricThis Compound (vs All)
Research Demand Index10.36 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (3.13%)5.53%
Reviews1 (1.56%)6.00%
Case Studies1 (1.56%)4.05%
Observational0 (0.00%)0.25%
Other60 (93.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Multicenter, Randomized, Double-blind, Placebo-controlled, Phase IV Clinical Trial to Evaluate and Compare the Efficacy and Safety of C-Trelin OD Tab 5mg(Taltirelin Hydrate) in Patients With Ataxia Induced by Spinocerebellar Degeneration [NCT04107740]Phase 4160 participants (Actual)Interventional2019-03-04Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]