Page last updated: 2024-12-05

xanthinol niacinate

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

Description

Xanthinol niacinate, also known as nicotinoyl xanthine, is a compound composed of xanthine and nicotinic acid. It is a vasodilator, meaning it widens blood vessels, and has been used to treat peripheral vascular disease, intermittent claudication, and cerebrovascular insufficiency. Xanthinol niacinate is thought to exert its effects by inhibiting the enzyme phosphodiesterase, which leads to an increase in cyclic adenosine monophosphate (cAMP) levels. Increased cAMP levels lead to vasodilation and improved blood flow. The synthesis of xanthinol niacinate involves the reaction of xanthine with nicotinic acid. Research on xanthinol niacinate has focused on its potential to improve blood flow and treat vascular disorders. However, its effectiveness and safety are still under investigation, and it is not currently widely used in clinical practice.'

Xanthinol Niacinate: A vasodilator used in peripheral vascular disorders and insufficiency. It may cause gastric discomfort and hypotension. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9912
CHEMBL ID1560089
SCHEMBL ID121655
MeSH IDM0023047

Synonyms (92)

Synonym
MLS001148608
HMS3394E09
smr000058741
pyridine-3-carboxylic acid - 7-{2-hydroxy-3-[(2-hydroxyethyl)(methyl)amino]propyl}-1,3-dimethyl-3,7-dihydro-1h-purine-2,6-dione (1:1)
nicotinato de xantinol [inn-spanish]
xanthinol niacinate [usan]
xantinoli nicotinas [inn-latin]
xanthinolium nicotinicum
nsc 113217
7- 2-hydroxy-3-((2-hydroxyethyl)methylamino)propyl theophylline, compound with nicotinic acid (1:1)
nicotinate de xantinol [inn-french]
7-(3-(n-(2-hydroxyethyl)amino)-2-hydroxypropyl)thiophylline nicotinate
angiomin
sadamin
xantinolo nicotinato [dcit]
7-{2-hydroxy-3-((2-hydroxyethyl)methylamino)propyl}theophylline, compound with nicotinic acid (1:1)
xavin
einecs 207-115-7
D06334
complamin (tn)
xantinol nicotinate
xanidil
complamex
nsc113217
3-pyridinecarboxylic acid,7-dihydro-7-[2-hydroxy-3-[(2-hydroxyethyl)methylamino]propyl]-1,3-dimethyl-1h-purine-2,6-dione (1:1)
complamin retard
437-74-1
vedrin
sadamine
xanthinol nicotinate
nsc-113217
sk 331a
sk 331 a
stenalgil
angioamin
7-[2-hydroxy-3-[(2-hydroxyethyl)methylamino]propyl]theophylline, compound with nicotinic acid (1:1)
xanthinol niacinate
complamin
landrina
teonicol
nicotinic acid compound with 7-(2-hydroxy-3-((2-hydroxyethyl)(methyl)amino)propyl)-1,3-dimethyl-3,7-dihydro-1h-purine-2,6-dione (1:1)
3-pyridinecarboxylic acid & {3,7-dihydro-7-[2-hydroxy-3-[(2-hydroxyethyl)methylamino]propyl]-1,} 3-dimethyl-1h-purine-2,6-dione (1:1)
xanthinol niacinate (usan)
{7-[2-hydroxy-3-[(2-hydroxyethyl)methylamino]propyl]theophylline,} compound with nicotinic acid (1:1)
7-[2-hydroxy-3-[2-hydroxyethyl(methyl)amino]propyl]-1,3-dimethyl-purine-2,6-dione; nicotinic acid
NCGC00164435-01
MLS000028609 ,
HMS2052E09
NCGC00021151-02
AKOS005267237
MLS001424204
tox21_110866
dtxsid0023743 ,
cas-437-74-1
dtxcid103743
HMS2230J12
CCG-101097
nicotinato de xantinol
nicotinate de xantinol
8g60h12x2d ,
xantinol nicotinate [inn]
xantinolo nicotinato
unii-8g60h12x2d
xantinoli nicotinas
FT-0603393
xantinol nicotinate [who-dd]
xantinol nicotinate [mart.]
7-{2-hydroxy-3-[(2-hydroxyethyl)methylamino]propyl}theophylline, compound with nicotinic acid (1:1)
xanthinol niacinate [mi]
(+/-)-7-(2-hydroxy-3-((2-hydroxyethyl)methylamino)propyl)theophylline, compound with nicotinic acid (1:1)
S4868
HMS3371O12
MLS006010909
SCHEMBL121655
NC00347
CHEMBL1560089
OPERA_ID_260
7-{2-hydroxy-3-[(2-hydroxyethyl)(methyl)amino]propyl}-1,3-dimethyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione; pyridine-3-carboxylic acid
SR-01000000242-4
sr-01000000242
7-(2-hydroxy-3-((2-hydroxyethyl)(methyl)amino)propyl)-1,3-dimethyl-1h-purine-2,6(3h,7h)-dione nicotinate
Q5814478
E75972
mfcd00058342
xantinol nicotinate ,(s)
HY-B1815
AS-11613
CCG-269063
CS-0013860
7-[2-hydroxy-3-[2-hydroxyethyl(methyl)amino]propyl]-1,3-dimethylpurine-2,6-dione;pyridine-3-carboxylic acid
A913692
angioamincomplamin

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In respect to bioavailability and tolerance the 1-g xanthinol nicotinate retard tablet was comparable with corresponding dosages of 500-mg retard tablets."( [Bioavailability and tolerance of xanthinol nicotinate depot preparations. Comparison of a conventional 500 mg xanthinol nicotinate depot tablet with new 500 mg and 1 g depot tablets].
Buscher, G; Dierdorf, D; Freytag, A; Mügge, H; von Schrader, HW; Wolf, D, 1985
)
0.27
"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
" Cinnarizine potentiated the effect of PGI2 shifting the anti-hypoxic dose-response curve of PGI2 to the left."( Study on the anti-hypoxic effect of cinnarizine and its interaction with prostacyclin.
Milanova, D; Nikolov, R; Nikolova, M, 1984
)
0.27
" In monitored patients, we started treatment with vasoactive therapy, ampules of xanthinol nicotinate (one ampule of 2 ml, 300 mg) or ampules of pentoxiphylline (one ampule of 5 ml, 100 mg) in form of infusions with addition of vitamins with an everyday gradual increase of dosage up to 12 ampules of xanthinol nicotinate and up to 5 ampules of pentoxiphylline."( [Sudden hearing loss--our experience in treatment with vasoactive therapy].
Stojanović, S; Zivić, D; Zivić, L,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin glutathione reductaseSchistosoma mansoniPotency39.81070.100022.9075100.0000AID485364
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.79430.000229.305416,493.5996AID588514
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
lamin isoform A-delta10Homo sapiens (human)Potency6.30960.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (27)

Assay IDTitleYearJournalArticle
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.
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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (226)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990191 (84.51)18.7374
1990's17 (7.52)18.2507
2000's6 (2.65)29.6817
2010's9 (3.98)24.3611
2020's3 (1.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.12

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 Index11.12 (24.57)
Research Supply Index5.67 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index4.00 (0.95)

This Compound (11.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials30 (11.63%)5.53%
Reviews7 (2.71%)6.00%
Case Studies14 (5.43%)4.05%
Observational0 (0.00%)0.25%
Other207 (80.23%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]