Page last updated: 2024-11-10

robalzotan

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

Description

robalzotan: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3055171
CHEMBL ID1628569
SCHEMBL ID115079
MeSH IDM0353737

Synonyms (23)

Synonym
nad299
(3r)-3-(di(cyclobutyl)amino)-8-fluorochroman-5-carboxamide
gtpl72
azd-7371
robalzotan [inn]
(r)-3-(dicyclobutylamino)-8-fluoro-5-chromancarboxamide
robalzotan
(3r)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2h-chromene-5-carboxamide
CHEMBL1628569
robalzotan [inn:ban]
(r)-3-(dicyclobutylamino)-8-fluoro-5-chromancarboxamide.
unii-i18m56ogme
i18m56ogme ,
3-n,n-dicyclobutylamino-8-fluoro-3,4-dihydro-2h-1-benzopyran-5-carboxamide hydrogen tartrate monohydrate
AKOS022180489
SCHEMBL115079
DTXSID30168743
NCGC00370859-01
(r)-3-(dicyclobutylamino)-8-fluorochroman-5-carboxamide
DB06538
[(3r)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2h-chromene-5-carboxamide]
Q7340703
A13092

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" The present study tested the effect of different selective 5-HT(1A) receptor antagonists (WAY 100635, NAD-299, p-MPPI and LY 426965) in combination with a SSRI (paroxetine), on postsynaptic 5-HT function measured by increased expression of the immediate early gene, Arc."( Effect of different 5-HT1A receptor antagonists in combination with paroxetine on expression of the immediate-early gene Arc in rat brain.
Gray, K; Newson, M; Pei, Q; Sharp, T; Sprakes, M; Tordera, R, 2003
)
0.32

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
" Dose-response studies revealed differential effects of both antagonists in the areas examined."( Differential regional antagonism of 8-OH-DPAT-induced decrease in serotonin synthesis by two 5-HT1A receptor antagonists.
Larsson, LG; Ross, SB; Stenfors, C, 1998
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.68400.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency30.11160.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1997The Journal of pharmacology and experimental therapeutics, Oct, Volume: 283, Issue:1
The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1997The Journal of pharmacology and experimental therapeutics, Oct, Volume: 283, Issue:1
The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (25.81)18.2507
2000's14 (45.16)29.6817
2010's7 (22.58)24.3611
2020's2 (6.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.50

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

MetricThis Compound (vs All)
Research Demand Index18.50 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (3.03%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other32 (96.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]