Page last updated: 2024-11-13
af-219
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Gefapixant: a P2X3 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 24764487 |
CHEMBL ID | 3716057 |
SCHEMBL ID | 1493905 |
MeSH ID | M000605061 |
Synonyms (58)
Synonym |
---|
AF9 , |
S6664 |
HLWURFKMDLAKOD-UHFFFAOYSA-N |
5-(2,4-diamino-pyrimidin-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide |
R1646 , |
SCHEMBL1493905 |
mk-7264;af-219 |
CHEMBL3716057 |
rg1646 |
5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide |
af219 |
gtpl9540 |
lyfnua |
gefapixant |
5-((2,4-diamino-5-pyrimidinyl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide |
1015787-98-0 |
gefapixant [who-dd] |
ro-4926219 |
af-219 |
gefapixant [usan] |
5-((2,4-diaminopyrimidin-5-yl)oxy)-2-methoxy-4-(propan-2-yl)benzenesulfonamide |
ro4926219 |
5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzenesulfonamide |
benzenesulfonamide, 5-((2,4-diamino-5-pyrimidinyl)oxy)-2-methoxy-4-(1-methylethyl)- |
gefapixant [inn] |
r-1646 |
6K6L7E3F1L , |
rg-1646 |
unii-6k6l7e3f1l |
c14h19n5o4s |
af-219; mk-7264 |
5-((2,4-diaminopyrimidin-5-yl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide |
gefapixant(af-219,mk-7264) |
BCP26079 |
HY-101588 |
CS-0021727 |
DB15097 |
5-[2,4-bis(azanyl)pyrimidin-5-yl]oxy-2-methoxy-4-propan-2-yl-benzenesulfonamide |
gefapixant (usan/inn) |
EX-A2788 |
D11349 |
AMY27911 |
5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide |
benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)- |
ro 4926219 |
A934898 |
AKOS037515637 |
AC-35643 |
bdbm50533006 |
5-[(2,4-diamino-5-pyrimidinyl)oxy]-4-isopropyl-2-methoxybenzenesulfonamide |
mfcd24539325 |
SY282739 |
AS-78086 |
BM170818 |
DTXSID401337212 |
EN300-345539 |
Z2751991970 |
5-[(2,4-diaminopyrimidin-5-yl)oxy]-4-isopropyl-2-methoxybenzenesulfonamide |
Research Excerpts
Toxicity
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
" However, initial pharmacokinetic (PK) characterization of the P2X3-receptor antagonist gefapixant, developed to treat refractory or unexplained chronic cough, was performed in healthy participants who were predominantly younger adult males." | ( A Randomized, Placebo-Controlled Study to Investigate the Safety, Tolerability, and Pharmacokinetics of 3 Weeks of Orally Administered Gefapixant in Healthy Younger and Older Adults. Butera, P; Ford, A; Hussain, A; Iwamoto, M; Kitt, M; Nussbaum, J; Smith, S; Stoch, A, 2022) | 0.72 |
" We report a population pharmacokinetic (PopPK) analysis that characterizes gefapixant pharmacokinetics (PKs), quantifies between- and within-participant variability, and evaluates the impact of intrinsic and extrinsic factors on gefapixant exposure." | ( Population pharmacokinetic analysis of the P2X3-receptor antagonist gefapixant. Ait-Oudhia, S; Anton, J; Chawla, A; Gheyas, F; Hussain, A; Kleijn, H; Krishna Ananthula, H; La Rosa, C; Largajolli, A; Nussbaum, J, 2023) | 0.91 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
" Also, many of the P2R ligands still lack bioavailability due to charged groups or hydrolytic (either enzymatic or chemical) instability." | ( Medicinal chemistry of adenosine, P2Y and P2X receptors. Jacobson, KA; Müller, CE, 2016) | 0.43 |
Dosage Studied
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Pathways (1)
Pathway | Proteins | Compounds |
---|---|---|
Purinergic signaling | 0 | 53 |
Protein Targets (3)
Inhibition Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
P2X purinoceptor 3 | Rattus norvegicus (Norway rat) | Ki | 0.0708 | 0.0098 | 0.0403 | 0.0708 | AID1259561 |
P2X purinoceptor 3 | Homo sapiens (human) | IC50 (µMol) | 0.0450 | 0.0000 | 0.2030 | 1.5136 | AID1627253; AID1863330 |
P2X purinoceptor 3 | Homo sapiens (human) | Ki | 0.0891 | 0.0090 | 0.0466 | 0.0891 | AID1259562 |
P2X purinoceptor 2 | Homo sapiens (human) | Ki | 0.0891 | 0.0090 | 0.0466 | 0.0891 | AID1259562 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (27)
Molecular Functions (5)
Process | via Protein(s) | Taxonomy |
---|---|---|
purinergic nucleotide receptor activity | P2X purinoceptor 3 | Homo sapiens (human) |
extracellularly ATP-gated monoatomic cation channel activity | P2X purinoceptor 3 | Homo sapiens (human) |
ATP binding | P2X purinoceptor 3 | Homo sapiens (human) |
purinergic nucleotide receptor activity | P2X purinoceptor 2 | Homo sapiens (human) |
extracellularly ATP-gated monoatomic cation channel activity | P2X purinoceptor 2 | Homo sapiens (human) |
ATP binding | P2X purinoceptor 2 | Homo sapiens (human) |
ligand-gated monoatomic ion channel activity | P2X purinoceptor 2 | Homo sapiens (human) |
identical protein binding | P2X purinoceptor 2 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Ceullar Components (9)
Process | via Protein(s) | Taxonomy |
---|---|---|
plasma membrane | P2X purinoceptor 3 | Homo sapiens (human) |
axon | P2X purinoceptor 3 | Homo sapiens (human) |
Schaffer collateral - CA1 synapse | P2X purinoceptor 3 | Homo sapiens (human) |
hippocampal mossy fiber to CA3 synapse | P2X purinoceptor 3 | Homo sapiens (human) |
postsynapse | P2X purinoceptor 3 | Homo sapiens (human) |
receptor complex | P2X purinoceptor 3 | Homo sapiens (human) |
plasma membrane | P2X purinoceptor 3 | Homo sapiens (human) |
plasma membrane | P2X purinoceptor 2 | Homo sapiens (human) |
apical plasma membrane | P2X purinoceptor 2 | Homo sapiens (human) |
neuronal cell body | P2X purinoceptor 2 | Homo sapiens (human) |
postsynapse | P2X purinoceptor 2 | Homo sapiens (human) |
neuronal dense core vesicle | P2X purinoceptor 2 | Homo sapiens (human) |
receptor complex | P2X purinoceptor 2 | Homo sapiens (human) |
plasma membrane | P2X purinoceptor 2 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Bioassays (8)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1627255 | Kinetic solubility of the compound in phosphate buffer at pH 7.4 by HPLC analysis | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds. |
AID1627258 | Ratio of efflux to influx in human Caco2 cells | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds. |
AID1627257 | Permeability in vinblastine-treated human Caco2 cells | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds. |
AID1627256 | Intrinsic clearance in human liver microsomes at 1 to 2.5 uM in presence of NADPH | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds. |
AID1627253 | Antagonist activity at human recombinant P2X3 receptor expressed in HEK293-Tet-on cells assessed as alpha,beta-methylene-ATP-stimulated Ca2+ influx by Fluo-4 assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds. |
AID1863330 | Antagonist activity at human P2X3R expressed in HEK293 cells assessed as reduction in alphabeta-MeATP-induced intracellular Ca2+ influx pretreated with compound followed by alphabeta-MeATP addition and measured by Fluo-4 dye fluorescence analysis | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | AI-based prediction of new binding site and virtual screening for the discovery of novel P2X3 receptor antagonists. |
AID1627259 | Inhibition of human ERG relative to control | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | New P2X3 receptor antagonists. Part 1: Discovery and optimization of tricyclic compounds. |
AID1346621 | Human P2X3 (P2X receptors) | 2016 | Neuropharmacology, 05, Volume: 104 | Medicinal chemistry of adenosine, P2Y and P2X receptors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (41)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 7 (17.07) | 24.3611 |
2020's | 34 (82.93) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 25.65
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.
| This Compound (25.65) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 11 (26.83%) | 5.53% |
Reviews | 9 (21.95%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 21 (51.22%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |