Page last updated: 2024-11-12

fr181157

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

Cross-References

ID SourceID
PubMed CID23685469
CHEMBL ID132589
SCHEMBL ID8057380
MeSH IDM0470166

Synonyms (14)

Synonym
CHEMBL132589 ,
fr-181157
171046-15-4
acetic acid, (3-((2-(4,5-diphenyl-2-oxazolyl)-2-cyclohexen-1-yl)methyl)phenoxy)-, sodium salt, (s)-
unii-25633y557y
acetic acid, (3-(((1s)-2-(4,5-diphenyl-2-oxazolyl)-2-cyclohexen-1-yl)methyl)phenoxy)-, sodium salt
(s)-fr-181157
25633y557y ,
acetic acid, 2-(3-(((1s)-2-(4,5-diphenyl-2-oxazolyl)-2-cyclohexen-1-yl)methyl)phenoxy)-, sodium salt (1:1)
SCHEMBL8057380
Q27253917
sodium;2-[3-[[(1s)-2-(4,5-diphenyl-1,3-oxazol-2-yl)cyclohex-2-en-1-yl]methyl]phenoxy]acetate
HY-120123
CS-0070017

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Compound (R)-4 was shown to exhibit good pharmacokinetic properties in rats and dogs, and also good bioavailability in healthy volunteers."( Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
Hattori, K; Higaki, M; Koyama, S; Nishio, M; Okitsu, O; Sakane, K; Seki, J; Tabuchi, S; Tanaka, A; Taniguchi, K, 2005
)
0.33
" FR193262 (4), (R,R)-diphenyloxazolyl pyrrolidine derivative, displays high potency and agonist efficacy at the IP receptor and has good bioavailability in rats and dogs."( Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
Hattori, K; Koyama, S; Nishio, M; Okitsu, O; Sakane, K; Seki, J; Tabuchi, S; Taniguchi, K, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thromboxane A2 receptor Homo sapiens (human)Ki1.00000.00061.24073.8040AID238480; AID239014; AID239181
Prostaglandin E2 receptor EP1 subtypeHomo sapiens (human)Ki1.00000.00910.66351.5849AID238329; AID238965; AID239139
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Ki1.02000.00010.47443.1623AID238332; AID238968; AID239142
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.05400.00020.484110.0000AID239037
Prostaglandin F2-alpha receptorHomo sapiens (human)Ki1.00000.03103.38039.9910AID238423; AID238939; AID239124
Prostaglandin E2 receptor EP3 subtypeHomo sapiens (human)Ki4.86670.00031.70816.8000AID238331; AID238967; AID239141
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Ki1.00000.00100.54483.0000AID238330; AID238966; AID239140
Prostacyclin receptorHomo sapiens (human)IC50 (µMol)0.06000.00840.07040.2880AID271029
Prostacyclin receptorHomo sapiens (human)Ki0.05500.00320.49586.6280AID160755; AID238503; AID238689; AID239037; AID239198; AID271031
Prostacyclin receptorRattus norvegicus (Norway rat)IC50 (µMol)1.20001.20001.20001.2000AID271030
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki0.05400.00000.73078.0000AID239198
Prostaglandin D2 receptorHomo sapiens (human)Ki1.00000.00060.49131.4000AID238422; AID238938; AID239123
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.05400.00020.502310.0000AID239037
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (58)

Processvia Protein(s)Taxonomy
smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to nutrientThromboxane A2 receptor Homo sapiens (human)
response to xenobiotic stimulusThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood coagulationThromboxane A2 receptor Homo sapiens (human)
response to testosteroneThromboxane A2 receptor Homo sapiens (human)
thromboxane A2 signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to ethanolThromboxane A2 receptor Homo sapiens (human)
positive regulation of angiogenesisThromboxane A2 receptor Homo sapiens (human)
positive regulation of smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
cellular response to lipopolysaccharideThromboxane A2 receptor Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisThromboxane A2 receptor Homo sapiens (human)
inflammatory responseThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood pressureThromboxane A2 receptor Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane A2 receptor Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationThromboxane A2 receptor Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
negative regulation of cytokine productionProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of cytokine productionProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
immune responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
JNK cascadeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to mechanical stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
regulation of ossificationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of integrin activationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
T-helper cell differentiationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
regulation of stress fiber assemblyProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
bone developmentProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
ERK1 and ERK2 cascadeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
cellular response to mechanical stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of eosinophil extravasationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin F2-alpha receptorHomo sapiens (human)
parturitionProstaglandin F2-alpha receptorHomo sapiens (human)
positive regulation of cell population proliferationProstaglandin F2-alpha receptorHomo sapiens (human)
positive regulation of gene expressionProstaglandin F2-alpha receptorHomo sapiens (human)
response to estradiolProstaglandin F2-alpha receptorHomo sapiens (human)
response to lipopolysaccharideProstaglandin F2-alpha receptorHomo sapiens (human)
negative regulation of apoptotic processProstaglandin F2-alpha receptorHomo sapiens (human)
cellular response to prostaglandin D stimulusProstaglandin F2-alpha receptorHomo sapiens (human)
inflammatory responseProstaglandin F2-alpha receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin F2-alpha receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin F2-alpha receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
cell deathProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
positive regulation of fever generationProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
intestine smooth muscle contractionProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
negative regulation of gastric acid secretionProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to progesteroneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
regulation of cell population proliferationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerProstacyclin receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
cell-cell signalingProstacyclin receptorHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
response to lipopolysaccharideProstacyclin receptorHomo sapiens (human)
negative regulation of smooth muscle cell proliferationProstacyclin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstacyclin receptorHomo sapiens (human)
inflammatory responseProstacyclin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptorHomo sapiens (human)
male sex determinationProstaglandin D2 receptorHomo sapiens (human)
sleepProstaglandin D2 receptorHomo sapiens (human)
mast cell degranulationProstaglandin D2 receptorHomo sapiens (human)
adenosine metabolic processProstaglandin D2 receptorHomo sapiens (human)
cellular response to prostaglandin D stimulusProstaglandin D2 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin D2 receptorHomo sapiens (human)
inflammatory responseProstaglandin D2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
thromboxane A2 receptor activityThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityThromboxane A2 receptor Homo sapiens (human)
protein bindingThromboxane A2 receptor Homo sapiens (human)
D1 dopamine receptor bindingProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
protein bindingProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
prostaglandin F receptor activityProstaglandin F2-alpha receptorHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
guanyl-nucleotide exchange factor activityProstacyclin receptorHomo sapiens (human)
prostacyclin receptor activityProstacyclin receptorHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptorHomo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptorHomo sapiens (human)
protein bindingProstaglandin D2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
acrosomal vesicleThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear speckThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
plasma membraneProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
extracellular regionProstaglandin F2-alpha receptorHomo sapiens (human)
cytoplasmProstaglandin F2-alpha receptorHomo sapiens (human)
plasma membraneProstaglandin F2-alpha receptorHomo sapiens (human)
plasma membraneProstaglandin F2-alpha receptorHomo sapiens (human)
nuclear envelopeProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
membraneProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP3 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
cytosolProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
membraneProstaglandin D2 receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (68)

Assay IDTitleYearJournalArticle
AID246857Effective dose for in vivo activity in D-GalN/LPS-induced rat hepatic injury model2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID7380Pharmacokinetic property (t1/2beta) was measured in dog at the dose of 0.032 mg/kg i.v.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID9098Pharmacokinetic property (Cmax) was measured in dog at the dose of 0.032 mg/kg2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID238965Inhibition of [3H]-PGE-2 binding to human prostanoid EP1 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID237181Half life in dog after iv administration (n=2-3)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID247519Inhibition of ADP-induced aggregation of human platelets2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID11998Pharmacokinetic property (Cmax) was measured in rat at the dose of 0.32 mg/kg p.o.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID238480Inhibition of [3H]SQ-29,548 binding to human Prostanoid TP receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID239139Displacement of [3H]PGE-2 from human Prostanoid EP1 receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID239123Displacement of [3H]PGD-2 from human Prostanoid DP receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID60970In vitro inhibition of ADP-induced platelet aggregation using dog platelet rich plasma2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID238331Inhibition of [3H]-PGE-2 binding to Prostanoid EP3 receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID12525Pharmacokinetic property (AUC) was measured in rat at the dose of 0.32 mg/kg p.o.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID237182Half life in rat after iv administration (n=2-3)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID10974Pharmacokinetic property (CLtot)of the compound was measured in rat at the dose of 0.32 mg/kg i.v.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID238423Inhibition of [3H]-PGF-2 binding to human Prostanoid FP receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID238330Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID239124Displacement of [3H]PGF-2 from human Prostanoid FP receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID239037Inhibition of [3H]iloprost binding to human prostanoid IP receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID238938Inhibition of [3H]PGD-2 binding to human prostanoid DP receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID238966Inhibition of [3H]PGE-2 binding to human prostanoid EP2 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID13662Pharmacokinetic property (F) was measured in rat at the dose of 0.32 mg/kg2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID271031Displacement of [3H]iloprost from cloned human PGI2 receptor2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
AID236688Maximal plasma concentration in rats after 0.32 mg/kg oral dose, n=32005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID10679Pharmacokinetic property (Tmax) was measured in rat at the dose of 0.32 mg/kg p.o.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID9732Pharmacokinetic property (Tmax) was measured in dog at the dose of 0.032 mg/kg p.o.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID238329Inhibition of [3H]PGE-2 binding to Prostanoid EP1 receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID8339Pharmacokinetic property (AUC) was measured in dog at the dose of 0.032 mg/kg p.o.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID239198Displacement of [3H]iloprost from human Prostanoid IP receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID247512Inhibition of ADP-induced aggregation of rat platelets2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID92397In vitro inhibition of ADP-induced platelet aggregation using human platelet rich plasma2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID238968Inhibition of [3H]PGE-2 binding to human prostanoid EP4 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID239141Displacement of [3H]PGE-2 from human Prostanoid EP3 receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID8549Pharmacokinetic property (CLtot) was measured in dog at the dose of 0.032 mg/kg i.v.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID236685Maximal plasma concentration in dogs after 0.32 mg/kg oral dose, n=32005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID236149Bioavailability of the drug after i.v. administration at a dose of 0.32 (mg/kg) in rat2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID9500Pharmacokinetic property (F) was measured in dog at the dose of 0.032 mg/kg2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID236706Maximum (Peak) plasma drug concentration after single-dose administration at a dose of 0.32 (mg/kg) in rat2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID247890In vitro inhibition of ADP-induced platelet aggregation in rat platelet rich plasma2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
AID271030Agonist activity at rat PGI2 receptor assessed as inhibition of ADP-induced platelet aggregation2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
AID238422Inhibition of [3H]PGD-2 binding to human Prostanoid DP receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID238332Inhibition of [3H]PGE-2 binding to Prostanoid EP4 receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID236419Area Under Plasma concentration-time curve after peroral administration at a dose of 0.32 (mg/kg) in rat2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID239014Inhibition of [3H]SQ-29,548 binding to human prostanoid TP receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID236243Clearance in rat after iv administration (n=2-3)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID247889In vitro inhibition of ADP-induced platelet aggregation in dog platelet rich plasma2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
AID247525Inhibition of ADP-induced aggregation of monkey platelets2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID239140Displacement of [3H]-PGE-2 from human Prostanoid EP2 receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID239181Displacement of [3H]SQ-29,548 from human Prostanoid TP receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID237205Elimination half-life after peroral administration at a dose of 0.32 (mg/kg) in rat2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID160755In vitro Prostacyclin (PGI-2) receptor binding assay was determined based on displacement of [3H]iloprost radioligand from cloned human IP receptor2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID271032Oral bioavailability in rat2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
AID247511Inhibition of ADP-induced aggregation of dog platelets2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID236092Bioavailability in dog at 0.32 mg/kg after po administration (n=3)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID238689Ability to inhibit binding of [3H]iloprost to cloned human prostaglandin I2 receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
AID271029Agonist activity at human PGI2 receptor assessed as inhibition of ADP-induced platelet aggregation2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
AID238939Inhibition of [3H]PGF-2 binding to human prostanoid FP receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID13083Pharmacokinetic property (t1/2beta) was measured in rat at the dose of 0.32 mg/kg i.v.2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID247935In vitro inhibition of ADP-induced platelet aggregation in human platelet rich plasma2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.
AID238503Inhibition of [3H]-Iloprost binding to human Prostanoid IP receptor2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
AID271035Cmax in rat at 0.32 mg/kg, po2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
AID238967Inhibition of [3H]PGE-2 binding to human prostanoid EP3 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID196104In vitro inhibition of ADP-induced platelet aggregation using rat platelet rich plasma2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
AID236242Clearance in dog after iv administration (n=2-3)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID239142Displacement of [3H]PGE-2 from human Prostanoid EP4 receptor2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
AID236093Bioavailability in rat at 0.32 mg/kg after po administration (n=3)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.
AID271036AUC in rat at 0.32 mg/kg, po2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
AID237350Total body clearance of drug from the plasma after i.v. administration at a dose of 0.32 (mg/kg) in rat2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (100.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]