Page last updated: 2024-11-11

vapiprost

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

Description

vapiprost: thromboxane receptor antagonist; prostaglandin receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918030
CHEMBL ID65030
SCHEMBL ID28550
MeSH IDM0166838

Synonyms (24)

Synonym
BRD-K02283807-003-01-4
gtpl1976
4-heptenoic acid, 7-(5-((1,1'-biphenyl)-4-ylmethoxy)-3-hydroxy-2-(1-piperidinyl)cyclopentyl)-, (1r-(1alpha(z),2beta,3beta,5alpha))-
vapiprostum [latin]
gr 32191
gr-32191
vapiprost [inn:ban]
vapiprost
CHEMBL65030 ,
bdbm50283049
(z)-7-[(1r,2r,3s,5s)-5-(biphenyl-4-ylmethoxy)-3-hydroxy-2-piperidin-1-yl-cyclopentyl]-hept-4-enoic acid
(z)-7-[(1r,2r,3s,5s)-3-hydroxy-5-[(4-phenylphenyl)methoxy]-2-piperidin-1-ylcyclopentyl]hept-4-enoic acid
h84xt1coau ,
vapiprostum
85505-64-2
unii-h84xt1coau
4-heptenoic acid, 7-(5-((1,1'-biphenyl)-4-ylmethoxy)-3-hydroxy-2-(1-piperidinyl)cyclopentyl)-, (1r-(1.alpha.(z),2.beta.,3.beta.,5.alpha.))-
(+)-(4z)-7-((1r,2r,3s,5s)-5-(4-biphenylmethoxy)-3-hydroxy-2-piperidinocyclopentyl)-4-heptenoic acid
vapiprost [inn]
SCHEMBL28550
DTXSID6048256
AKOS027378112
Q27089125
(4z)-7-[(1r,2r,3s,5s)-5-([1,1'-biphenyl]-4-ylmethoxy)-3-hydroxy-2-(1-piperidinyl)cyclopentyl]-4-heptenoic acid hydrochloride

Research Excerpts

Actions

ExcerptReferenceRelevance
"Vapiprost did not inhibit the primary aggregation or ATP release of human platelets stimulated with adenosine 5'-diphosphate (ADP), epinephrine (Epi) or platelet activating factor (PAF), but inhibited the secondary aggregation stimulated with those agonists at an IC50 of less than 1.3 x 10(-7) M."( The potent inhibition of vapiprost, a novel thromboxane A2 receptor antagonist, on the secondary aggregation and ATP release of human platelets.
Hiraishi, S; Horie, S; Ishii, H; Kazama, M; Kizaki, K; Kurusu, O; Nakahara, T; Noritake, S; Satoh, M; Yamada, M, 1997
)
1.32

Treatment

ExcerptReferenceRelevance
"Pretreatment with vapiprost (0.1, 0.3 and 1.0 mg kg-1, i.v., 5 min before the reaction) prolonged the time required to occlude the femoral artery in a dose-dependent manner."( Effects of vapiprost, a novel thromboxane receptor antagonist, on thrombus formation and vascular patency after thrombolysis by tissue-type plasminogen activator.
Matsuno, H; Nakashima, M; Takiguchi, Y; Uematsu, T; Umemura, K; Wada, K, 1992
)
1

Toxicity

ExcerptReferenceRelevance
" In CyA toxic rats, renal dysfunction can be partially reversed by inhibitors of thromboxane synthase."( Thromboxane receptor blockade improves cyclosporine nephrotoxicity in rats.
Coffman, T; Collins, D; Klotman, PE; Mayros, SD; Ruiz, P; Spurney, RF, 1990
)
0.28

Pharmacokinetics

Vapiprost was rapidly cleared from plasma, with an elimination half-life of 69-84 min. Across the dose range, vapiprost had a plasma clearance of 514-721 ml min-1.

ExcerptReferenceRelevance
" 4 Across the dose range, vapiprost was rapidly cleared from plasma, with an elimination half-life of 69-84 min and a plasma clearance of 514-721 ml min-1."( The pharmacodynamics and pharmacokinetics of a novel thromboxane receptor blocking drug vapiprost (GR32191) after single intravenous doses in healthy subjects.
Charter, MK; Chilton, JE; Keery, RJ; Lumley, P; Scully, NL; Thomas, M, 1991
)
0.8
"A selective thromboxane A2 (TXA2) receptor blocking agent, vapiprost, was orally administered to healthy male Japanese volunteers to investigate the pharmacokinetic and pharmacodynamic properties."( Pharmacokinetic and pharmacodynamic profiles of vapiprost, a selective, long-lasting thromboxane receptor antagonist, after single and multiple oral administration to healthy volunteers.
Hirano, K; Mizuno, A; Nagashima, S; Nakashima, M; Uematsu, T, 1991
)
0.78
"The effects of a single-dose oral administration of a thromboxane A2 receptor antagonist, vapiprost (SN-309), on pharmacokinetic profile and inhibition of platelet aggregation were investigated in six healthy elderly volunteers (age: 65-72 years) and the influence of age on these parameters was studied by comparison with the results obtained in phase-I data involving healthy young participants."( Influence of age on the pharmacokinetics of vapiprost, a thromboxane A2 receptor antagonist, and platelet aggregation: comparison of pharmacokinetics by routine approach and population pharmacokinetics.
Aso, R; Ohashi, K, 2001
)
0.79

Bioavailability

ExcerptReferenceRelevance
" The failure of a receptor blocker of leukotrienes to moderate disease expression suggests either a less important role for these chemicals in AOM or an insufficient bioavailability of the specific MK 571 inhibitor."( Expression of acute otitis media after receptor blockade of platelet activating factor, thromboxane, and leukotrienes in the chinchilla.
Alper, CM; Burckart, GJ; Diven, WF; Doyle, WJ; Evans, RW; Jaffe, R, 1998
)
0.3

Dosage Studied

ExcerptRelevanceReference
" Multiple dosing with GR32191, 17."( Preliminary assessment of a novel thromboxane A2 receptor-blocking drug, GR32191, in healthy subjects.
Lumley, P; Thomas, M, 1990
)
0.28
" These inhibitory effects were observed within 30 min and sustained for 24 h at a single dosage of 5 mg/kg of vapiprost."( The potent inhibition of vapiprost, a novel thromboxane A2 receptor antagonist, on the secondary aggregation and ATP release of human platelets.
Hiraishi, S; Horie, S; Ishii, H; Kazama, M; Kizaki, K; Kurusu, O; Nakahara, T; Noritake, S; Satoh, M; Yamada, M, 1997
)
0.81
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.07950.035520.977089.1251AID504332
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

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.
AID1346422Human TP receptor (Prostanoid receptors)1989British journal of pharmacology, Jul, Volume: 97, Issue:3
GR32191, a highly potent and specific thromboxane A2 receptor blocking drug on platelets and vascular and airways smooth muscle in vitro.
AID1346422Human TP receptor (Prostanoid receptors)1993British journal of pharmacology, Oct, Volume: 110, Issue:2
Characteristics of the binding of [3H]-GR32191 to the thromboxane (TP-) receptor of human platelets.
AID1346405Mouse TP receptor (Prostanoid receptors)1997British journal of pharmacology, Sep, Volume: 122, Issue:2
Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (129)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (6.20)18.7374
1990's106 (82.17)18.2507
2000's13 (10.08)29.6817
2010's2 (1.55)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.17

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 Index18.17 (24.57)
Research Supply Index4.99 (2.92)
Research Growth Index5.53 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (13.18%)5.53%
Reviews1 (0.78%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other111 (86.05%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]