Page last updated: 2024-12-07

ici 198615

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

Description

ICI 198615: an LTD4 receptor antagonist; SRS-A antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID115219
CHEMBL ID22033
SCHEMBL ID9806720
MeSH IDM0153210

Synonyms (36)

Synonym
PDSP1_000520
PDSP2_000518
ici 198615
CHEMBL22033 ,
ici-198615
carbamic acid, (1-((2-methoxy-4-(((phenylsulfonyl)amino)carbonyl)phenyl)methyl)-1h-indazol-6-yl)-, cyclopentyl ester
zm-198,615
104448-53-5
ici-198,615
zm 198615
(1-((2-methoxy-4-(((phenylsulfonyl)amino)carbonyl)phenyl)methyl)-1h-indazol-6-yl)carbamic acid cyclopentyl ester
[1-(4-benzenesulfonylaminocarbonyl-2-methoxy-benzyl)-1h-indazol-6-yl]-carbamic acid cyclopentyl ester
bdbm50009075
[1-(4-benzenesulfonylaminocarbonyl-2-methoxy-benzyl)-1h-indazol-6-yl]-carbamic acid cyclopentyl ester(ici 198, 615)
[1-(4-benzenesulfonylaminocarbonyl-2-methoxy-benzyl)-1h-indazol-5-yl]-carbamic acid cyclopentyl ester
[1-(4-benzenesulfonylaminocarbonyl-2-methoxy-benzyl)-1h-indazol-6-yl]-carbamic acid cyclopentyl ester (ici 198,615)
[1-(4-benzenesulfonylaminocarbonyl-2-methoxy-benzyl)-1h-indazol-6-yl]-carbamic acid cyclopentyl ester(ici 198615)
cyclopentyl n-[1-[[4-(benzenesulfonylcarbamoyl)-2-methoxyphenyl]methyl]indazol-6-yl]carbamate
[3h]ici-198,615
[3h]-ici198615
gtpl3358
[3h]ici198615
cyclopentyl n-[1-({4-[(benzenesulfonyl)carbamoyl]-2-methoxyphenyl}methyl)-1h-indazol-6-yl]carbamate
gtpl3414
[3h]ici-198615
ici198615
SCHEMBL9806720
DTXSID80146490
cyclopentyl (1-(2-methoxy-4-((phenylsulfonyl)carbamoyl)benzyl)-1h-indazol-6-yl)carbamate
Q27078030
AKOS040748555
cyclopentyl n-[1-[[2-methoxy-4-[[(phenylsulfonyl)amino]carbonyl]phenyl]methyl]-1h-indazol-6-yl]carbamate
4-((6-(cyclopentyloxycarbonylamino)indazol-1-yl)methyl)-3-methoxy-n-(phenylsulfonyl)benzenecarboximidic acid
zm-198615
carbamic acid, n-[1-[[2-methoxy-4-[[(phenylsulfonyl)amino]carbonyl]phenyl]methyl]-1h-indazol-6-yl]-, cyclopentyl ester
E9XYB5543A

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" LTD4 produced a positive inotropic response; however, rapid desensitization required the construction of noncumulative dose-response curves to naive tissues."( Evidence for leukotriene D4 receptors in guinea pig left atria.
Aharony, D; Falcone, RC; Orzechowski, RF, 1991
)
0.28
" Complete dose-response curves were first generated to LTC4, LTD4 and LTE4: those agents produced dose-dependent increases in arterial blood pressure, with ED20 values (i."( ICI 198615 is an antagonist of leukotriene C4, leukotriene D4 and leukotriene E4 vasopressor responses in the conscious rat.
Slivjak, MJ; Smith, EF, 1990
)
1.72
" Although LTC4 was as potent as LTD4 in stimulating TxB2 generation, LTC4's dose-response curve was shifted significantly to the right by AT-125, an irreversible gamma-glutamyl transpeptidase inhibitor, suggesting that at least a part of LTC4 sensitized lungs with antigen (0."( Evidence that peptidoleukotriene is a prerequisite for antigen-dependent thromboxane synthesis in IgG1-passively sensitized guinea pig lungs.
Breslow, R; Cheng, JB; Conklyn, MJ; Pillar, JS; Shirley, JT; Showell, HJ, 1990
)
0.28
" Infusion of the selective peptidoleukotriene receptor antagonist, SK&F 104353, produced dose-dependent shifts in the leukotriene D4 dose-response curve."( Evidence for high and low affinity leukotriene D4 receptors mediating vascular responses in the conscious rat.
Slivjak, MJ; Smith, EF, 1989
)
0.28
" This LTD4 antagonist was then evaluated to determine whether it could inhibit the IgE-mediated ascaris antigen response using the threshold antigen dose-response system or the single antigen dose-response system."( Effect of a leukotriene D4 (LTD4) antagonist on LTD4 and ascaris antigen-induced airway responses in rhesus monkeys.
Harris, KE; Krell, RD; Patterson, R, 1988
)
0.27
" The leukotriene receptor antagonist ICI-198,615 (3 x 10(-8)M) produced an approximate 50-fold rightward shift of the leukotriene C4 dose-response curve (n = 5)."( Influence of atherosclerosis on the vascular reactivity of isolated human epicardial coronary arteries to leukotriene C4.
Allen, SP; Chester, AH; Collins, M; Dashwood, MR; Piper, PJ; Tadjkarimi, S; Yacoub, MH, 1993
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID55072Compound was evaluated for its ability to displace [3H]LTD4 from LTD4 receptor in guinea pig lung membranes1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID55212Binding affinity against LTD4 receptor in guinea pig lung membranes.1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.
AID77399Tested in vivo for LTD4-induced bronchoconstriction after oral administration by Dermal wheal assay method1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID79874Inhibition of leukotriene-induced contractions of peripheral guinea pig lung strip1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID76433Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after intravenous administration at a dose of 10 mg/kg1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID55054Inhibitory activity to block binding of [3H]leukotriene D4 to LTD4 receptor sites in homogenized guinea pig lung at 10 uM1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID101460Dissociation constant KB = [antagonist]/(dose ratio -1).KB determined in guinea pig tracheal spirals with LTE4 as agonist1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles.
AID76429Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after aerosol administration as 1% solution1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76753In vivo percent protection against aerosolized LTD4 induced dyspnea in guinea pig at 10 umol/kg po (180 minutes post oral dosing); 37/81990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles.
AID233485Antagonist activity was determined1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Synthesis and in vitro LTD4 antagonist activity of bicyclic and monocyclic cyclopentylurethane and cyclopentylacetamide N-arylsulfonyl amides.
AID54903Inhibitory activity to block binding of [3H]leukotriene D4 to LTD4 receptor sites in homogenized guinea pig lung1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76976Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after intravenous administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76084Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after aerosol administration as 1% solution1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID55075In vitro binding affinity against cysteinyl leukotriene D4 receptor from guinea pig lung membrane1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID79332Antagonistic activity against LTD4 induced contraction in guinea pig trachea1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID76901In vivo percent protection against aerosolized LTD4 induced dyspnea in guinea pig at 30 umol/kg po (180 minutes post oral dosing); 89/81990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles.
AID74774In vitro antagonism of 8 nM of peptidoleukotriene (LTE4) induced contraction of guinea pig tracheal spirals at 0.033 X E-7M concentration1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles.
AID74773In vitro antagonism of 8 nM of peptidoleukotriene (LTE4) induced contraction of guinea pig tracheal spirals at 0.01 X E-7M concentration1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
A novel series of selective leukotriene antagonists: exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles.
AID77465Tested in vivo for antigen-induced systemic anaphylaxis after oral administration1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID1346031Human CysLT1 receptor (Leukotriene receptors)1992Biochemical pharmacology, Oct-06, Volume: 44, Issue:7
Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.
AID1346073Human CysLT2 receptor (Leukotriene receptors)1992Biochemical pharmacology, Oct-06, Volume: 44, Issue:7
Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (72)

TimeframeStudies, This Drug (%)All Drugs %
pre-199015 (20.83)18.7374
1990's55 (76.39)18.2507
2000's2 (2.78)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]

Market Indicators

Research Demand Index: 10.36

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 Index10.36 (24.57)
Research Supply Index4.29 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (4.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other69 (95.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]