Page last updated: 2024-11-07

rg 12525

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

Description

RG 12525: leukotriene D4 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID129044
CHEMBL ID18518
SCHEMBL ID1223335
MeSH IDM0164516

Synonyms (24)

Synonym
brn 3573814
rg 12525
quinoline, 2-((4-((2-(1h-tetrazol-5-ylmethyl)phenyl)methoxy)phenoxy)methyl)-
2-((4-((2-(1h-tetrazol-5-ylmethyl)phenyl)methoxy)phenoxy)methyl)quinoline
rg-12525
L001358
CHEMBL18518 ,
2-{4-[2-(1h-tetrazol-5-ylmethyl)-benzyloxy]-phenoxymethyl}-quinoline (rg 12525)
2-{4-[2-(1h-tetrazol-5-ylmethyl)-benzyloxy]-phenoxymethyl}-quinoline
2-{4-[2-(1h-tetrazol-5-ylmethyl)-benzyloxy]-phenoxymethyl}-quinoline(rg 12525)
bdbm50006799
2-[[4-[[2-(2h-tetrazol-5-ylmethyl)phenyl]methoxy]phenoxy]methyl]quinoline
unii-1l8mx40l35
1l8mx40l35 ,
120128-20-3
SCHEMBL1223335
nid 525
DTXSID30152687
nid-525
CS-6763
HY-101676
2-((4-((2-((1h-tetrazol-5-yl)methyl)benzyl)oxy)phenoxy)methyl)quinoline
Q27252567
AKOS040742545

Research Excerpts

Overview

RG 12525 is a new oral leukotriene D4 (LTD4) antagonist with proven activity in animal and human models. It is being evaluated for the treatment of type II diabetes.

ExcerptReferenceRelevance
"RG 12525 is a new oral leukotriene D4 (LTD4) antagonist with proven activity in animal and human models of leukotriene-induced bronchoconstriction. "( Effect of RG 12525, a new leukotriene antagonist, on pulmonary function of asthmatic adults.
Feiss, G; Nelson, HS; Paull, BR; Smith, JA; Tobey, RE; Welch, MJ, 1994
)
2.13
"RG 12525 is a new chemical entity recently evaluated for the treatment of type II diabetes. "( Characterization of 2-[[4-[[2-(1H-tetrazol-5-ylmethyl)phenyl]methoxy]methyl]quinoline N-glucuronidation by in vitro and in vivo approaches.
Cassidy, KC; Fayer, JL; Stevens, JC, 2001
)
1.75

Bioavailability

ExcerptReferenceRelevance
" The possibility also existed for inhibition of intestinal and hepatic CYP3A4 by RG 12525 to reduce "first-pass" metabolism and increase absolute bioavailability of CYP3A4 substrates orally coadministered."( Lack of correlation between in vitro inhibition of CYP3A-mediated metabolism by a PPAR-gamma agonist and its effect on the clinical pharmacokinetics of midazolam, an in vivo probe of CYP3A activity.
Fayer, JL; Kirkesseli, S; Luo, Y; Sidhu, R; Stevens, JC; Zannikos, PN, 2001
)
0.54

Dosage Studied

The pharmacokinetics of oral midazolam, a probe for intestinal and hepatic CYP3A activity, was not influenced by either the low (100 mg qd for 4 days) or high (600 mg qD for4 days) RG 12525 dosing regimen. Total plasma concentrations of inhibitor were well above in vitro Ki values.

ExcerptRelevanceReference
" RG 12525 800 mg displaced the dose-response curve for LTD4 to the right."( Effect of RG 12525, an oral leukotriene D4 antagonist, on the airway response to inhaled leukotriene D4 in subjects with mild asthma.
Tattersfield, AE; Wahedna, I; Wisniewski, AS, 1991
)
1.59
" Bronchodilator activity was assessed by spirometry before and at multiple time points after dosing for eight hours."( Effect of RG 12525, a new leukotriene antagonist, on pulmonary function of asthmatic adults.
Feiss, G; Nelson, HS; Paull, BR; Smith, JA; Tobey, RE; Welch, MJ, 1994
)
0.69
" The pharmacokinetics of oral midazolam, a probe for intestinal and hepatic CYP3A activity, was not influenced by either the low (100 mg qd for 4 days) or high (600 mg qd for4 days) RG 12525 dosing regimen despite the resulting total plasma concentrations of inhibitor that were well above in vitro Ki values."( Lack of correlation between in vitro inhibition of CYP3A-mediated metabolism by a PPAR-gamma agonist and its effect on the clinical pharmacokinetics of midazolam, an in vivo probe of CYP3A activity.
Fayer, JL; Kirkesseli, S; Luo, Y; Sidhu, R; Stevens, JC; Zannikos, PN, 2001
)
0.5
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Ki0.00300.00010.23581.5000AID55067
Cysteinyl leukotriene receptor 2Homo sapiens (human)Ki0.00300.00020.94296.2000AID55237
Cysteinyl leukotriene receptor 1Homo sapiens (human)Ki0.00300.00021.56248.8720AID55237
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Kb0.00300.00300.22100.4800AID55224
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
immune responseCysteinyl leukotriene receptor 2Homo sapiens (human)
leukotriene signaling pathwayCysteinyl leukotriene receptor 2Homo sapiens (human)
neuropeptide signaling pathwayCysteinyl leukotriene receptor 2Homo sapiens (human)
inflammatory response to antigenic stimulusCysteinyl leukotriene receptor 1Homo sapiens (human)
calcium ion transportCysteinyl leukotriene receptor 1Homo sapiens (human)
chemotaxisCysteinyl leukotriene receptor 1Homo sapiens (human)
defense responseCysteinyl leukotriene receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationCysteinyl leukotriene receptor 1Homo sapiens (human)
respiratory gaseous exchange by respiratory systemCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of angiogenesisCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of vasoconstrictionCysteinyl leukotriene receptor 1Homo sapiens (human)
establishment of localization in cellCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of glial cell proliferationCysteinyl leukotriene receptor 1Homo sapiens (human)
leukotriene signaling pathwayCysteinyl leukotriene receptor 1Homo sapiens (human)
cellular response to hypoxiaCysteinyl leukotriene receptor 1Homo sapiens (human)
neuropeptide signaling pathwayCysteinyl leukotriene receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
leukotriene receptor activityCysteinyl leukotriene receptor 2Homo sapiens (human)
protein bindingCysteinyl leukotriene receptor 2Homo sapiens (human)
cysteinyl leukotriene receptor activityCysteinyl leukotriene receptor 2Homo sapiens (human)
G protein-coupled peptide receptor activityCysteinyl leukotriene receptor 2Homo sapiens (human)
leukotriene receptor activityCysteinyl leukotriene receptor 1Homo sapiens (human)
cysteinyl leukotriene receptor activityCysteinyl leukotriene receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityCysteinyl leukotriene receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
cellular_componentCysteinyl leukotriene receptor 2Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 2Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 2Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 1Homo sapiens (human)
membraneCysteinyl leukotriene receptor 1Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay IDTitleYearJournalArticle
AID229063The effective dose for inhibition of LTD4-induced wheal formation after oral administration1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID55224Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig lung was determined using [3H]LTD4 (0.2 nM) at compound concentration of 1 uM1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
AID184420The compound was tested for inhibition of [3H]LTD4 binding to lung membrane1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
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.
AID227923Compound was tested for spasmogenic activity of LTE4 on lung strips1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID79331Antagonistic activity against LTD4 induced contraction in guinea pig lung parenchymal strips1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID229064The effective dose for inhibition of anaphylactic death after oral administration1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID77262Oral activity expressed as effective dose in LTD4-induced wheal assay in guinea pig1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
AID227922Compound was tested for spasmogenic activity of LTD4 on lung strips1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID77265Oral activity expressed as effective dose in leukotriene mediated anaphylaxis assay in guinea pig1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
AID88888LTD4 induced broncho constriction (shift in dose response curve 2 hr following 800 mg oral dose)1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID76080Inhibition of LTC4-induced contractions from guinea pig peripheral lung strips1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
AID227921Compound was tested for spasmogenic activity of LTC4 on lung strips1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID55071Compound was evaluated for its ability to displace [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranes1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID55237Binding affinity against Cysteinyl leukotriene D4 receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID79494Compound was tested for LTD4 guinea pig trachea contraction.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID55067Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig lung was determined using [3H]-LTD4 (0.2 nM)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (14.29)18.7374
1990's10 (71.43)18.2507
2000's2 (14.29)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: 11.96

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 Index11.96 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.85 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (21.43%)5.53%
Reviews4 (28.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]