Page last updated: 2024-11-11

bradyzide

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

Description

bradyzide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5312119
CHEMBL ID308468
SCHEMBL ID8488232
MeSH IDM0360580

Synonyms (8)

Synonym
gtpl680
(2s)-n-[2-(2-dimethylaminoethyl-methylamino)ethyl]-1-[4-[2-[di(phenyl)methylcarbamothioyl]hydrazinyl]-3-nitrophenyl]sulfonylpyrrolidine-2-carboxamide
bradyzide
CHEMBL308468 ,
SCHEMBL8488232
(2s)-1-[4-[2-(benzhydrylcarbamothioyl)hydrazinyl]-3-nitrophenyl]sulfonyl-n-[2-[2-(dimethylamino)ethyl-methylamino]ethyl]pyrrolidine-2-carboxamide
263011-13-8
Q27075476

Research Excerpts

Overview

Bradyzide inhibits B(2) receptor-induced (45)Ca efflux from NG108-15 cells with a pK(B) of 8.0+/-0.16 (n=5) and a Schild slope of 1.05. Bradyzide is a potent antagonist at the rat B2 receptor, but a weak one at the human receptor.

ExcerptReferenceRelevance
"Bradyzide is a competitive antagonist, inhibiting B(2) receptor-induced (45)Ca efflux from NG108-15 cells with a pK(B) of 8.0+/-0.16 (n=5) and a Schild slope of 1.05."( Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
Bloomfield, GC; Brown, MC; Burgess, GM; Campbell, EA; Davis, AJ; Davis, C; Drake, GS; Dunstan, A; Dziadulewicz, EK; Hallett, A; Hughes, GA; Lee, W; McIntyre, P; Perkins, MN; Phagoo, SB; Phillips, E; Rang, HP; Ritchie, TJ; Snell, CR; Urban, L; Wrigglesworth, R, 2000
)
2.47
"Bradyzide is a potent antagonist at the rat B2 receptor, but a weak one at the human receptor; a series of analogues in which the diphenylmethyl moiety of this drug has been substituted with dibenzosuberane have been reported to gain potency at the human B2 receptor, with some loss of affinity at the rat receptor."( A non-peptide antagonist unusually selective for the human form of the bradykinin B2 receptor.
Dziadulewicz, EK; Fortin, JP; Marceau, F; Morissette, G, 2003
)
1.04

Effects

ExcerptReferenceRelevance
"Bradyzide has high affinity for the rodent B(2) receptor, displacing [(3)H]-bradykinin binding in NG108-15 cells and in Cos-7 cells expressing the rat receptor with K(I) values of 0.51+/-0.18 nM (n=3) and 0.89+/-0.27 nM (n=3), respectively."( Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
Bloomfield, GC; Brown, MC; Burgess, GM; Campbell, EA; Davis, AJ; Davis, C; Drake, GS; Dunstan, A; Dziadulewicz, EK; Hallett, A; Hughes, GA; Lee, W; McIntyre, P; Perkins, MN; Phagoo, SB; Phillips, E; Rang, HP; Ritchie, TJ; Snell, CR; Urban, L; Wrigglesworth, R, 2000
)
2.47
[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)
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.00050.00010.739610.0000AID43308
B2 bradykinin receptorRattus norvegicus (Norway rat)Ki0.00050.00010.00030.0005AID43308
B2 bradykinin receptorHomo sapiens (human)Ki0.77200.00000.70577.6740AID43294
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
smooth muscle contractionB2 bradykinin receptorHomo sapiens (human)
inflammatory responseB2 bradykinin receptorHomo sapiens (human)
cell surface receptor signaling pathwayB2 bradykinin receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayB2 bradykinin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationB2 bradykinin receptorHomo sapiens (human)
blood circulationB2 bradykinin receptorHomo sapiens (human)
response to salt stressB2 bradykinin receptorHomo sapiens (human)
regulation of vasoconstrictionB2 bradykinin receptorHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationB2 bradykinin receptorHomo sapiens (human)
vasoconstrictionB2 bradykinin receptorHomo sapiens (human)
vasodilationB2 bradykinin receptorHomo sapiens (human)
regulation of vascular permeabilityB2 bradykinin receptorHomo sapiens (human)
arachidonic acid secretionB2 bradykinin receptorHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediatorB2 bradykinin receptorHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediatorB2 bradykinin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayB2 bradykinin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
protease bindingB2 bradykinin receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityB2 bradykinin receptorHomo sapiens (human)
bradykinin receptor activityB2 bradykinin receptorHomo sapiens (human)
protein bindingB2 bradykinin receptorHomo sapiens (human)
type 1 angiotensin receptor bindingB2 bradykinin receptorHomo sapiens (human)
protein heterodimerization activityB2 bradykinin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endosomeB2 bradykinin receptorHomo sapiens (human)
Golgi apparatusB2 bradykinin receptorHomo sapiens (human)
plasma membraneB2 bradykinin receptorHomo sapiens (human)
intracellular membrane-bounded organelleB2 bradykinin receptorHomo sapiens (human)
plasma membraneB2 bradykinin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID196528Duration of action (excess) in FCAT-induced mechanical hyperplasia in rats2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.
AID176439Oral efficacy against FCAT-induced mechanical hyperplasia in rats2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.
AID43294Displacement of [3H]BK (1 nM) from human Bradykinin receptor B2 expressed in Cos-7 cells2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.
AID43308Inhibition of specific binding of [3H]-BK (1 nM) to rat Bradykinin receptor B2 by 50% in NG108-15 cell membranes2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.
AID1347008Rat B2 receptor (Bradykinin receptors)2000British journal of pharmacology, Jan, Volume: 129, Issue:1
Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
AID1346473Human B2 receptor (Bradykinin receptors)2000British journal of pharmacology, Jan, Volume: 129, Issue:1
Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (60.00)29.6817
2010's3 (30.00)24.3611
2020's1 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.60

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 Index12.60 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.99 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.60)

All Compounds (24.57)

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%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]