Page last updated: 2024-12-07

kallidin, des-arg(10)-

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

Description

Kallidin, des-Arg(10)-, also known as Lys-bradykinin, is a peptide that is a potent vasodilator. It is a derivative of bradykinin, with the arginine residue at position 10 removed. This modification leads to an increase in its potency compared to bradykinin. Kallidin, des-Arg(10)-, is produced by the action of kininogenases on high molecular weight kininogen. It is found in various tissues and fluids, including plasma, saliva, and urine. The compound is involved in various physiological processes, including inflammation, pain, and blood pressure regulation. It exerts its effects by binding to the B2 receptor, a G protein-coupled receptor, leading to the activation of downstream signaling pathways. Kallidin, des-Arg(10)-, has been studied extensively for its potential therapeutic applications in conditions such as hypertension, inflammation, and pain. Its increased potency and longer half-life compared to bradykinin make it an attractive target for drug development. Research on Kallidin, des-Arg(10)-, continues to explore its pharmacological effects, potential therapeutic uses, and its role in various physiological processes.'

kallidin, des-Arg(10)-: includes both L and D isomers of Phe(8) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122227
CHEMBL ID264100
SCHEMBL ID20298769
MeSH IDM0149739

Synonyms (39)

Synonym
[des-arg10]kallidin
lys-[des-arg9]bk
kallidin1-9
[lys,des-arg9]bradykinin
lys-[des-arg9]-bradykinin
gtpl644
des-arg10-kallidin (lys-des-arg9 bradykinin)
kallidin[1-9]
NCGC00167261-01
bradykinin, lys-desarg(9)
lys-arg-pro-pro-gly-phe-ser-pro-phe
lys-des-arg(9)-bk
des-arg(10)-kallidin
bradykinin, lys-d-phe(8)-des-arg(9)
71800-36-7
10-de-arg-kallidin
kallidin, des-arginine(10)-
bradykinin, lysyl-des-arginine(9)
kallidin, des-arg(10)-
bdbm50156454
des-arg10-kallidin
CHEMBL264100 ,
(2s)-2-[[(2s)-1-[(2s)-2-[[(2s)-2-[[2-[[(2s)-1-[(2s)-1-[(2s)-2-[[(2s)-2,6-diaminohexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-
bradykinin, n2-l-lysyl-9-de-l-arginine-
[lys-des-arg9]-bradykinin
[3h]lys-[des-arg9]bk
[3h]-lys-[des-arg9]-bradykinin
gtpl3825
[3h]-lys-[des-arg9]bk
DTXSID50222058
lys-[des-arg9]bradykinin
AKOS024457490
SCHEMBL20298769
[lys-des-arg9]-bradykinin, >=95% (hplc)
1-9-kallidin
bdbm50214792
Q27077021
HY-103295
CS-0027286

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" ELN441958 is a novel small molecule bradykinin B(1) receptor antagonist exhibiting high oral bioavailability and potent systemic efficacy in rhesus monkey inflammatory pain."( Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958.
Bova, MP; Butelman, ER; Chavez, RA; Chen, L; Dreyer, M; Fukuda, JY; Garofalo, AW; Hawkinson, JE; Holcomb, R; Hom, DS; Ko, MC; Liao, A; Malmberg, AB; Ruslim, L; Samant, B; Simmonds, S; Szoke, BG; Wadsworth, A; Zeitz, KP; Zhang, H; Zmolek, W, 2007
)
0.34

Dosage Studied

ExcerptRelevanceReference
" However, when animals were pre-treated with BCG, the dose-response curves for both B1 agonists were shifted 2 to 8-fold to the left."( Systemic treatment with Mycobacterium bovis bacillus Calmette-Guérin (BCG) potentiates kinin B1 receptor agonist-induced nociception and oedema formation in the formalin test in mice.
Calixto, JB; de Campos, RO; Henriques, MG, 1998
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
B1 bradykinin receptorHomo sapiens (human)IC50 (µMol)0.00090.00091.62093.2410AID751693
B1 bradykinin receptorHomo sapiens (human)Ki0.00020.00020.09570.3820AID239710; AID751693
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (12)

Processvia Protein(s)Taxonomy
negative regulation of protein phosphorylationB1 bradykinin receptorHomo sapiens (human)
positive regulation of leukocyte migrationB1 bradykinin receptorHomo sapiens (human)
inflammatory responseB1 bradykinin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationB1 bradykinin receptorHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayB1 bradykinin receptorHomo sapiens (human)
response to mechanical stimulusB1 bradykinin receptorHomo sapiens (human)
cell migrationB1 bradykinin receptorHomo sapiens (human)
negative regulation of cell growthB1 bradykinin receptorHomo sapiens (human)
response to lipopolysaccharideB1 bradykinin receptorHomo sapiens (human)
negative regulation of blood pressureB1 bradykinin receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolB1 bradykinin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayB1 bradykinin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
bradykinin receptor activityB1 bradykinin receptorHomo sapiens (human)
protein bindingB1 bradykinin receptorHomo sapiens (human)
peptide bindingB1 bradykinin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
endoplasmic reticulumB1 bradykinin receptorHomo sapiens (human)
plasma membraneB1 bradykinin receptorHomo sapiens (human)
plasma membraneB1 bradykinin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1346495Human B1 receptor (Bradykinin receptors)1999European journal of pharmacology, Jun-25, Volume: 374, Issue:3
Molecular characterisation of cloned bradykinin B1 receptors from rat and human.
AID1346495Human B1 receptor (Bradykinin receptors)1997The Journal of biological chemistry, Apr-25, Volume: 272, Issue:17
Stable expression of the human kinin B1 receptor in Chinese hamster ovary cells. Characterization of ligand binding and effector pathways.
AID1346510Mouse B2 receptor (Bradykinin receptors)1994Molecular pharmacology, Jan, Volume: 45, Issue:1
Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
AID1346532Mouse B1 receptor (Bradykinin receptors)1996Immunopharmacology, Jun, Volume: 33, Issue:1-3
The agonist selectivity of a mouse B1 bradykinin receptor differs from human and rabbit B1 receptors.
AID1346495Human B1 receptor (Bradykinin receptors)1997British journal of pharmacology, Sep, Volume: 122, Issue:2
Stable expression of human kinin B1 receptor in 293 cells: pharmacological and functional characterization.
AID1346530Rat B1 receptor (Bradykinin receptors)1999European journal of pharmacology, Jun-25, Volume: 374, Issue:3
Molecular characterisation of cloned bradykinin B1 receptors from rat and human.
AID239710Binding affinity (radioligand) to human Bradykinin receptor B1 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay; value ranges from 0.1-0.2 nM2004Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
AID751758Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells at 10 uM after 60 mins relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID751693Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (79)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (1.27)18.7374
1990's24 (30.38)18.2507
2000's37 (46.84)29.6817
2010's16 (20.25)24.3611
2020's1 (1.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.74

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 Index11.74 (24.57)
Research Supply Index4.44 (2.92)
Research Growth Index6.18 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (5.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other76 (95.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]