Page last updated: 2024-11-12

eledoisin

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

Description

Eledoisin: A peptide extracted from the posterior salivary glands of certain small octopi (Eledone spp., Mollusca), or obtained by synthesis. Its actions resemble those of SUBSTANCE P; it is a potent vasodilator and increases capillary permeability. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1364) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10328936
CHEMBL ID373569
CHEBI ID135903
SCHEMBL ID158143
MeSH IDM0007224

Synonyms (34)

Synonym
gtpl2086
eledone peptide
eledoisina [inn-spanish]
fi 6225 tf/ocoa
eledoisine [inn-french]
eld 950
brn 4796573
5-oxo-l-prolyl-l-prolyl-l-seryl-l-lysyl-l-aspartyl-l-alanyl-l-phenylalanyl-l-isoleucylglycyl-l-leucyl-l-methioninamide
eledoisin
eledoisinum
eledoisin [inn]
NCGC00167276-01
CHEBI:135903
bdbm50194558
CHEMBL373569 ,
eld-950
69-25-0
D07936
eledoisin (inn)
C20029
NTOC00000202-01
cas-69-25-0
dtxcid9026926
dtxsid1046926 ,
tox21_112815
oky3285j18 ,
eledoisina
eledoisine
unii-oky3285j18
SCHEMBL158143
eledoisin acetate
AKOS024456851
Q5358600
5-oxo-l-prolyl-l-prolyl-l-seryl-l-lysyl-l-alpha-aspartyl-l-alanyl-l-phenylalanyl-l-isoleucylglycyl-l-leucyl-l-methioninamide

Research Excerpts

Effects

ExcerptReferenceRelevance
"Eledoisin has been tried as a possible treatment for dry eye based on the hypothesis that it pharmacologically stimulates tear secretion when topically applied to the eye. "( Eledoisin and lacrimal secretion in the rabbit.
Dartt, DA; Gilbard, JP; Rossi, SR, 1990
)
3.16

Actions

ExcerptReferenceRelevance
"Eledoisin failed to cause tachyphylaxis under the conditions of these experiments."( Classification of tachykinin receptors in muscularis mucosae of opossum oesophagus.
Bowker, P; Cipris, S; Daniel, EE; Manaka, Y; Regoli, D, 1989
)
1

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The substance P antagonist produced parallel log dose-response curve shifts to both substance P and eledoisin on five in vitro smooth muscle preparations. The order of potency, the maximal effect and the slope of the dose- response curve were examined with six tachykinins - substance P (SP), physalaemin, phyllomedusin, uperolein, eledoin, kassinin.

ExcerptRelevanceReference
" Eledoisin did not alter the dose-response curve to noradrenaline and its inhibitory action is likely, therefore, to be presynaptic."( The actions of some vasoactive polypeptides and their antagonists on the anococcygeus muscle.
Gillespie, JS; McKnight, AT, 1978
)
1.17
" The order of potency, the maximal effect and the slope of the dose-response curve were examined with six tachykinins - substance P (SP), physalaemin, phyllomedusin, uperolein, eledoisin, kassinin - and several substance P fragments - SP-(2-11), SP-(3-11), SP-(4-11) and SP-(6-11)."( Interaction of tachykinins with an adrenergic receptor in the rat urinary bladder.
Mathison, R; Solomos, D, 1985
)
0.46
" Apnoea occurred with K and E throughout the effective dosage range."( Effect of substance P and other tachykinins on arterial pressure in guinea-pigs.
Hancock, JC; Hoover, DB, 1985
)
0.27
" When the concentration was raised to between 100 and 300 microM, however, the convulsants all reduced the monosynaptic reflex, thus producing a biphasic dose-response relationship."( Differing actions of convulsant and nonconvulsant barbiturates: an electrophysiological study in the isolated spinal cord of the rat.
Johnston, GA; Nicholson, GM; Spence, I, 1988
)
0.27
" At the beginning of an experiment some dose-response relationship could often be observed, but later tachyphylaxis developed."( The action of bombesin on the systemic arterial blood pressure of some experimental animals.
Erspamer, V; Melchiorri, P; Sopranzi, N, 1972
)
0.25
"The substance P antagonist [D-Arg1,D-Pro2,D-Trp7,9,Leu11]-substance P produced parallel log dose-response curve shifts to both substance P and eledoisin on five in vitro smooth muscle preparations."( Pharmacological characterization of a substance P antagonist, [D-Arg1,D-Pro2,D-Trp7,9,Leu11]-substance P.
Watson, SP, 1983
)
0.47
" Substance P was shown to produce rapid, small contractions of trhe lung strip at doses from 10(-9) to 10(-5) M, and there was no apparent dose-response relationship."( The effect of substance P and related peptides on the guinea-pig lung strip.
Foreman, JC; Webber, SE, 1984
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
peptideAmide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another with formal loss of water. The term is usually applied to structures formed from alpha-amino acids, but it includes those derived from any amino carboxylic acid. X = OH, OR, NH2, NHR, etc.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.53540.000214.376460.0339AID720691
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuromedin-K receptorHomo sapiens (human)IC50 (µMol)0.09600.00100.28822.9900AID738397
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuromedin-K receptorHomo sapiens (human)EC50 (µMol)0.00420.00020.08960.7930AID276405; AID276452; AID738396
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
tachykinin receptor signaling pathwayNeuromedin-K receptorHomo sapiens (human)
positive regulation of heart rateNeuromedin-K receptorHomo sapiens (human)
response to estradiolNeuromedin-K receptorHomo sapiens (human)
regulation of dopamine metabolic processNeuromedin-K receptorHomo sapiens (human)
response to cocaineNeuromedin-K receptorHomo sapiens (human)
positive regulation of blood pressureNeuromedin-K receptorHomo sapiens (human)
regulation of feeding behaviorNeuromedin-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionNeuromedin-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilityNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
protein bindingNeuromedin-K receptorHomo sapiens (human)
tachykinin receptor activityNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneNeuromedin-K receptorHomo sapiens (human)
dendrite membraneNeuromedin-K receptorHomo sapiens (human)
neuronal cell body membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346386Human NK3 receptor (Tachykinin receptors)1996The Journal of biological chemistry, Aug-23, Volume: 271, Issue:34
The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
AID1346386Human NK3 receptor (Tachykinin receptors)1992FEBS letters, Mar-24, Volume: 299, Issue:1
Molecular characterisation, expression and localisation of human neurokinin-3 receptor.
AID1346346Human NK1 receptor (Tachykinin receptors)1996The Journal of biological chemistry, Aug-23, Volume: 271, Issue:34
The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
AID188034Potency of compound was determined in rat duodenum relative to substance E1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID276405Activity at human NK3 receptor expressed in CHO cells assessed as increase in inositol phosphate generation2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
AID76469Potency of compound was determined for contraction of guinea pig vas deferens relative to substance P(=1)1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID738394Displacement of [125I]-NKA from NK2R (unknown origin) transfected in CHO cells at 10 uM by gamma counting analysis2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
AID738396Agonist activity at NK3R (unknown origin) transfected in CHO cells assessed as calcium influx at 10 mM2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
AID76468Potency of compound was determined for contraction of guinea pig ileum relative to substance P(=1)1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID276452Activity at human NK3 receptor assessed as stimulation of inositol phosphate generation in CHO cells2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
AID224494In vitro inhibition of protein synthesis in tobacco mosaic virus mRNA-encoded proteins in rabbit reticulocyte lysate2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Inhibition of protein synthesis by didemnins: cell potency and SAR.
AID144552Evaluated for the binding affinity against NK3 receptor at 1 uM1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.
AID738397Displacement of ([125I]-His3, MePhe7)-NKB from NK3R (unknown origin) transfected in CHO cells by gamma counting analysis2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
AID188035Potency of compound was determined in rat vas deferens relative to substance E1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID211355Potency for [3H]SP binding to Tachykinin receptor 1 in rat brain central nervous system (CNS)1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID86004Potency of compound was determined in hamster bladder relative to substance E1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID188033Potency of compound was determined for contraction of rat bladder relative to substance P(=1)1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Substance P.
AID738395Displacement of [125I]-BH-SP from NK1R (unknown origin) transfected in CHO cells at 10 uM by gamma counting analysis2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (461)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990401 (86.98)18.7374
1990's46 (9.98)18.2507
2000's9 (1.95)29.6817
2010's4 (0.87)24.3611
2020's1 (0.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 45.89

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index45.89 (24.57)
Research Supply Index6.20 (2.92)
Research Growth Index4.02 (4.65)
Search Engine Demand Index76.15 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (45.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (1.44%)5.53%
Reviews14 (2.87%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other466 (95.69%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]