Page last updated: 2024-11-08

substance p, sar(9)-met(o2)(11)-

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

Description

substance P, Sar(9)-Met(O2)(11)-: a neurokinin-1 receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID163829
CHEMBL ID1651026
MeSH IDM0173220

Synonyms (28)

Synonym
substance p [sar9,met(o2)11]
bdbm50335566
[sar...9...,met(o..2..)...11...]substance p
NCGC00167322-01
substance p, 9-(n-methylglycine)-11-(4-(methylsulfonyl)-l-2-aminobutanamide)-
9-sar-substance p sulfone
(sar(9))sp sulfone
bolton hunter-9-sar-11-met(02)-substance p
substance p, sarcosyl(9)-methionine(o2)(11)-
substance p, sar(9)-met(o2)(11)-
sarcosyl(9)-substance p sulfone
9-sar-11-met(o2)-substance p
9-sarcosyl-11-methionine(o2)-substance p
bolton-hunter reagent-substance p. sar(9)-met(02)(11)
substance p, sar(9) sulfone
substance p, sarcosyl(9)-methionine(02)(11)-bhr
(sar(9),met(o2)(11))sp
bhsar-sp
CHEMBL1651026 ,
(sar(9)kmet(o(2))(11))-substance p
8v0qafprxv ,
unii-8v0qafprxv
AKOS024456442
mfcd00076787
(sar9,met(o2)11)-substance p
sar9, met (o2)11-substance p
DB05875
[sar9,met(o2)11]-substance-p

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
" SR 48968 (10(-6) M shifted the [Pro9]SP dose-response curve but did not modify the septide dose-response curve."( Involvement of septide-sensitive tachykinin receptors in inositol phospholipid hydrolysis in the rat urinary bladder.
Beaujouan, JC; Glowinski, J; Saffroy, M; Torrens, Y, 1995
)
0.29
" The dose-response curves (0."( Substance P-(1-7) and substance P-(5-11) locally modulate dopamine release in rat striatum.
Brooks, N; Khan, S; Michael-Titus, AT; Whelpton, R, 1995
)
0.29
" Thus, we have compared the actions of the selective neurokinin 1 (NK1) (CP-99,994) and neurokinin 2 (NK2) (SR-48,968) receptor antagonists against dose-response curves (DRC) induced by intravenously administered substance P (SP), neurokinin A (NKA), neurokinin B (NKB), beta Ala8-NKA (4-10),Sar9-Met(O2)11SP, and single dose (intravenous) challenge with resiniferatoxin (RTX), a capsaicin-like sensory neurotoxin, leukotriene D4 (LTD4) and antigen."( NK1 and NK2 receptors mediate tachykinin and resiniferatoxin-induced bronchospasm in guinea pigs.
Champion, E; Foulon, DM; Jones, TR; Masson, P; Rodger, IW, 1993
)
0.29
[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)
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.00060.00000.09526.8130AID1285641; AID1336336; AID566270; AID751872; AID752234
Substance-P receptorHomo sapiens (human)Ki0.00010.00000.79368.7470AID751872
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

Processvia Protein(s)Taxonomy
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID752234Binding affinity to human NK1 receptor by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID751872Binding affinity to human NK1 receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID566270Inhibition of human tachykinin NK1 receptor2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID1285641Displacement of [125I]BH-SP from NK1 receptor in human U373MG cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID1336336Displacement of [125I]BH-SP from NK1 receptor in human U373MG cells measured after 30 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (148)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.68)18.7374
1990's100 (67.57)18.2507
2000's39 (26.35)29.6817
2010's8 (5.41)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other151 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]