Page last updated: 2024-12-11

enkephalinamide-leu, ala(2)-

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

Description

enkephalinamide-Leu, Ala(2)-: RN given refers to (L-leucinamide)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
Daleagenus[no description available]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID5486816
CHEMBL ID2311114
MeSH IDM0095891

Synonyms (21)

Synonym
2-ala-leu-enkephalinamide
dalea
(2s)-2-[(2s)-2-{2-[(2r)-2-[(2s)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]acetamido}-3-phenylpropanamido]-4-methylpentanamide
[d-ala2, leu5]enkephalin amide
bdbm21124
h-tyr-d-ala-gly -phe-leu-nh2
dale
(2s)-2-[[(2s)-2-[[2-[[(2r)-2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide
l-leucinamide, l-tyrosyl-d-alanylglycyl-l-phenylalanyl-
enkephalinamide-leu, ala(2)-
d-ale
leucine-enkephalinamide, ala(2)-
65189-64-2
leu-enkephalinamide, ala(2)-
enkephalinamide-leu, alanine(2)-
CHEMBL2311114
DTXSID40215494
tyr-d-ala-gly-phe-l-leu amide
[d-ala2] leu-enkephalinamide
HY-P3549
CS-0615666

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" A similar effect was obtained only with a dose 25 times higher (500 ng X kg-1) administered intravenously; at this dosage DALAMIDE administered intravenously also reduced the colonic motility index by 66%."( Central and peripheral control of gastrointestinal and colonic motility by endogenous opiates in conscious dogs.
Bueno, L; Fargeas, MJ; Fioramonti, J; Hondé, C; Primi, MP, 1985
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00590.00000.38458.6000AID1798043; AID1831030
Delta-type opioid receptorHomo sapiens (human)Ki0.00420.00000.59789.9300AID1798043; AID1831032
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID1831030Displacement of [3H]-DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cells assessed as inhibition constant by radioligand binding assay2021Bioorganic & medicinal chemistry, 12-01, Volume: 51C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
AID180325Inhibitory effect on the binding of 2 nM [3H]naloxone to rat brain membrane1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens.
AID226729Relative potency calculated from the ratio of IC50 of [Leu]-enkephalin to that of the compound1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens.
AID76218Inhibitory effect on electrically induced contraction of guinea pig ileum (GPI)1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens.
AID132836Inhibitory effect on electrically induced contraction of Mouse vas deferens (MVD)1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
A photoaffinity reagent to label the opiate receptors of guinea pig ileum and mouse vas deferens.
AID1831032Displacement of [3H]-DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells assessed as inhibition constant by radioligand binding assay2021Bioorganic & medicinal chemistry, 12-01, Volume: 51C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
AID1798043Radioligand Labeled Binding Assay from Article 10.1021/jm061465o: \\Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.\\2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (59)

TimeframeStudies, This Drug (%)All Drugs %
pre-199043 (72.88)18.7374
1990's12 (20.34)18.2507
2000's2 (3.39)29.6817
2010's1 (1.69)24.3611
2020's1 (1.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.11

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 Index10.11 (24.57)
Research Supply Index4.34 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.11)

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%
Other76 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]