Page last updated: 2024-12-07

bw 373u86

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Description

BW 373U86: a nonpeptidic delta opioid receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID119029
CHEMBL ID25230
CHEBI ID114187
SCHEMBL ID232127
MeSH IDM0223039

Synonyms (53)

Synonym
bw373u86
4-[(r)-((2s,5r)-4-allyl-2,5-dimethyl-piperazin-1-yl)-(3-hydroxy-phenyl)-methyl]-n,n-diethyl-benzamide
4-((r)-((2s,5r)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-n,n-diethylbenzamide
bdbm50039026
4-[(4-allyl-2,5-dimethyl-piperazin-1-yl)-(3-hydroxy-phenyl)-methyl]-n,n-diethyl-benzamide(snc-86)
HMS3268M05 ,
BRD-K74990253-001-01-0
tocris-1663
NCGC00025250-01
bw 373u86
CHEBI:114187
bw-373u86
snc-86
CHEMBL25230 ,
4-[(r)-[(2s,5r)-2,5-dimethyl-4-prop-2-enylpiperazin-1-yl]-(3-hydroxyphenyl)methyl]-n,n-diethylbenzamide
benzamide, 4-((2,5-dimethyl-4-(2-propenyl)-1-piperazinyl)(3-hydroxyphenyl)methyl)-n,n-diethyl-, (1(s*),2alpha,5beta)-(+-)-
150428-54-9
(+-)-4-((alpha-r*)-alpha-((2s*,5r*)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-n,n-diethylbenzamide
benzamide, 4-((2,5-dimethyl-4-(2-propenyl)-1-piperazinyl)(3-hydroxyphenyl)methyl)-n,n-diethyl-, (1(s*),2alpha,5beta)-
rr2qfn29k7 ,
unii-rr2qfn29k7
4-[(r)-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)-(3-hydroxyphenyl)-methyl]-n,n-diethylbenzamide
4-[(r)-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)(3-hydroxyphenyl)methyl]-n,n-diethylbenzamide
4-((alpha-r)-alpha-((2s,5r)4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-n,n-diethylbenzamide
(+/-)-4-((alphar*)-alpha-((2s*,5r*)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxy -benzyl)-n,n-diethylbenzamide
(+/-)-4-((alphar*)-alpha-((2s*,5r*)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-n,n-diethylbenzamide
4-((alpha-r)-alpha-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-n,n-diethylbenzamide
LBLDMHBSVIVJPM-YZIHRLCOSA-N ,
(+/-)-4-((alphar*)-alpha-((2s*,5r*)-4-allyl-2,5dimethyl-1-piperazinyl)-3-hydroxybenzyl)-n,n-diethylbenzamide
4-[(r)-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl) (3-hydroxyphenyl)methyl]-n,n-diethylbenzamide
4-[(r)-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)(3-hydroxyphenyl)-methyl]-n,n-diethylbenzamide
(+/-)-4-((alphar*)-alpha((2s*,5r*)-4-allyi-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-n,n-diethylbenzamide
SCHEMBL232127
4-[(?r*)-?-((2s*,5r*)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl]-n,n-diethylbenzamide
155836-50-3
155836-52-5
4-[(ar*)-alpha-((2s*,5r*)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl]-n,n-diethylbenzamide
AKOS024456733
gtpl9002
SR-01000597509-1
sr-01000597509
(+)-bw373u86
(+)-4-[(r)-[(2s,5r)-2,5-dimethyl-4-(2-propenyl)-1-piperazinyl]-(3-hydroxyphenyl)methyl]-n,n-diethylbenzamide
HMS3676P19
DTXSID00933945
HMS3412P19
CS-0029464
HY-107751
benzamide, 4-[(r)-[(2s,5r)-2,5-dimethyl-4-(2-propen-1-yl)-1-piperazinyl](3-hydroxyphenyl)methyl]-n,n-diethyl-, rel-
rel-4-[(r)-[(2s,5r)-2,5-dimethyl-4-(2-propen-1-yl)-1-piperazinyl](3-hydroxyphenyl)methyl]-n,n-diethylbenzamide
benzamide, 4-[[2,5-dimethyl-4-(2-propenyl)-1-piperazinyl](3-hydroxyphenyl)methyl]-n,n-diethyl-, [1(s*),2alpha,5beta]-(+/-)-
bw-373u86, (+/-)-
155836-51-4

Research Excerpts

Overview

BW 373U86 is a novel, non-peptidic delta-opioid receptor ligand with agonist properties in mouse brain and in the mouse isolated vas deferens.

ExcerptReferenceRelevance
"BW 373U86 is a novel, non-peptidic delta-opioid receptor ligand with agonist properties in mouse brain and in the mouse isolated vas deferens. "( Binding of BW 373U86, a non-peptidic delta opioid receptor agonist, is not regulated by guanine nucleotides and sodium.
Borsodi, A; Chang, KJ; Fang, L; McNutt, RW; Porreca, F; Toth, G; Wild, KD; Yamamura, HI, 1993
)
2.12

Bioavailability

ExcerptReferenceRelevance
" Subsequent lead optimization identified compound 20 (ADL5859) as a potent, selective, and orally bioavailable delta agonist."( Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Ajello, CW; Barker, WM; Belanger, S; Brogdon, BL; Cassel, JA; Christ, DD; Chu, GH; DeHaven, RN; DeHaven-Hudkins, DL; Derelanko, MJ; Dolle, RE; Feschenko, MS; Graczyk, TM; Gu, M; Koblish, M; Kutz, S; Le Bourdonnec, B; Leister, LK; Little, PJ; Smith, SA; Tuthill, PA; Wiant, DD; Windh, RT, 2008
)
0.35

Dosage Studied

ExcerptRelevanceReference
" Administration of U50,488H (3 mg/kg), in conjunction with several doses of cocaine, did not shift the cocaine dose-response curve."( Assessment of the discriminative stimulus effects of cocaine in the rat: lack of interaction with opioids.
Broadbent, J; Dworkin, SI; Gaspard, TM,
)
0.13
" Cumulative dosing with cocaine (0."( Role of delta opioid receptors in the reinforcing and discriminative stimulus effects of cocaine in rhesus monkeys.
Lukas, SE; Mello, NK; Mendelson, JH; Negus, SS; Portoghese, PS, 1995
)
0.29
" Finally dose-response curves were found highly reproducible across transfection experiments, opening the possibility for a direct comparison of distinct recombinant receptor preparations."( [35S]GTP gamma S binding: a tool to evaluate functional activity of a cloned opioid receptor transiently expressed in COS cells.
Befort, K; Kieffer, BL; Tabbara, L, 1996
)
0.29
"01 mg/kg) prior to cumulative doses of cocaine produced dose-dependent leftward shifts in the cocaine dose-response function."( Opioid enhancement of the discriminative stimulus effects of cocaine: evidence for involvement of mu and delta opioid receptors.
Rowlett, JK; Spealman, RD, 1998
)
0.3
" When compared to desipramine and fluoxetine, SNC80 was more active with a single dose whereas both desipramine and fluoxetine produced greater effects with subchronic dosing (3 doses)."( Nonpeptidic delta-opioid receptor agonists reduce immobility in the forced swim assay in rats.
Broom, DC; Folk, JE; Jutkiewicz, EM; Rice, KC; Traynor, JR; Woods, JH, 2002
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[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 (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency21.13600.000811.382244.6684AID686978
cytochrome P450 2C9 precursorHomo sapiens (human)Potency3.98110.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency11.22020.001815.663839.8107AID894
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.58930.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.84890.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency3.98110.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
[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)
Delta-type opioid receptorMus musculus (house mouse)Ki0.00090.00000.53939.4000AID56283; AID56424
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.02000.00030.38877.0000AID149405; AID149522
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.00140.00000.60689.2330AID149649; AID149667
Mu-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.93460.00010.887410.0000AID151300; AID151443
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.02760.00000.38458.6000AID138708; AID141653; AID151606; AID152374
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00210.00010.813310.0000AID148355
Mu-type opioid receptorHomo sapiens (human)Ki0.26000.00000.419710.0000AID386608
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00020.00020.75218.0140AID148076
Delta-type opioid receptorHomo sapiens (human)Ki0.00030.00000.59789.9300AID386572
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00030.00030.71237.0700AID149405
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)0.02000.00001.201110.0000AID147858
Kappa-type opioid receptorHomo sapiens (human)Ki1.76500.00000.362410.0000AID386575; AID386607
[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)
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00030.00000.43328.3000AID148060; AID386574
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorRattus norvegicus (Norway rat)Activity0.00040.00000.11931.2200AID310939
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
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)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
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)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
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)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (51)

Assay IDTitleYearJournalArticle
AID151606Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
AID147858Binding affinity against cloned human Opioid receptor kappa 1 using [125I]-D-Pro10-dynorphin A[1-11] as radioligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID231107Ratio of binding affinities (Mu/Delta)1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
AID149649Affinity of [H]DADLE to the delta opioid receptor from rat brain2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
AID260584Agonist activity at delta opioid receptor in mouse vas deferens2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.
AID141645Evaluated for inhibition of [3H]DAMGO binding from mu receptor in rat brain membranes1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
AID56283Binding affinity towards opioid Delta receptor using [3H]DADLE as radioligand1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
AID78840Inhibition of the electrically induced muscle contractions was determined using the guinea pig ileum2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
AID386572Displacement of [3H]diprenorphine from human delta opioid receptor in CHO cells2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID19938Maximal efficacy (Emax value)2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID386575Displacement of [3H]diprenorphine from human kappa opioid receptor in CHO cells at 10 uM2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID386576Inhibition of human ERG channel in HEK293 cells by voltage-clamp method2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID231026Mu/delta inhibitory ratio of compound determined Rat brain receptors1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80)
AID149522Inhibition of radioligand [3H]DADLE binding to rat brain Opioid receptor delta 11997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80)
AID151300Binding affinity was measured against Opioid receptor mu 1 using [3H]-DAMGO as radioligand.1998Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.
AID310939Displacement of [3H]naltrindole from rat delta opioid receptor expressed in C6 cells2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Quantitative conformationally sampled pharmacophore for delta opioid ligands: reevaluation of hydrophobic moieties essential for biological activity.
AID386574Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID95361Binding affinity towards opioid kappa receptor using [3H]U69,593 as radioligand; not active1999Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
AID231108Ratio of binding affinities (Mu/Delta)1999Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
AID233969Ratio of binding affinity of mu opioid receptor to that of delta opioid receptor2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID56424Binding affinity towards opioid Delta receptor using [3H]DADLE as radioligand1999Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
AID231904Ratio between the IC50 values of mu and delta receptors1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
AID95360Binding affinity towards opioid kappa receptor using [3H]U-69593 as radioligand; Not available1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
AID30004Metabolic stability at a concentration of 10 uM in rat liver microsomes after 1 hr incubation2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID224725Binding affinity ratio between mu and delta receptor was determined2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
AID149667Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
AID151443Inhibition of radioligand [3H]DAMGO binding to rat brain Opioid receptor mu 1 using 100 nM DAMGO1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80)
AID152374Affinity of [3H]DAMGO to the mu opioid receptor from rat brain2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
AID148355Binding affinity against cloned human Opioid receptor mu 1 using [125I]FK33824 as radioligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID148660Tested for inhibition of binding of [3H]DADLE to mouse brain membranes depleted of mu binding sites by pretreatment with irreversible ligand BIT for delta opioid receptor1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
AID138708Binding affinity towards opioid Mu receptor using [3H]DAMGO as radioligand1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
AID148076Binding affinity against human opioid receptor delta 1 using [125I]-[D-Ala2]-deltorphin II as radioligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID148601Affinity to opioid receptor kappa 1 from rat brain using [3H]U-69593 as radioligand; NA =2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
AID386607Displacement of [3H]diprenorphine from human kappa opioid receptor in CHO cells2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID149405Binding affinity was measured against Opioid receptor delta 1 using [3H]p-Cl-DPDPE as radioligand.1998Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24
De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.
AID138330Inhibition of the electrically induced muscle contractions was determined using the mouse vas deferens2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
AID141653Binding affinity towards opioid Mu receptor using [3H]DAMGO as radioligand1999Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
AID148060Agonist potency was measured using GTP gamma-[35S] binding assay2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID386608Displacement of [3H]diprenorphine from human mu opioid receptor in CHO cells2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID30005Metabolic stability at a concentration of 100 uM in rat liver microsomes after 1 hr incubation2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346361Human delta receptor (Opioid receptors)2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID1346364Human mu receptor (Opioid receptors)2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
AID1346411Rat kappa receptor (Opioid receptors)1993The Journal of pharmacology and experimental therapeutics, Nov, Volume: 267, Issue:2
A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.
AID1346400Rat mu receptor (Opioid receptors)1993The Journal of pharmacology and experimental therapeutics, Nov, Volume: 267, Issue:2
A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.
AID1346406Rat delta receptor (Opioid receptors)1993The Journal of pharmacology and experimental therapeutics, Nov, Volume: 267, Issue:2
A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86.
AID1346329Human kappa receptor (Opioid receptors)2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (77)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's38 (49.35)18.2507
2000's35 (45.45)29.6817
2010's2 (2.60)24.3611
2020's2 (2.60)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.96

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 Index9.96 (24.57)
Research Supply Index4.39 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (2.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other78 (97.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]