Page last updated: 2024-11-10

nalorphine

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Description

Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5284595
CHEMBL ID415284
CHEBI ID7458
SCHEMBL ID38920
MeSH IDM0014439

Synonyms (57)

Synonym
n-allyl-normorphine
(1s,5r,13r,14s,17r)-4-(prop-2-en-1-yl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10,15-tetraene-10,14-diol
gtpl1629
(5alpha,6alpha)-17-prop-2-en-1-yl-7,8-didehydro-4,5-epoxymorphinan-3,6-diol
nalorfina
antorfin
nanm
morphinan-3,6-diol, 7,8-didehydro-4,5-epoxy-17-(2-propenyl)-, (5alpha,6alpha)-
nalorphin
antorphin
normorphine, n-allyl-
7,8-didehydro-4,5-epoxy-17-(2-propenyl)morphinan-3,6-diol
n-allyl-7,8-dehydro-4,5-epoxy-3,6-dihydroxymorphinan
anarcon
nalorphinium
norfin
nalorphine [inn:ban]
antorphine
einecs 200-546-1
n-allylnormorphine
nallin
anthorphine
n-allyl-n-desmethylmorphine
allorphine
nalorphinum [inn-latin]
morphinan-3,6-alpha-diol, 17-allyl-7,8-didehydro-4,5-alpha-epoxy-
nalorfina [dcit]
dea no. 9400
hsdb 3278
acetorfin [czech]
nalorphine
62-67-9
PDSP2_001572
NCGC00168255-01
nalorphine (inn)
nalorphine serb (tn)
D08247
nalorphine serb
CHEMBL415284
chebi:7458 ,
bdbm50367061
nalorphinum
u59wb2wry2 ,
acetorfin
unii-u59wb2wry2
SCHEMBL38920
nalorphine [mi]
nalorphine [mart.]
morphinan-3,6-diol, 7,8-didehydro-4,5-epoxy-17-(2-propenyl)-(5.alpha.,6.alpha.)-
nalorphine [inn]
nalorphine [who-dd]
nalorphine [hsdb]
UIQMVEYFGZJHCZ-SSTWWWIQSA-N
(4r,4ar,7s,7ar,12bs)-3-allyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol
DTXSID3023348
DB11490
Q2622916

Research Excerpts

Overview

summarize : Nalorphine is an unusual opiate.

ExcerptReferenceRelevance
"Nalorphine is an unusual opiate. "( Pharmacological characterization of nalorphine, a kappa 3 analgesic.
Pasternak, GW; Paul, D; Pick, CG; Tive, LA, 1991
)
2

Actions

ExcerptReferenceRelevance
"Nalorphine did not increase responding at any dose in the monkeys and the pigeons, nalorphine was only one-tenth as potent as naloxone in antagonizing the effects of morphine on FI and FR responding."( Some behavioral effects of morphine, naloxone and nalorphine in the squirrel monkey and the pigeon.
Goldberg, DM; Goldberg, SR; Morse, WH, 1976
)
1.23

Toxicity

ExcerptReferenceRelevance
"Sufentanil (R 30 730), N-[4-methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenylpropanamide, is a chemically novel, highly potent and extremely safe intravenous morphine-like agent in laboratory animals."( Sufentanil, a very potent and extremely safe intravenous morphine-like compound in mice, rats and dogs.
Janssen, PA; Niemegeers, CJ; Schellekens, KH; Van Bever, WF, 1976
)
0.26
"A simplified, safe and flexible technique of anesthesia, based on a limited number of relatively cheap drugs, and allowing ventilation with air, was applied to 60 patients undergoing operations of at least 60 minutes' duration."( A simple, cheap, effective and safe procedure for general anesthesia.
Lelkens, JP, 1976
)
0.26
" Nalorphine (20 mg/kg) did not affect the toxic action of kainic acid."( Effects of morphine, nalorphine and morphine withdrawal on lethal toxicity of intracerebroventricular kainic acid in mice.
Czuczwar, SJ; Kleinrok, Z; Turski, L, 1981
)
1.49

Dosage Studied

The relative potency in increasing sensitivity to naloxone was as follows: levorphan greater than morphine greater than Met-enkephalin greater than nalorphine greater than pentazocine. The analgesia dose-response curves for the surrogate pairs were parallel but had significantly different slopes.

ExcerptRelevanceReference
" Total daily drug intake was related to the unit dose delivered per injection in that a higher drug dosage led to more drug intake."( Intravenous self-administration of drugs in rats.
de Wied, D; Slangen, JL; van Ree, JM, 1978
)
0.26
" The analgesia dose-response curves for the surrogate pairs, nalodeine-nalorphine and codeine-morphine, were parallel but had significantly different slopes."( A comparative study of the analgesic and respiratory effects of N-allylnorcodeine (nalodeine), nalorphine, codeine and morphine.
Elliott, HW; Rundlett Beyer, J, 1976
)
0.71
"Morphine in therapeutic dosage has been shown to impair the plasma 11-hydroxycorticosteroid response to the stress of insulin-induced hypoglycaemia."( The effects of morphine and nalorphine on the plasma 11-hydroxycorticosteroid response to insulin-induced hypoglycaemia in patients with rheumatoid arthritis.
Bell, MA; Buchanan, W; Downie, WW; Nuki, G; Shenkin, A; Wasson, J, 1975
)
0.55
" But a number of kappa agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves."( Profile of activity of kappa receptor agonists in the rabbit vas deferens.
Hayes, A; Kelly, A, 1985
)
0.27
"Systemic administration of beta-funaltrexamine (beta-FNA) 24 hr before analgesic testing produced approximately a 10-fold parallel shift in the dose-response curves of the prototypic mu agonists morphine, I-methadone, fentanyl and etorphine in the mouse abdominal constriction test."( Use of beta-funaltrexamine to determine mu opioid receptor involvement in the analgesic activity of various opioid ligands.
Hynes, MD; Leander, JD; Reel, JK; Zimmerman, DM, 1987
)
0.27
" Schedule-controlled responding was disrupted when morphine maintenance was abruptly discontinued but not when the maintenance dosage was gradually reduced to zero."( Behavioral effects of naloxone and nalorphine preceding and following morphine maintenance in the rhesus monkey.
Bergman, J; Schuster, CR, 1985
)
0.55
" The dose-response relationship for hyperactivity in grouped mice following the injection of morphine sulphate has been established."( Monoamine mediation of the morphine-induced activation of mice.
Carroll, BJ; Sharp, PT, 1972
)
0.25
" Rats were dosed continuously with morphine hydrochloride by giving a daily dose through tubes connected to small, subcutaneously implanted reservoirs."( An implanted reservoir of morphine solution for rapid induction of physical dependence in rats.
Goode, PG, 1971
)
0.25
") produced a dose-response curve with a reduced maximum effect."( Relative involvement of receptor subtypes in opioid-induced inhibition of intestinal motility in mice.
Takemori, AE; Ward, SJ,
)
0.13
" The use of the newly developed piperidine derivative R 33799 at weight treated dosage levels can be strongly recommended for the immobilisation of hartebeest."( On the immobilization of hartebeest and kob in Upper Volta.
Dräger, N; Küpper, W; Mehlitz, D; Zillmann, U, 1981
)
0.26
" 2 The dose-response curves to naloxone obtained in tissues individually exposed to different opiates showed that their relative potency in increasing sensitivity to naloxone was as follows: levorphan greater than morphine greater than Met-enkephalin greater than nalorphine greater than pentazocine."( Pharmacological characterization of opiate physical dependence in the isolated ileum of the guinea-pig.
Luján, M; Rodríguez, R, 1981
)
0.44
" Naloxone (1 microM) or norbinaltorphimine (10 nM) shifted the dose-response curve of (-)-U50,488H to the right by 100-fold."( Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
Chen, C; Li, JG; Liu-Chen, LY; Luo, LY; Zhu, J, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
morphinane alkaloidAn isoquinoline alkaloid based on a morphinan skeleton and its substituted derivatives.
[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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency28.18380.35487.935539.8107AID624170
[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)IC50 (µMol)0.10950.00010.729810.0000AID150245; AID150246
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00400.00030.38877.0000AID1146187; AID1146188
Kappa-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.10950.00131.538010.0000AID150245; AID150246
Mu-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00400.00010.887410.0000AID1146187; AID1146188
Kappa-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00400.00050.36987.0000AID1146187; AID1146188
Mu-type opioid receptorHomo sapiens (human)Ki0.00030.00000.419710.0000AID1282207; AID410718
Delta-type opioid receptorHomo sapiens (human)Ki0.12000.00000.59789.9300AID410719
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.01500.00000.20186.4240AID149268
Kappa-type opioid receptorHomo sapiens (human)Ki0.00120.00000.362410.0000AID1282208; AID410720
Mu-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.10950.00081.699210.0000AID150245; AID150246
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00600.00040.16800.9772AID1146188
[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)
Histidine decarboxylaseRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00050.00150.0030AID1133438
Delta-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00050.36496.9000AID1133438
Mu-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00000.06470.9320AID1133438
Kappa-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00040.00390.0180AID1133438
[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)
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km2,075.00004.49006.51339.0000AID624630
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (74)

Processvia Protein(s)Taxonomy
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
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 (19)

Processvia Protein(s)Taxonomy
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
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 (27)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneKappa-type opioid receptorMus musculus (house mouse)
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 membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (108)

Assay IDTitleYearJournalArticle
AID114499Compound was administered subcutaneously and was evaluated for opioid agonist activity by antinociceptive tail-flick (TF) assay in mice; I denotes Inactive at 30 mg/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Racemic and optically active 2,9-dimethyl-5-(m-hydroxyphenyl)morphans and pharmacological comparison with the 9-demethyl homologues.
AID320413Antinociceptive activity in sc dosed mouse by hot plate method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID229192Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID150243Opioid receptors antagonist potency in reversing the effects of normorphine was determined in mouse isolated vas deferens1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.
AID1146187Displacement of [3H]-naloxone from rat opioid receptor after 30 mins by liquid scintillation counting analysis in absence of NaCl1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
AID624607Specific activity of expressed human recombinant UGT1A32000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID132133The effective dose was measured by using mouse writhing assay after the compound administered subcutaneously.1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Analgesic narcotic antagonists. 2. 8-Alkymorphinan-6-ones.
AID229190Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID410720Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID178879Narcotic antagonist activity against an ED80 of morphine in the modified rat tail-flick assay1981Journal of medicinal chemistry, Jun, Volume: 24, Issue:6
Analgesic narcotic antagonists. 5. 7,7-Dimethyldihydrocodeinones and 7,7-dimethyldihydromorphinones.
AID624620Specific activity of expressed human recombinant UGT2B7H2000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID180011The effective dose was measured by using rat tail flick assay after the compound administered intraperitoneally.1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Analgesic narcotic antagonists. 2. 8-Alkymorphinan-6-ones.
AID1146233Narcotic antagonist activity in rat at 1 to 10 mg/kg, sc by tail-flick test1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans.
AID624616Specific activity of expressed human recombinant UGT2B152000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID177002Dose (sc) required for a 2-s increase in reaction time in rat tail heat analgesia test1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
AID149268Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
AID231884Compound was tested for ability to protect against the irreversible antagonism of morphine''s effects by beta-FNA in guinea pig ileum at 1 uM concentration1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Different receptor sites mediate opioid agonism and antagonism.
AID624608Specific activity of expressed human recombinant UGT1A42000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID169767Narcotic antagonist activity was measured by rat tail flick procedure after the drug was injected intraperitoneally1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Novel opiates and antagonists. 5. 7-Carbethoxy-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones.
AID1146574Narcotic analgesic activity in sc dosed rat assessed as inhibition of phenazocine-induced effect by D'Amour-Smith tail flick test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
(2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists.
AID76240Opioid agonistic activity was measured in guinea pig ileum1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.
AID1146262Narcotic antagonist activity in morphine-dependent monkey by precipitated withdrawl test1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans.
AID231886Compound was tested for ability to protect against the irreversible antagonism of morphine''s effects by beta-FNA in guinea pig ileum at 200 nM concentration1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Different receptor sites mediate opioid agonism and antagonism.
AID229191Inhibition of specific binding of [3H]DTG to sigma receptor in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID320417Displacement of [3H]etorphine from opioid receptor in rat cerebrum2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID128019Inhibition of acetic acid induced mouse writhing assay following s.c. administration.1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Analgesic narcotic antagonists. 9. 6-Methylene-8 beta-alkyl-N-(cycloalkylmethyl)-3-hydroxy- or -methoxymorphinans.
AID151744Binding affinity to Opioid receptor mu 1 in rat brain using [3H]-NAL as radioligand1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
AID178684Narcotic antagonist activity in heat stimulus rat tail flick assay after subcutaneous administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Analgesic narcotic antagonists. 8. 7 alpha-Alkyl-4,5 alpha-epoxymorphinan-6-ones.
AID138523Opioid antagonist activity of compound was measured as inhibiting the binding of normorphine to mouse vas deferens1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.
AID1146261Narcotic antagonist activity in morphine-dependent monkey by single dose suppression test1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans.
AID1146575Narcotic analgesic activity in po dosed rat assessed as inhibition of phenazocine-induced effect by D'Amour-Smith tail flick test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
(2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists.
AID108540Compound was administered subcutaneously and was evaluated for opioid antagonist activity (versus morphine) by tail-flick (TF) antagonism test. 1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Racemic and optically active 2,9-dimethyl-5-(m-hydroxyphenyl)morphans and pharmacological comparison with the 9-demethyl homologues.
AID1146191Analgesic activity in Swiss-Webster mouse assessed as reduction of phenylquinine-induced writhing1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
AID1146247Narcotic analgesic activity in sc dosed mouse by Nilsen test1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans.
AID624640Drug glucuronidation reaction catalyzed by human recombinant UGT2B72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1145722Narcotic agonist activity in sc dosed albino mouse assessed as protection against acetylcholine-induced writhing administered 20 mins prior to acetylcholine challenge measured for 2 mins1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Synthesis and narcotic agonist-antagonist evaluation of some 2,6-methano-3-benzazocine-11 propanols. Analogues of the ring C bridged oripavine-7-mehtanols.
AID1133437Agonist activity at pig ileum opioid receptor1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1133441Narcotic antagonist activity in sc dosed rat assessed as inhibition of oxymorphone-induced straub tail effect1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID76232Irreversible antagonistic potency in guinea pig ileal longitudinal muscle (GPI)1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Importance of C-6 chirality in conferring irreversible opioid antagonism to naltrexone-derived affinity labels.
AID1146231Narcotic analgesic activity in sc dosed mouse by hot-plate test1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Synthesis and pharmacological activity of some N-alkyl-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans.
AID624621Specific activity of expressed human recombinant UGT2B7Y2000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID178158Antagonist activity in rat tail flick assay by intraperitoneal administration1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones.
AID178685Inhibition of morphine analgesia in modified rat tail flick test.1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Analgesic narcotic antagonists. 9. 6-Methylene-8 beta-alkyl-N-(cycloalkylmethyl)-3-hydroxy- or -methoxymorphinans.
AID1149608Analgesic activity in sc dosed mouse assessed as inhibition of phenylquinone-induced writhing1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
AID624613Specific activity of expressed human recombinant UGT1A102000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID128033Compound was tested for analgesic activity in mouse using mouse writhing test following subcutaneous administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1282208Binding affinity to human kappa opioid receptor2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
AID1146572Antiwrithing activity in sc dosed mouse assessed as prevention of phenyl-p-benzoquinone-induced abdominal constriction response1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
(2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists.
AID1146192In vivo inhibition of morphine-induced straub-tail response in sc dosed Swiss-Webster mouse measured for 30 mins1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID1149612Narcotic antagonist activity in sc dosed mouse assessed as inhibition of oxymorphone-induced narcosis1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
AID114494Compound was administered subcutaneously and was evaluated for opioid agonist activity by antinociceptive p-phenylquinone-writhing (PPQ) assay in mice1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Racemic and optically active 2,9-dimethyl-5-(m-hydroxyphenyl)morphans and pharmacological comparison with the 9-demethyl homologues.
AID229193Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID229189Inhibition of specific binding of [3H]3-PPP to sigma receptor in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID131000Compound was tested for narcotic antagonist potency using tail flick test in mouse following subcutaneous administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID230878Ratio of agonist potency to antagonist potency was determined1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones.
AID410721Ratio of Ki for human mu opioid receptor to Ki for human kappa opioid receptor expressed in CHO cells2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID624630Drug glucuronidation reaction catalyzed by human recombinant UGT1A12005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID129304Antinociceptive activity determined in acetic acid induced mouse writhing test1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
(-)-4-Hydroxymorphinanones: their synthesis and analgesic activity.
AID150245Concentration required to inhibit the stereospecific [3H]diprenorphine binding Opioid receptors in the absence of sodium(Na+) was determined in mouse isolated vas deferens1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.
AID131898Effective dose to show narcotic analgesic activity was evaluated in mouse tail-flick test when administered subcutaneously1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.
AID320415Antinociceptive activity in sc dosed mouse by tail flick method2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID128214Narcotic agonistic activity in acetic acid mouse writhing assay after subcutaneous administration of the drug1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Analgesic narcotic antagonists. 8. 7 alpha-Alkyl-4,5 alpha-epoxymorphinan-6-ones.
AID177941Antagonist activity (administered subcutaneously) determined by rat tail flick test1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
(-)-4-Hydroxymorphinanones: their synthesis and analgesic activity.
AID229188Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID125753Antagonistic activity to show narcotic effect induced by subcutaneous administration of 21.08 umol/kg of morphine in mouse tail-flick test1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.
AID114491Compound was administered subcutaneously and was evaluated for opioid agonist activity by antinociceptive hotplate (HP) assay in mice,1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Racemic and optically active 2,9-dimethyl-5-(m-hydroxyphenyl)morphans and pharmacological comparison with the 9-demethyl homologues.
AID132845Opioid agonistic activity was measured in mouse vas deferens1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.
AID1146570Antiwrithing activity in sc dosed mouse assessed as prevention of acetylcholine-induced abdominal constriction response1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
(2-exo-3-endo)-2-Aryltropane-3-carboxylic esters, a new class of narcotic antagonists.
AID410719Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID148625Evaluated the ability to protect against the irreversible antagonism of morphines effects by beta-FNA in guinea pig ileal longitudinal muscle.1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Different receptor sites mediate opioid agonism and antagonism.
AID131337Dose (sc) required for 50% reduction in frequency of writhing in mouse writhing analgesia test1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
AID229187Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID230879Ratio of agonist to that of antagonist activity1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Analgesic narcotic antagonists. 2. 8-Alkymorphinan-6-ones.
AID229186Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
AID1146188Displacement of [3H]-naloxone from rat opioid receptor after 30 mins by liquid scintillation counting analysis in presence of NaCl1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
AID320416Antinociceptive activity in sc dosed mouse assessed as inhibition of morphin response by tail flick assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID131018Analgesic agonist activity in acetic acid induced mouse writhing assay, subcutaneous administration1981Journal of medicinal chemistry, Jun, Volume: 24, Issue:6
Analgesic narcotic antagonists. 5. 7,7-Dimethyldihydrocodeinones and 7,7-dimethyldihydromorphinones.
AID1282207Binding affinity to human mu opioid receptor2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
AID410722Ratio of Ki for human delta opioid receptor to Ki for human kappa opioid receptor expressed in CHO cells2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID1133439Narcotic agonist activity in rat by writhing test1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID1133285Narcotic agonist activity in sc dosed mouse by acetylcholine writhing test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
2,6-Methano-3-benzazocine-11-ropanols. Lack of antagonism between optical antipodes and observation of potent narcotic antagonism by two n-methyl derivatives.
AID1146189Ratio of IC50 for rat opioid receptor in presence of NaCl to IC50 for rat opioid receptor in absence of NaCl1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics. 1. Synthesis and analgesic properties of N-sec-alkyl- and N-tert-alkylnormorphines.
AID1145723Narcotic antagonist activity in sc dosed rat assessed as 50% inhibition of phenazocine-induced response1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Synthesis and narcotic agonist-antagonist evaluation of some 2,6-methano-3-benzazocine-11 propanols. Analogues of the ring C bridged oripavine-7-mehtanols.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1149610Narcotic antagonist activity in sc dosed mouse assessed as inhibition of oxymorphone-induced straub tail response1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
AID1133287Narcotic antagonist activity in sc dosed rat assessed as antagonism of phenazocine response by tail flick assay1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
2,6-Methano-3-benzazocine-11-ropanols. Lack of antagonism between optical antipodes and observation of potent narcotic antagonism by two n-methyl derivatives.
AID128023Compound was tested for analgesia in mouse writhing assay by subcutaneous administration1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones.
AID1149613Narcotic antagonist activity in sc dosed rat assessed as inhibition of morphine-induced analgesic activity by tail flick test1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
AID17665Compound was evaluated for equilibrium constant, Ke1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Different receptor sites mediate opioid agonism and antagonism.
AID1133442Narcotic antagonist activity in sc dosed mouse assessed as inhibition of oxymorphone-induced nacrosis1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID128644Analgesic activity by mouse writhing test after subcutaneous injection.1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Novel opiates and antagonists. 5. 7-Carbethoxy-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones.
AID320414Antinociceptive activity in sc dosed mouse by phenylquinone antiwrithing assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
AID1133436Binding affinity to pig ileum opioid receptor1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID150246Concentration required to inhibit the stereospecific [3H]diprenorphine binding Opioid receptors in the presence of sodium(Na+) was determined in mouse isolated vas deferens1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.
AID624611Specific activity of expressed human recombinant UGT1A82000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID79203Opioid receptor antagonist activity as inhibiting binding of normorphine to guinea pig ileum1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.
AID1132930Inhibition of morphine-induced mania in sc dosed CD-1 mouse assessed as inhibition of stereotypic activity measured after 15 to 30 mins1978Journal of medicinal chemistry, Aug, Volume: 21, Issue:8
Synthesis and analgetic activity of some 5-aryl-2azabicyclo[3.2.1]octanes.
AID150242Opioid receptors antagonist potency in reversing the effects of Met5E was determined in mouse isolated vas deferens1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.
AID1133438Binding affinity to rat brain opioid receptor1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Quantum chemical studies of N-substituent variation in the oxymorphone series of opiate narcotics.
AID410718Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346364Human mu receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1346361Human delta receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
AID1346329Human kappa receptor (Opioid receptors)1997The Journal of pharmacology and experimental therapeutics, Aug, Volume: 282, Issue:2
Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands.
AID1346329Human kappa receptor (Opioid receptors)1998NIDA research monograph, Mar, Volume: 178Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,026)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990963 (93.86)18.7374
1990's43 (4.19)18.2507
2000's13 (1.27)29.6817
2010's7 (0.68)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 45.01

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 Index45.01 (24.57)
Research Supply Index7.07 (2.92)
Research Growth Index4.00 (4.65)
Search Engine Demand Index76.15 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (45.01)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials41 (3.62%)5.53%
Reviews48 (4.23%)6.00%
Case Studies9 (0.79%)4.05%
Observational0 (0.00%)0.25%
Other1,036 (91.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]