Page last updated: 2024-11-11

naloxone hydrochloride

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Description

naloxone hydrochloride : A hydrochloride resulting from the formal reaction of equimolar amounts of naloxone and hydrogen chloride. A specific opioid antagonist, it is used to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. [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]

Cross-References

ID SourceID
PubMed CID5464092
CHEMBL ID1718
CHEBI ID31892
SCHEMBL ID41390
MeSH IDM0330064

Synonyms (107)

Synonym
nalonee
narcanti
naloxone hcl
normorphinone, n-allyl-7,8-dihydro-14-hydroxy-, hydrochloride, (-)-
17-allyl-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride
c19h21no4.hcl
einecs 206-611-0
en 15304
morphinan-6-one, 17-allyl-4,5-alpha-epoxy-3,14-dihydroxy-, hydrochloride
17-allyl-4,5-alpha-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride
nih 7890
l-n-allyl-14-hydroxynordihydromorphinone hydrochloride
morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, hydrochloride, (5alpha)-
(-)-n-allyl-14-hydroxynordihydromorphinone hydrochloride
(5alpha)-17-allyl-4,5-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride
naloxone hydrochloride
357-08-4
PRESTWICK_879
evzio (tn)
naloxone hydrochloride (jp17/usp)
narcan (tn)
D01340
hydrochloride, naloxone
CHEMBL1718
nsc-757109
naloxone hydrochloride anhydrous
anhydrous naloxone hydrochloride
chebi:31892 ,
naloxoni hydrochloridum anhydrous
en-15304
HMS1568G04
unii-f850569pqr
evzio
naloxone hydrochloride [usan:usp:jan]
nsc 757109
f850569pqr ,
HY-17417
naloxone (hydrochloride) ,
CS-1335
S3066
naloxone hydrochloride [orange book]
targiniq component naloxone hydrochloride
talwin nx component naloxone hydrochloride
naloxone hydrochloride component of suboxone
naloxone hydrochloride [who-dd]
naloxone hydrochloride [mart.]
naloxoni hydrochloridum anhydrous [who-ip latin]
suboxone component naloxone hydrochloride
kloxxado
naloxone hydrochloride [jan]
naloxone hydrochloride [usan]
naloxone hydrochloride component of talwin nx
naloxone hydrochloride component of targiniq
naloxone hydrochloride [usp monograph]
naloxone hydrochloride [vandf]
naloxone hydrochloride [green book]
morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, hydrochloride, (5.alpha.)-
naloxone hydrochloride [mi]
naloxone hydrochloride anhydrous [who-ip]
CCG-220111
NC00587
SCHEMBL41390
RGPDIGOSVORSAK-STHHAXOLSA-N
W-106655
AKOS024418753
(5?)-4,5-epoxy-3,14-dihydro-17-(2-propenyl)morphinan-6-one hydrochloride
HB2451
(5alpha)-4,5-epoxy-3,14-dihydro-17-(2-pr openyl)morphinan-6-one hydrochloride
(5a)-4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)-morphinan-6-one hydrochloride
(17r)-17-allyl-3,14-dihydroxy-6-oxo-4,5alpha-epoxymorphinan-17-ium chloride
(5alpha,17r)-17-allyl-3,14-dihydroxy-6-oxo-4,5-epoxymorphinan-17-ium chloride
17-allyl-3,14-dihydroxy-4,5alpha-epoxymorphinan-6-one hydrochloride
(5alpha)-17-allyl-3,14-dihydroxy-4,5-epoxymorphinan-6-one hydrochloride
mfcd00069322
nafoxone hydrochloride
KS-5379
sr-01000597918
SR-01000597918-1
SR-01000737374-3
sr-01000737374
(4r,4as,7ar,12bs)-3-allyl-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7ah)-one hydrochloride
nal-oxon hydrochloride
SW197001-3
357-08-4 (hcl)
Q27114711
DTXSID70957097 ,
(4r,4as,7ar,12bs)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one;hydrochloride
(4r,4as,12bs)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one;hydrochloride
(5alpha)-4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)morphinan-6-one hydrochloride (1:1)
naloxone?hydrochloride
evzio(r) naloxone hcl
naloxone hydrochloride (autoinjector)
zimhi
dtxcid701385046
(5r,14s)-17-allyl-4,5-epoxy-3,14-dihydroxymorphinan-6-one monohydrochloride
rextovy
nalxone hydrochloride
naloxone hci
naloxone hydrochloride (usp monograph)
naloxone hydrochloride injection, usp, auto-injector
evzio (autoinjector)
narcan naloxone hci
naloxone hydrochloride nasal spray
naloxone hydrochloride (usan:usp:jan)
rivive
naloxone hydrochloride (mart.)
naloxone hydrochloride nasal
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antidote to opioid poisoningA role borne by a molecule that acts to counteract or neutralise the deleterious effects of opioids.
mu-opioid receptor antagonistAny compound that exhibits antagonist activity at the mu-opioid receptor
central nervous system depressantA loosely defined group of drugs that tend to reduce the activity of the central nervous system.
[role 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]

Drug Classes (1)

ClassDescription
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
[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 (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency70.79460.100020.879379.4328AID588453
thioredoxin glutathione reductaseSchistosoma mansoniPotency44.66840.100022.9075100.0000AID485364
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
[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)
kappa-type opioid receptor isoform 1Homo sapiens (human)IC50 (µMol)0.39900.00322.673715.6000AID1778; AID2136
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00490.00010.813310.0000AID1134661; AID1134662
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00490.00020.75218.0140AID1134661; AID1134662
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00490.00001.201110.0000AID1134661; AID1134662
[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)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)31.50000.00132.612925.7000AID1966
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)31.50000.00133.394625.7000AID1966
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)31.50000.00133.394625.7000AID1966
Beta-galactosidaseEscherichia coliEC50 (µMol)31.500025.700025.700025.7000AID1966
[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
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (63)

Assay IDTitleYearJournalArticle
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1135278Narcotic antagonist activity in sc dosed rat assessed as reversal of morphine-induced analgesia by tail-flick test1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
5-allyl-9-oxobenzomorphans. 3. Potent narcotic antagonists and analgesics-antagonists in the series of substituted 2',9beta-dihydroxy-6,7-benzomorphans.
AID521221Induction of neurosphere phenotype changes in mouse neural precursor cells at 3 uM2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID108554The ability to reverse an ED50 dose of morphine when tested in mice by the tail-flick procedure at the dose of 3 mg/kg (s.c.) value expressed as narcotic-antagonistic activity1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins.
AID128200Compound was tested for its analgesic activity in mouse hotplate assay; Inactive1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Preparation and analgesic activity of (-)-11 alpha-substituted 1,2,3,4,5,6-hexahydro-6 alpha,7-(methyleneoxy)-2,6-methano-3-benzazocines.
AID1854010Invivo antagonist activity at MOR in fentanyl induced anti-nociception in C57BL/6J mouse model assessed as latency on hotplate at 10 mg/kg, sc preincubated for 24 hrs followed by fentanyl stimulation and measured after 15 mins by hot plate assay2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Design, synthesis, and biological evaluation of C
AID1132902Analgesic activity in sc dosed mouse at maximum tolerated dose by hot plate method1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1132012Inhibition of morphine sulfate-induced analgesic activity in Swiss albino mouse at 0.4 mg/kg, sc measured 40 mins post morphine sulfate challenge by mouse tail-flick test1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
3-Benzazocine amidinium nitronates. An unusual type of opiate antagonist.
AID131035Compound was tested in mouse tail-flick antinociceptive assay; Inactive1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Preparation and analgesic activity of (-)-11 alpha-substituted 1,2,3,4,5,6-hexahydro-6 alpha,7-(methyleneoxy)-2,6-methano-3-benzazocines.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID112973Compound was tested for morphine antagonist activity by measuring blockade of morphine-induced elevation of tail flick latency in CF-1 female mice1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
4-aryl-4-aminocyclohexanones and their derivatives, a novel class of analgesics. 3. m-Hydroxyphenyl derivates.
AID1136977Narcotic antagonist activity in iv dosed rabbit assessed as inhibition of morphine-induced respiratory depression1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Azabicycloalkanes as analgetics. 3. Structure-activity relationships of 1-phenyl-6-azabicyclo[3.2.1]octanes and absolute stereochemistry of (+)-1-(3-hydroxyphenyl)-6-methyl-6-azabicyclo[3.2.1]octane and its 7-endo-methyl derivative.
AID1132894Inhibition of morphine-induced analgesia in mouse by tail clip method1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1136988Narcotic antagonist activity in morphine-dependent rhesus monkey assessed as mild to severe abstinence1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Azabicycloalkanes as analgetics. 3. Structure-activity relationships of 1-phenyl-6-azabicyclo[3.2.1]octanes and absolute stereochemistry of (+)-1-(3-hydroxyphenyl)-6-methyl-6-azabicyclo[3.2.1]octane and its 7-endo-methyl derivative.
AID1132903Analgesic activity in sc dosed mouse assessed as inhibition of phenylquinone-induced writhing at maximum tolerated dose1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID123622The Narcotic-antagonistic activity the ability to reverse an ED50 dose of morphine when tested in mice by the tail-flick procedure1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins.
AID108553The ability to reverse an ED50 dose of morphine when tested in mice by the tail-flick procedure at the dose of 30 mg/kg (s.c.) value expressed as narcotic-antagonistic activity1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins.
AID1135280Analgesic activity in sc dosed rat assessed as reduction in phenylquinone-induced writhing administered 15 mins prior to phenylquinone-challenge measured up to 10 mins1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
5-allyl-9-oxobenzomorphans. 3. Potent narcotic antagonists and analgesics-antagonists in the series of substituted 2',9beta-dihydroxy-6,7-benzomorphans.
AID594450Agonist activity at kappa opioid receptor in rat C6 cells assessed as induction of ERK1/2 phosphorylation at 40 uM after 10 min by Western blot analysis2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor.
AID1132014Inhibition of morphine sulfate-induced analgesic activity in sc dosed Swiss albino mouse measured 8 hrs post morphine sulfate challenge by mouse tail-flick test1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
3-Benzazocine amidinium nitronates. An unusual type of opiate antagonist.
AID1132015Inhibition of morphine sulfate-induced analgesic activity in sc dosed Swiss albino mouse measured 24 hrs post morphine sulfate challenge by mouse tail-flick test1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
3-Benzazocine amidinium nitronates. An unusual type of opiate antagonist.
AID1135279Narcotic antagonist activity in sc dosed rat assessed as reversal of oxymorphone-induced loss of righting reflex1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
5-allyl-9-oxobenzomorphans. 3. Potent narcotic antagonists and analgesics-antagonists in the series of substituted 2',9beta-dihydroxy-6,7-benzomorphans.
AID131038Compound was tested in phenylquinone antinociceptive assay; Inactive1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Preparation and analgesic activity of (-)-11 alpha-substituted 1,2,3,4,5,6-hexahydro-6 alpha,7-(methyleneoxy)-2,6-methano-3-benzazocines.
AID1135289Narcotic antagonist activity in sc dosed mouse assessed as inhibition of oxymorphone-induced straub tail response administered 10 mins post oxymorphone-challenge1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
5-allyl-9-oxobenzomorphans. 3. Potent narcotic antagonists and analgesics-antagonists in the series of substituted 2',9beta-dihydroxy-6,7-benzomorphans.
AID1132901Analgesic activity in sc dosed mouse at maximum tolerated dose by tail clip method1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID112275Analgesic activity test by employing tail-pinch procedure in CF-1 female mice1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
4-aryl-4-aminocyclohexanones and their derivatives, a novel class of analgesics. 3. m-Hydroxyphenyl derivates.
AID1134663Displacement of [3H] naloxone from opioid receptor (unknown origin) in presence of 100 mM NaCl relative to absence of NaCl1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Stereochemical studies on medicinal agents. 23. Synthesis and biological evaluation of 6-amino derivatives of naloxone and naltrexone.
AID594449Displacement of [3H]DAMGO from mu opioid receptor in BALB/c mouse brain membrane at 5 uM by liquid scintillation counting relative to control2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor.
AID1132900Suppression of abstinence in withdrawn, morphine-dependent rhesus monkey1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1132897Agonist activity at opioid receptor in myenteric plexus of guinea pig ileum relative to morphine1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1132898Antagonist activity at opioid receptor in myenteric plexus of guinea pig ileum relative to nalorphine1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1134661Displacement of [3H] naloxone from opioid receptor (unknown origin)1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Stereochemical studies on medicinal agents. 23. Synthesis and biological evaluation of 6-amino derivatives of naloxone and naltrexone.
AID1132896Toxicity in sc dosed mouse1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID125896Compound was tested in mouse tail-flick analgesic antagonist assay vs morphine at 30 mg/kg1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Preparation and analgesic activity of (-)-11 alpha-substituted 1,2,3,4,5,6-hexahydro-6 alpha,7-(methyleneoxy)-2,6-methano-3-benzazocines.
AID128014Compound was evaluated in vivo for the antagonist activity by the tail flick assay using morphine as the agonist in mice.1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Opioid agonists and antagonists. 6,6-Hydrazi and 6-oximino derivatives of 14-hydroxydihydromorphinones.
AID112273Analgesic activity test by employing HCl writhing procedure in CF-1 female mice1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
4-aryl-4-aminocyclohexanones and their derivatives, a novel class of analgesics. 3. m-Hydroxyphenyl derivates.
AID1135281Analgesic activity in sc dosed mouse assessed as reduction in phenylquinone-induced writhing administered 15 mins prior to phenylquinone-challenge measured up to 10 mins1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
5-allyl-9-oxobenzomorphans. 3. Potent narcotic antagonists and analgesics-antagonists in the series of substituted 2',9beta-dihydroxy-6,7-benzomorphans.
AID1132013Inhibition of morphine sulfate-induced analgesic activity in Swiss albino mouse at 0.04 mg/kg, sc measured 40 mins post morphine sulfate challenge by mouse tail-flick test1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
3-Benzazocine amidinium nitronates. An unusual type of opiate antagonist.
AID108551The ability to reverse an ED50 dose of morphine when tested in mice by the tail-flick procedure at the dose of 10 mg/kg (s.c.) value expressed as narcotic-antagonistic activity1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins.
AID112274Analgesic activity test by employing tail-flick procedure in CF-1 female mice1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
4-aryl-4-aminocyclohexanones and their derivatives, a novel class of analgesics. 3. m-Hydroxyphenyl derivates.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID108552The ability to reverse an ED50 dose of morphine when tested in mice by the tail-flick procedure at the dose of 1 mg/kg (s.c.) value expressed as narcotic-antagonistic activity1982Journal of medicinal chemistry, Mar, Volume: 25, Issue:3
Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins.
AID1132895Toxicity in mouse assessed as Straub tail activity1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1854008Invivo antagonist activity at MOR in fentanyl induced anti-nociception in C57BL/6J mouse model assessed as latency on hotplate at 10 mg/kg, sc preincubated for 1 hrs followed by fentanyl stimulation and measured after 15 mins by hot plate assay2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Design, synthesis, and biological evaluation of C
AID1854009Invivo antagonist activity at MOR in fentanyl induced anti-nociception in C57BL/6J mouse model assessed as latency on hotplate at 10 mg/kg, sc preincubated for 8 hrs followed by fentanyl stimulation and measured after 15 mins by hot plate assay2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Design, synthesis, and biological evaluation of C
AID1134662Displacement of [3H] naloxone from opioid receptor (unknown origin) in presence of 100 mM NaCl1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Stereochemical studies on medicinal agents. 23. Synthesis and biological evaluation of 6-amino derivatives of naloxone and naltrexone.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID112975Sedation test by employing inclined screen test in CF-1 female mice1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
4-aryl-4-aminocyclohexanones and their derivatives, a novel class of analgesics. 3. m-Hydroxyphenyl derivates.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (42.86)18.7374
1990's0 (0.00)18.2507
2000's2 (9.52)29.6817
2010's8 (38.10)24.3611
2020's2 (9.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.98

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

MetricThis Compound (vs All)
Research Demand Index56.98 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index89.32 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]