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cyclorphan

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Description

cyclorphan: was heading 1965-94 (see under MORPHINANS 1965-90); use MORPHINANS to search CYCLORPHAN 1966-94 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5359966
CHEMBL ID49269
SCHEMBL ID159134
MeSH IDM0224731

Synonyms (22)

Synonym
(-)-3-hydroxy-n-cyclopropylmethylmorphinan
17-(cyclopropylmethyl)morphinan-3-ol
cyclorphan
morphinan, (-)-3-hydroxy-n-cyclopropylmethyl-
einecs 224-007-5
PDSP2_000668
3-hydroxy-n-cyclopropylmethylmorphinan
17-cyclopropylmethyl-(1r,9r,10r)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-trien-4-ol
(-)-3-hydroxy-n-cycloproypylmethylmorphinan mandelate
bdbm50135800
(-)-17-(cyclopropylmethyl)morphinan-3-ol
CHEMBL49269 ,
morphinan-3-ol, 17-(cyclopropylmethyl)-
4163-15-9
u6z73n36v0 ,
unii-u6z73n36v0
cyclorphan [mi]
morphinan, n-(cyclopropylmethyl)-3-hydroxy-
SCHEMBL159134
Q5199001
n-cyclopropylmethyl 3-hydroxymorphinan
DTXSID50878519
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)0.00170.00010.813310.0000AID150824; AID259402; AID290265; AID296062; AID592442; AID670121
Mu-type opioid receptorHomo sapiens (human)Ki0.00010.00000.419710.0000AID148328; AID151001; AID259394; AID290256; AID296053; AID445095; AID592435; AID670110
Delta-type opioid receptorHomo sapiens (human)Ki0.00190.00000.59789.9300AID147944; AID148369; AID149778; AID259395; AID290258; AID296055; AID445097; AID592436; AID670113
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00100.00000.20186.4240AID147944; AID149121
Kappa-type opioid receptorHomo sapiens (human)Ki0.00000.00000.362410.0000AID148149; AID149978; AID259396; AID290257; AID296054; AID445096; AID592432; AID670111
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00010.00000.27869.0000AID147903
[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)
Mu-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00080.00000.32639.4000AID148326; AID148341; AID259402; AID290264; AID296061; AID592439; AID670119
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.00020.00000.22448.9900AID149976; AID149994; AID259400; AID290262; AID296058; AID592433; AID670123
Mu-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.00020.00000.04930.9320AID149994
[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 (98)

Assay IDTitleYearJournalArticle
AID290259Selectivity for kappa opioid receptor over mu opioid receptor expressed in CHO cells2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID670111Displacement of [3H]-U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID149976Agonistic activity against kappa opioid receptor in Chinese hamster ovary membranes2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID1148433Narcotic antagonist activity in sc dosed mouse assessed as reversal of oxymorphone-induced straub tail response administered 10 mins before oxymorphone challenge1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics and narcotic antagonists in the benzomorphan and 8-oxamorphinan series. 5.
AID592432Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID149121Binding affinity against opioid receptor kappa 1 using [3H]-U-69,593 as radioligand in guinea pig brain membranes.2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
AID149778Binding affinity against opioid receptor delta 1 using [3H]naltrindole as radioligand in guinea pig brain membranes.2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
AID149904Binding affinity towards Opioid receptor delta 1 in guinea pig brain membranes using [3H]naltrindole as radioligand2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
AID259402Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID592434Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase in U50488-induced [35S]GTPgammaS binding by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID1148435Narcotic antagonist activity in sc dosed mouse assessed as reversal of oxymorphone-induced narcosis1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics and narcotic antagonists in the benzomorphan and 8-oxamorphinan series. 5.
AID296055Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO membrane2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID296054Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO membrane2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID235330Selectivity ratio of kappa opioid receptor to that of mu opioid receptor in guinea pig brain membranes2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
AID229388Relative affinity for delta and kappa opioid receptors2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID148369Inhibitory activity against Opioid receptor delta 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]naltrindole radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID150824Inhibitory activity was determined in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO)membranes2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID259396Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID259395Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID592437Selectivity ratio of Ki for human mu opioid receptor to Ki for human kappa opioid receptor2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID235329Selectivity ratio of kappa opioid receptor to that of delta opioid receptor in guinea pig brain membranes2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
AID670113Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID592436Displacement of [3H]Naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID296059Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced stimulation of [35S]GTP-gamma-S binding after 60 mins2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID259399Functional activity at human kappa opioid receptor expressed CHO cells by [35S]GTPgammaS binding assay2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID592438Selectivity ratio of Ki for human delta opioid receptor to Ki for human kappa opioid receptor2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID233831Selective inhibitory activity was determined against kappa & mu opioid receptor in chinese Hamster Ovary (CHO) cell membranes2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID296057Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to basal level after 60 mins2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID259394Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID290256Displacement of [3H]DAMGO from human mu opioid receptors expressed in CHO cell membrane2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID670117Selectivity index, ratio of inhibition of human mu opioid receptor to inhibition of human kappa opioid receptor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID259398Selectivity for human kappa opioid receptor over delta opioid receptor2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID148351Percent maximal stimulation in [35S]-GTP-gamma S binding assay mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO)membranes2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID259400Activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID592435Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID670122Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [33S]GTPgammaS binding after 60 mins by scintillation counting relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID235164Selectivity ratio expressed as Ki of delta opioid receptor to that of mu opioid receptor.2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
AID290264Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID445097Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
AID445098Selectivity ratio of Ki for human kappa opioid receptor to Ki for human mu opioid receptor2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
AID290257Displacement of [3H]U-69593 from human kappa opioid receptors expressed in CHO cell membrane2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID670123Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID296058Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID296060Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding relative to basal level after 60 mins2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID592442Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID233830Selective inhibitory activity was determined against kappa & delta opioid receptor in chinese Hamster Ovary (CHO) cell membranes2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID147944Inhibition of [3H]naltrindole binding to opioid receptor delta 1 of Chinese hamster ovary membrane2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID149977Binding ability against kappa opioid receptor by stimulating the [35S]GTP-gamma-S, radioligand in Chinese hamster ovary membranes2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID148327Binding ability against Opioid receptor mu 1 by stimulating the [35S]GTP-gamma-S radioligand in Chinese hamster ovary membranes2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID149994Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID259397Selectivity for human kappa opioid receptor over mu opioid receptor2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID592373Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting relative to control2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID296061Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID290258Displacement of [3H]naltrindole from human delta opioid receptors expressed in CHO cell membrane2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID150827Maximal percent inhibitory activity was determined in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID148158Maximal percent inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes; Not Tested2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID592441Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting relative to control2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID445096Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
AID296053Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO membrane2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID149270Binding affinity towards Opioid receptor kappa 1 by displacing the radioligand [3H]U-69593 from guinea pig brain membrane2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
AID290263Antagonist activity against [35S]GTP-gamma-S binding from human kappa opioid receptors expressed in CHO cell membrane2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID592433Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID290261Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding relative to control2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID445095Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
AID296062Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding after 60 mins2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
AID148326Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID148734Selectivity kappa/delta2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
AID259401Functional activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
AID147851Percent maximal stimulation in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID445099Selectivity ratio of Ki for human delta opioid receptor to Ki for human mu opioid receptor2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
AID139099Analgesic Potency was tested against mice1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
A Free-Wilson/Fujita-Ban analysis and prediction of the analgesic potency of some 3-hydroxy- and 3-methoxy-N-alkylmorphinan-6-one opioids.
AID149272Binding affinity towards Opioid receptor kappa 1 in guinea pig brain membranes using [3H]U-69593 as radioligand2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
AID670118Selectivity index, ratio of inhibition of human delta opioid receptor to inhibition of human kappa opioid receptor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID290265Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as DAMGO-stimulated [35S]GTP-gamma-S binding2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID148341Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID148036Binding affinity towards Opioid receptor mu 1 in guinea pig brain membranes using [3H]DAMGO as radioligand2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
AID670110Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID670119Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID151001Inhibitory activity against Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cells membranes was determined using [3H]-DAMGO radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID235163Selectivity ratio expressed as Ki of delta opioid receptor to that of kappa opioid receptor.2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
AID229399Relative affinity for mu and kappa opioid receptors2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID148034Binding affinity towards Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO from guinea pig brain membrane2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
AID290262Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID290260Selectivity for kappa opioid receptor over delta opioid receptor2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
High-affinity carbamate analogues of morphinan at opioid receptors.
AID148149Inhibitory activity against Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]U-69593 radioligand2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
AID670124Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID148328Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of Chinese hamster ovary membrane2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
AID1148432Analgesic activity in sc dosed mouse assessed as phenylquinone-induced writhing measured for 10 mins1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics and narcotic antagonists in the benzomorphan and 8-oxamorphinan series. 5.
AID147903Binding affinity against opioid receptor mu 1 using [3H]DAMGO as radioligand in guinea pig brain membranes.2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
AID592444Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding by scintillation counting relative to control2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID670121Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced [33S]GTPgammaS binding after 60 mins by scintillation counting2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID149902Binding affinity towards Opioid receptor delta 1 by displacing the radioligand [3H]naltrindole from guinea pig brain membrane2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
AID1148434Analgesic activity in sc dosed rat assessed as phenylquinone-induced writhing measured for 10 mins1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics and narcotic antagonists in the benzomorphan and 8-oxamorphinan series. 5.
AID670120Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
AID592439Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Aminothiazolomorphinans with mixed κ and μ opioid activity.
AID148735Selectivity kappa/mu2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
AID1148436Antagonist activity in rat assessed as morphine-induced analgesia by hot plate tail flick test1978Journal of medicinal chemistry, May, Volume: 21, Issue:5
Analgesics and narcotic antagonists in the benzomorphan and 8-oxamorphinan series. 5.
AID149978Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of Chinese hamster ovary membrane2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (7.14)18.7374
1990's1 (7.14)18.2507
2000's8 (57.14)29.6817
2010's4 (28.57)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: 21.52

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index21.52 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.93 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]