Page last updated: 2024-11-12

9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester

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Description

9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2H-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11431898
CHEMBL ID363324
SCHEMBL ID3540059
MeSH IDM0488179

Synonyms (19)

Synonym
CHEMBL363324 ,
herkinorin
(3s,4ar,4bs,6s,8r,8ar,10ar)-6-benzoyloxy-3-furan-3-yl-4a,8a-dimethyl-1,5-dioxo-dodecahydro-2-oxa-phenanthrene-8-carboxylic acid methyl ester
bdbm50170678
unii-5xn29vgr24
5xn29vgr24 ,
9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho(2,1-c)pyran-7-carboxylic acid methyl ester
862073-77-6
SCHEMBL3540059
(2s,4ar,6ar,7r,9s,10as,10br)-9-(benzoyloxy)-2-(3-furanyl)-dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho[2,1-c]pyran-7-carboxylic acid methyl ester
PYDQMXRFUVDCHC-XAGHGKQISA-N
DTXSID30235444
Q4137203
methyl (2s,4ar,6ar,7r,9s,10as,10br)-9-benzoyloxy-2-(furan-3-yl)-6a,10b-dimethyl-4,10-dioxo-2,4a,5,6,7,8,9,10a-octahydro-1h-benzo[f]isochromene-7-carboxylate
2h-naphtho(2,1-c)pyran-7-carboxylic acid, 9-(benzoyloxy)-2-(3-furanyl)dodecahydro-6a,10b-dimethyl-4,10-dioxo-, methyl ester, (2s,4ar,6ar,7r,9s,10as,10br)-
methyl (2r,4ar,6ar,7s,9r,10as,10br)-2-(furan-3-yl)-6a,10b-dimethyl-4,10-bis(oxidanylidene)-9-(phenylcarbonyloxy)-2,4a,5,6,7,8,9,10a-octahydro-1h-benzo(f)isochromene-7-carboxylate
CS-0081983
HY-121415
AKOS040748524

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" In cumulative dosing studies (0."( The effects of herkinorin, the first mu-selective ligand from a salvinorin A-derived scaffold, in a neuroendocrine biomarker assay in nonhuman primates.
Butelman, ER; Kreek, MJ; Prisinzano, TE; Rus, S; Simpson, DS; Wolf, A, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorHomo sapiens (human)Ki0.01200.00000.419710.0000AID238663; AID329899; AID377275
Delta-type opioid receptorHomo sapiens (human)Ki1.17000.00000.59789.9300AID238721; AID329900; AID377276
Kappa-type opioid receptorHomo sapiens (human)Ki0.09000.00000.362410.0000AID238722; AID329901; AID377277
[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)0.98800.00000.32639.4000AID1165896; AID1714467; AID1714470; AID240131; AID329904
Delta-type opioid receptorHomo sapiens (human)EC50 (µMol)10.00000.00000.43328.3000AID1714469
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.93670.00000.22448.9900AID1714468; AID240142; AID329906
[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 (44)

Assay IDTitleYearJournalArticle
AID377279Selectivity ratio of Ki for delta opioid receptor to kappa opioid receptor2006Journal of natural products, Jun, Volume: 69, Issue:6
Synthesis of salvinorin A analogues as opioid receptor probes.
AID238722Inhibition of [125I]- IOXY binding to human Opioid receptor kappa12005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID377277Displacement of [125]OXY from kappa opioid receptor2006Journal of natural products, Jun, Volume: 69, Issue:6
Synthesis of salvinorin A analogues as opioid receptor probes.
AID329903Selectivity for human recombinant kappa opioid receptor over human recombinant delta opioid receptor2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID1714474Antinociceptive activity in male B6-SJL mouse at 1 to 10 mg/kg, ip measured up to 120 mins by warm water tail-flick assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID244153Relative affinity for human opioid receptor delta1 and kappa12005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID377278Selectivity ratio of Ki for mu opioid receptor to kappa opioid receptor2006Journal of natural products, Jun, Volume: 69, Issue:6
Synthesis of salvinorin A analogues as opioid receptor probes.
AID1714483Neurotoxicity in B6-SJL mouse assessed as induction of motor coordination by rotarod test2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID329909Agonist activity at mu opioid receptor expressed in HEK293 cells overexpressing GRK2 assessed as induction of beta-arrestin-2-GFP plasma membrane translocation at 10 uM after 10 mins2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID329906Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID1609949Agonist activity at full length kappa opioid receptor (unknown origin) relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Progress in the development of more effective and safer analgesics for pain management.
AID329904Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID1714481Reward liability in Sprague-Dawley rat assessed as increase in conditioned place preference at 5 mg/kg, ip administered starting from day 2 to 7 for 60 mins measured on day 8 for 15 mins2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID329912Agonist activity at mu opioid receptor expressed in HEK293 cells overexpressing GRK2 assessed as induction of yellow fluorescent protein internalization at 10 uM after 24 hrs2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID1714473Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay relative to DAMGO2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID1165896Agonist activity at MOR (unknown origin)2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.
AID238663Inhibition of [125I]- IOXY binding to human Opioid receptor mu12005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID1714486Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay relative to control2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID329900Displacement of [125I]IOXY from human recombinant delta opioid receptor expressed in CHO cells2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID244145Relative affinity for human opioid receptor mu1 and kappa12005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID329905Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay relative to DAMGO2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID1714470Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID1714469Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID329901Displacement of [125I]IOXY from human recombinant kappa opioid receptor expressed in CHO cells2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID1714491Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production up to 10 uM measured after 30 mins by HitHunter luminescence based assay relative to control2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID240131Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor mu1 expressed in CHO cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID238721Inhibition of [125I]- IOXY binding to human Opioid receptor delta12005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID1714467Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID240231Stimulation of [35S]-GTP gammaS binding to Opioid receptor delta 1 expressed in CHO cells; ND = Not determined2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID377275Displacement of [125]OXY from mu opioid receptor2006Journal of natural products, Jun, Volume: 69, Issue:6
Synthesis of salvinorin A analogues as opioid receptor probes.
AID1714472Selectivity ratio of EC50 for agonist activity at human kappa opiod receptor expressed in CHO-K1 cells to EC50 for agonist activity at human mu opiod receptor expressed in CHO-K1 cells2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID329899Displacement of [125I]IOXY from human recombinant mu opioid receptor expressed in CHO cells2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID377276Displacement of [125]OXY from delta opioid receptor2006Journal of natural products, Jun, Volume: 69, Issue:6
Synthesis of salvinorin A analogues as opioid receptor probes.
AID240459Stimulatory effect on [35S]-GTP gammaS binding to Opioid receptor mu1 expressed in CHO cells compared to 10 uM DAMGO2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID1714485Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay relative to control2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID1714488Bias factor, ratio of biased agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment to biased agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID329907Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to (-)-U50,4882008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID240142Stimulation of [35S]GTP-gamma-S, binding to Opioid receptor kappa1 expressed in CHO cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID1714471Selectivity ratio of EC50 for agonist activity at human delta opiod receptor expressed in CHO-K1 cells to EC50 for agonist activity at human mu opiod receptor expressed in CHO-K1 cells2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
AID1609948Agonist activity at full length HA-tagged mu opioid receptor (unknown origin) expressed in HEK293 cells after 1 hr relative too control2019European journal of medicinal chemistry, Dec-01, Volume: 183Progress in the development of more effective and safer analgesics for pain management.
AID329902Selectivity for human recombinant kappa opioid receptor over human recombinant mu opioid receptor2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Herkinorin analogues with differential beta-arrestin-2 interactions.
AID240464Stimulatory effect on [35S]GTP gammaS binding to Opioid receptor kappa1 expressed in CHO cells compared to 500 nM U50,4882005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID240469Stimulatory effect on [35S]GTP gammaS binding to Opioid receptor delta 1 expressed in CHO cells compared to 500 nM SNC80; ND = Not determined2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
AID1714468Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (35.00)29.6817
2010's12 (60.00)24.3611
2020's1 (5.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.58

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.58 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (15.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (85.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]