Page last updated: 2024-11-12

mitragynine, (3beta,16e,20beta)-isomer

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID15560576
CHEMBL ID4546925
SCHEMBL ID15979409
MeSH IDM0307748

Synonyms (16)

Synonym
speciociliatine
14382-79-7
speciociliatin
SCHEMBL15979409
methyl (3beta,16e,20beta)-9-methoxy-16-(methoxymethylidene)corynan-17-oate
DTXSID50574160
methyl (e)-2-[(2s,3s,12br)-3-ethyl-8-methoxy-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-2-yl]-3-methoxyprop-2-enoate
speciociliatine(sh)
indolo(2,3-a)quinolizine-2-acetic acid, 3-ethyl-1,2,3,4,6,7,12,12b-octahydro-8-methoxy-.alpha.-(methoxymethylene)-, methyl ester, (.alpha.e,2s,3s,12br)-
unii-m3nn8z8zjw
M3NN8Z8ZJW ,
indolo(2,3-a)quinolizine-2-acetic acid, 3-ethyl-1,2,3,4,6,7,12,12b-octahydro-8-methoxy-alpha-(methoxymethylene)-, methyl ester, (alphae,2s,3s,12br)-
17,18-seco-3beta,20alpha-yohimban-16-carboxylic acid, 16,17-didehydro-9,17-dimethoxy-, methyl ester, (e)-
(3beta,16e,20beta)-16,17-didehydro-9,17-dimethoxycorynan-16-carboxylic acid methyl ester
bdbm50519927
CHEMBL4546925 ,
[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)IC50 (µMol)4.20000.00010.813310.0000AID1872149
Mu-type opioid receptorHomo sapiens (human)Ki0.22300.00000.419710.0000AID1581727; AID1749821; AID1872031
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)10.00000.00020.75218.0140AID1872150
Delta-type opioid receptorHomo sapiens (human)Ki10.00000.00000.59789.9300AID1872032
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)10.00000.00001.201110.0000AID1872151
Kappa-type opioid receptorHomo sapiens (human)Ki0.22250.00000.362410.0000AID1581726; AID1872033
[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)0.03920.00000.32639.4000AID1581734
[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 (76)

Assay IDTitleYearJournalArticle
AID1830049Displacement of [125I](+/-)DOI from human recombinant 5-HT2C receptor expressed in CHO cells at 100 nM measured after 60 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1581714Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581713Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581722Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes at 1000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581726Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581725Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes incubated for 60 mins2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1872150Inhibition of DOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1581738Agonist activity at human recombinant kappa opioid receptor expressed in rat RBL cells assessed as stimulation of intracellular calcium levels incubated at room temperature by fluorimetry2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775314Dose normalized Cmax in Sprague-Dawley rat plasma at 2.03 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581727Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775278Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 2.5 ng/ml measured in autosampler for 24 hrs by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1775315Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 2.03 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581750Metabolic stability in human liver microsomes assessed as elimination rate constant in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1749821Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis
AID1581707Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775282Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 2.5 ng/ml measured at -80 degC for 4 weeks by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1830051Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells at 100 nM measured after 60 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1830052Displacement of [125I](+/-)DOI from human recombinant 5-HT2A receptor expressed in HEK293 cells at 10 uM measured after 60 to 90 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1581718Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581755Metabolic stability in human liver microsomes assessed as hepatic clearance in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1872032Binding affinity to DOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1872031Binding affinity to MOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1581746Antinociceptive activity in Sprague-Dawley rat dosed intravenously using cumulative dosing every 5 mins until rat maxed-out on hot plate by hot plate test relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775318AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 2.24 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1830047Displacement of [3H]BRL43694 from human recombinant 5-HT3 receptor expressed in CHO cells at 100 nM measured after 120 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1775341Stability of the compound in rat plasma assessed as drug recovery2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581754Metabolic stability in human liver microsomes assessed as intrinsic clearance in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581724Displacement of radioligand from ORL1 (unknown origin) at 10000 nM incubated for 120 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581719Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1830050Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells at 10 uM measured after 60 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1581715Displacement of radioligand from ORL1 (unknown origin) at 100 nM incubated for 120 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1872149Inhibition of MOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1830048Displacement of [125I](+/-)DOI from human recombinant 5-HT2C receptor expressed in CHO cells at 10 uM measured after 60 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1775317Cmax in Sprague-Dawley rat plasma at 2.24 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581723Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1830033Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in cells at 100 nM measured after 60 to 90 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1581756Metabolic stability in human liver microsomes assessed as hepatic extraction ratio in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775311Tmax in Sprague-Dawley rat plasma at 2.03 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581751Metabolic stability in human liver microsomes assessed as half life in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581747Antinociceptive activity in Sprague-Dawley rat dosed intravenously using cumulative dosing every 5 mins until rat maxed-out on hot plate co-treated with 0.1 mg/kg naltrexone by hot plate test2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581710Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581711Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775313AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 2.03 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581709Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581716Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1830053Displacement of [125I](+/-)DOI from human recombinant 5-HT2A receptor expressed in HEK293 cells at 100 nM measured after 60 to 90 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1872033Binding affinity to KOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1872151Inhibition of KOP (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources.
AID1581749Toxicity in Sprague-Dawley rat assessed as induction of hypothermia at 0.0032 to 10 mg/kg, iv2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581720Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775275Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 2.5 ng/ml measured on the bench-top for 2 hrs by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581708Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775279Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 160 ng/ml measured in autosampler for 24 hrs by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1775277Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 160 ng/ml measured on the bench-top for 2 hrs by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1830035Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor at 100 nM measured after 120 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1775342Stability of the compound in water-methanol mixture (1:1) assessed as drug recovery2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581734Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775320Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 2.24 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1830032Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor at 10 uM measured after 120 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1830046Displacement of [3H]BRL43694 from human recombinant 5-HT3 receptor expressed in CHO cells at 10 uM measured after 120 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1775312Cmax in Sprague-Dawley rat plasma at 2.03 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581736Antagonist activity at human recombinant kappa opioid receptor expressed in rat RBL cells assessed as inhibition of U50,488 -induced intracellular calcium levels incubated at room temperature by fluorimetry2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581721Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581753Fraction unbound in human liver microsomes at 1 uM by equilibrium dialysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1830034Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in cells at 10 uM measured after 60 to 90 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1775321Ratio of Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 2.24 mg/kg, po administered as OPMS liquid formulation to Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 2.03 mg/kg, po administered as LKT formulation2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581717Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1581752Fraction unbound in human plasma at 1 uM by equilibrium dialysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775280Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 2.5 ng/ml measured under freeze-thaw conditions for 3 cycles by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1775283Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 160 ng/ml measured at -80 degC for 4 weeks by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581712Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes at 100 nM incubated for 60 mins relative to control2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
AID1775316Tmax in Sprague-Dawley rat plasma at 2.24 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1830058Antinociceptive activity against Sprague-Dawley rats assessed as lower lip retraction at 17.8 mg/kg, ip measured for 15 mins in presence of WAY1006352021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID1775319Dose normalized Cmax in Sprague-Dawley rat plasma at 2.24 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1775281Stability of the compound in rat plasma assessed as proportion of compound deviation from nominal concentration at 160 ng/ml measured under freeze-thaw conditions for 3 cycles by UPLC-MS analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
AID1581745Antinociceptive activity in Sprague-Dawley rat dosed intravenously using cumulative dosing every 5 mins until rat maxed-out on hot plate by hot plate test2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's5 (100.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]