Page last updated: 2024-12-10
mitragynine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
speciogynine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 3034396 |
| CHEMBL ID | 299031 |
| CHEBI ID | 6956 |
| SCHEMBL ID | 875799 |
| SCHEMBL ID | 875800 |
| MeSH ID | M0042144 |
| PubMed CID | 15560577 |
| CHEMBL ID | 4859858 |
| SCHEMBL ID | 15979410 |
| MeSH ID | M0042144 |
Synonyms (45)
| Synonym |
|---|
| 4098-40-2 |
| mitragynine |
| C09226 |
| chebi:6956 , |
| CHEMBL299031 , |
| sk&f 12711 |
| 9-methoxycorynantheidine |
| ep479k822j , |
| skf 12711 |
| hsdb 7901 |
| (-)-mitragynine |
| unii-ep479k822j |
| 16,17-didehydro-9,17-dimethoxy-17,18-seco-20-alpha-yohimban-16-carboxylic acid methyl ester |
| mitragynin |
| (.alpha.e,2s,3s,12.beta.s)-3-ethyl-1,2,3,4,6,7,12,12b-octahydro-8-methoxy-.alpha.-(methoxymethylene)-indolo(2,3-a)quinolizine-2-acetic acid methyl ester |
| mitragynine [mi] |
| mitragynine [who-dd] |
| 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,12bs)- |
| SCHEMBL875799 |
| SCHEMBL875800 |
| methyl (2e)-2-[(2s,4s,5s)-5-ethyl-12-methoxy-7,17-diazatetracyclo[8.7.0.0^{2,7}.0^{11,16}]heptadeca-1(10),11,13,15-tetraen-4-yl]-3-methoxyprop-2-enoate |
| bdbm50474152 |
| Q414299 |
| methyl(e)-2-[(2s,3s,12bs)-3-ethyl-8-methoxy-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-2-yl]-3-methoxyprop-2-enoate |
| mitragynine picrate |
| mitragynine - 95% |
| BM164595 |
| DTXSID701032140 |
| mitragynine 100 microg/ml in methanol |
| mitragynine, 1mg/ml in methanol |
| mitragynine, 0.1mg/ml in methanol |
| 4697-67-0 |
| speciogynine |
| SCHEMBL15979410 |
| 17,18-secoyohimban-16-carboxylic acid, 16,17-didehydro-9,17-dimethoxy-, methyl ester, (e)- |
| 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,3r,12bs)- |
| unii-bb185of16a |
| 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,3r,12bs)- |
| (+)-speciogynine |
| BB185OF16A , |
| (16e)-16,17-didehydro-9,17-dimethoxycorynan-16-carboxylic acid methyl ester |
| DTXSID901318037 |
| methyl (e)-2-[(2s,3r,12bs)-3-ethyl-8-methoxy-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-2-yl]-3-methoxyprop-2-enoate |
| CHEMBL4859858 , |
| bdbm50566316 |
Research Excerpts
Overview
Mitragynine (MG) is a major alkaloidal component in the Thai traditional medicinal herb, Mitragyna speciosa. It has been proven to exhibit analgesic activity mediated by opioid receptors.
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " However, there have also been increasing numbers of reports of adverse effects resulting from use of kratom products." | ( Kratom policy: The challenge of balancing therapeutic potential with public safety. Avery, BA; Boyer, EW; Grundmann, O; Henningfield, JE; Kruegel, AC; McCurdy, CR; McMahon, LR; Prozialeck, WC; Singh, D; Swogger, MT; Veltri, CA, 2019) | 0.51 |
Pharmacokinetics
The method was successfully applied in pharmacokinetic and stability studies of mitragynine.
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The obtained ADME and cytotoxicity data demonstrated that both MSAE and mitragynine have poor bioavailability and have the potential to be significantly cytotoxic." | ( Physicochemical Characterization of Mitragyna speciosa Alkaloid Extract and Mitragynine using In Vitro High Throughput Assays. Alshawsh, MA; Chik, Z; Kong, WM; Mohamed, Z, 2017) | 0.92 |
| "2 L/hr/kg), and absolute oral bioavailability (20." | ( Preclinical pharmacokinetic study of speciociliatine, a kratom alkaloid, in rats using an UPLC-MS/MS method. Avery, BA; Berthold, EC; Kamble, SH; King, TI; León, F; McCurdy, CR; McMahon, LR; Popa, R; Raju, KS; Sharma, A, 2021) | 0.62 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " The understanding of mitragynine derivative metabolism in human body is required to develop effective detection techniques in case of drug abuse or establish an appropriate dosage in case of medicinal uses." | ( In silico investigation of mitragynine and 7-hydroxymitragynine metabolism. Limpanuparb, T; Noorat, R; Tantirungrotechai, Y, 2019) | 1.13 |
| " A rational approach is warranted for accurate prediction of dose-response relationship; as this is essential for the development of MG as an alternative medicinal drug for pain management." | ( Pharmacokinetics and pharmacodynamics of mitragynine, the principle alkaloid of Mitragyna speciosa: present knowledge and future directions in perspective of pain. Damodaran, T; Murugaiyah, V; Ramachandram, DS; Ramanathan, S; Zainal, H, 2019) | 0.78 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| monoterpenoid indole alkaloid | A terpenoid indole alkaloid which is biosynthesised from L-tryptophan and diisoprenoid (usually secolaganin) building blocks. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (20)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 5.8800 | 0.0001 | 0.5326 | 10.0000 | AID1830045 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 4.7200 | 0.0001 | 0.8074 | 10.0000 | AID1581731 |
| Cytochrome P450 2D6 | Homo sapiens (human) | Ki | 1.1000 | 0.0001 | 1.1986 | 8.0000 | AID1775306 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 9.2900 | 0.0002 | 0.7257 | 10.0000 | AID1581732 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 2.3200 | 0.0003 | 0.4834 | 10.0000 | AID1581733 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 5.4800 | 0.0000 | 0.3609 | 10.0000 | AID1581730 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 5.0100 | 0.0000 | 0.3855 | 10.0000 | AID1830041 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.9549 | 10.0000 | AID1830039 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 4.0000 | 0.0001 | 0.7298 | 10.0000 | AID1629752 |
| Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 1.0110 | 0.0000 | 0.5393 | 9.4000 | AID1629755 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | IC50 (µMol) | 4.0000 | 0.0013 | 1.5380 | 10.0000 | AID1629759 |
| Kappa-type opioid receptor | Mus musculus (house mouse) | Ki | 0.2310 | 0.0003 | 0.3594 | 2.7500 | AID1629754 |
| 5-hydroxytryptamine receptor 7 | Homo sapiens (human) | Ki | 10.0000 | 0.0003 | 0.3806 | 10.0000 | AID1830042 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Ki | 1.3400 | 0.0000 | 0.2726 | 10.0000 | AID1581728 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Ki | 4.7700 | 0.0000 | 0.4713 | 10.0000 | AID1581729 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.1850 | 0.0000 | 0.4197 | 10.0000 | AID1581727; AID1749821; AID1872031 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0002 | 0.7521 | 8.0140 | AID1872150 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.5978 | 9.9300 | AID1872032 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 1.0000 | 0.0000 | 0.2018 | 6.4240 | AID754487 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.4850 | 0.0000 | 0.3624 | 10.0000 | AID1581726; AID1872033 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 1.2600 | 0.0003 | 0.7693 | 10.0000 | AID1830040 |
| Mu-type opioid receptor | Mus musculus (house mouse) | Ki | 0.2300 | 0.0000 | 0.1228 | 1.3000 | AID1629753 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0072 | 0.0000 | 0.2786 | 9.0000 | AID754489 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 0.0670 | 0.0001 | 0.5326 | 10.0000 | AID1830044; AID1830045 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 1.3200 | 0.0000 | 0.3855 | 10.0000 | AID1830041 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 5.4300 | 0.0001 | 0.9549 | 10.0000 | AID1830039 |
| 5-hydroxytryptamine receptor 7 | Homo sapiens (human) | Ki | 1.6000 | 0.0003 | 0.3806 | 10.0000 | AID1830042 |
| Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 5.7000 | 0.0001 | 0.8133 | 10.0000 | AID1872149 |
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.7280 | 0.0000 | 0.4197 | 10.0000 | AID1749821; AID1872031 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0002 | 0.7521 | 8.0140 | AID1872150 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.5978 | 9.9300 | AID1872032 |
| Kappa-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 1.2011 | 10.0000 | AID1872151 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ki | 3.2000 | 0.0000 | 0.3624 | 10.0000 | AID1872033 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.0655 | 0.0003 | 0.7693 | 10.0000 | AID1830038; AID1830040 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.2454 | 0.0000 | 0.3263 | 9.4000 | AID1581734; AID1581748; AID1809484; AID1872142 |
| Kappa-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 8.5000 | 0.0000 | 0.2244 | 8.9900 | AID1872153 |
| Mu-type opioid receptor | Mus musculus (house mouse) | EC50 (µMol) | 0.2030 | 0.0002 | 0.0393 | 0.2030 | AID1629756 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Homo sapiens (human) | Kb | 0.1792 | 0.0000 | 0.0331 | 0.1792 | AID1581737 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (209)
Molecular Functions (44)
Ceullar Components (43)
Bioassays (297)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347387 | Cytotoxicity qHTS for assessment of Hepg2 cells membrane integrity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347401 | Redox Reaction Profiling qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347394 | Vero-766 cells viability qHTS against the NCATS CANVASS Library: Counterscreen for Zika virus inhibition assay | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347369 | MCF7 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347367 | qHTS for ATAD5 Agonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347376 | 10-beta competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347366 | KB-3-1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347347 | UWB1.289 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347360 | HPAF-II 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347375 | qHTS for Hypoxia signaling pathway (HIF-1) agonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347346 | HPAF-II Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347379 | qHTS for Inflammasome Signaling Inhibitors: IL-1-beta AlphaLISA screen against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347380 | qHTS for Antimalaria activity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347372 | qHTS for Constitutive Androstane Receptor (CAR) Antagonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347368 | G06 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347345 | OV-KATE Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347365 | SDT Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347391 | qHTS for activators of Nrf2/ARE signaling pathway screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347390 | Secretion counterscreen for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347378 | qHTS for H2AX Agonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347393 | qHTS for inhibitors of ER calcium dysfunction: SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347352 | COV-362 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347374 | qHTS for Hypoxia signaling pathway (HIF-1) antagonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347358 | HPAF-II 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347348 | OV-SAHO Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347361 | HEK293 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347349 | Panc-1005 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347357 | HEK293 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347396 | qHTS for inhibitors of Wild type Zika virus screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347392 | qHTS for activators of dead-cell proteases activity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347354 | UWB1.289-WTBRCA1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347355 | HEK-293 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347353 | A2780 Cisplatin Sensitive Ovarian Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347351 | U-118MG Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347356 | HPAF-II 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347359 | HEK293 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347370 | qHTS for ATAD5 Antagonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347402 | qHTS for inhibitors of Rabies Virus screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347373 | qHTS for Constitutive Androstane Receptor (CAR) Agonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347381 | Inflammasome Signaling qHTS Counterscreen: IL-1-beta AlphaLISA counterscreen against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347350 | SW1088 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347377 | DH5-alpha competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347389 | qHTS assay for small molecule disruptors of mitochondrial membrane potential screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347371 | J3T Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347363 | Firefly luciferase counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347388 | qHTS for Activators of p53 Stress Response Pathway screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347362 | Diaphorse counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347400 | Viability qHTS for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347364 | KB-8-5-11 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1775301 | Dose normalized Cmax in Sprague-Dawley rat plasma at 9.6 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1872033 | Binding affinity to KOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID222755 | activity evaluated by its ability to inhibit the electrically induced twitch contraction in guinea pig ileum, which is reversed by naloxone (300 nM)(P < 0.01) | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1581712 | Displacement 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 control | 2020 | Journal 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. |
| AID754489 | Displacement of [3H]DAMGO from mu opoid receptor in Dunkin-Hartley guinea pig brain after 1.5 hrs by liquid scintillation spectrometry | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID1775306 | Inhibition of CYP2D6 in human liver microsomes assessed as inhibition of dextromethorphan O-demethylation using dextromethorphan as substrate preincubated for 5 mins followed by NADPH addition by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1830048 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1872142 | Agonist activity at MOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1581742 | Competitive antagonist activity at human recombinant adrenergic alpha-1B receptor expressed in CHO cells assessed as inhibition of epinephrine-induced intracellular calcium levels incubated at room temperature by fluorimetry | 2020 | Journal 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. |
| AID1775282 | Stability 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 analysis | 2021 | Journal 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. |
| AID1775322 | Drug metabolism in Sprague-Dawley rat plasma assessed as 7-HMG metabolite formation by measuring percentage metabolic ratio of AUC(0-24 hrs) of 7-HMG/AUC(0-24hrs) of parent compound at 5.73 mg/kg, po administered as LKT formulation measured for 24 hrs by | 2021 | Journal 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. |
| AID1830035 | Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor at 100 nM measured after 120 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830045 | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in CHO cells measured after 60 to 90 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1629753 | Displacement of [125I]-IBNtxA from mouse mu opioid receptor-1 expressed in CHO cell membranes incubated for 90 mins | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID148204 | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor mu 1 using [3H]- DAMGO as radioligand | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1581727 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID754479 | Inhibition of gastrointestinal transit of charcoal meal in rat at 55.2 mg/kg, po | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID1830062 | Antinociceptive activity against Sprague-Dawley rats assessed as lower lip retraction at 56 mg/kg, ip measured for 15 mins | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581748 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of cAMP accumulation by HTRF assay | 2020 | Journal 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. |
| AID1581708 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1872155 | Antinociceptive activity in po dosed mouse by tail flick assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1581741 | Competitive antagonist activity at human recombinant adrenergic alpha-1A receptor expressed in CHO cells assessed as inhibition of epinephrine-induced intracellular calcium levels incubated at room temperature by fluorimetry | 2020 | Journal 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. |
| AID1629759 | Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1581715 | Displacement of radioligand from ORL1 (unknown origin) at 100 nM incubated for 120 mins relative to control | 2020 | Journal 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. |
| AID150056 | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor delta 1 using [3H]DPDPE as radioligand | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1830047 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1610010 | Inhibition of kappa opioid receptor in guinea pig brain membranes | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1629757 | Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis relative to DAMGO | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1581750 | Metabolic stability in human liver microsomes assessed as elimination rate constant in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal 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. |
| AID1775337 | Dose normalized Cmax in rat plasma at 20 mg/kg, po administered as LKT formulation | 2021 | Journal 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. |
| AID1581729 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID222419 | Relative inhibitory activity expressed as the percentage of the maximum inhibition by the compound against that of morphine | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1830039 | Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581752 | Fraction unbound in human plasma at 1 uM by equilibrium dialysis | 2020 | Journal 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. |
| AID754485 | Selectivity ratio of Ki for mu opioid receptor in Dunkin-Hartley guinea pig brain over Ki for kappa opioid receptor in Dunkin-Hartley guinea pig brain | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID1610009 | Inhibition of delta opioid receptor in guinea pig brain membranes | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1581725 | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1629755 | Displacement of [125I]-IBNtxA from mouse delta opioid receptor-1 expressed in CHO cell membranes incubated for 90 mins | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1775342 | Stability of the compound in water-methanol mixture (1:1) assessed as drug recovery | 2021 | Journal 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. |
| AID1581734 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay | 2020 | Journal 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. |
| AID1775305 | Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 5.73 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1581737 | Antagonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-induced of cAMP accumulation incubated for 10 mins by HTRF assay | 2020 | Journal 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. |
| AID1610016 | Agonist activity at delta opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1775287 | Cmax in Sprague-Dawley rat plasma at 9.6 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1610017 | Agonist activity at kappa opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1830023 | AUCinfinity in Sprague-Dawley rat at 5 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID149837 | Relative affinity evaluated for Opioid receptor kappa 1 | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1581740 | Partial agonist activity at human recombinant adrenergic alpha-1D receptor expressed in rat RBL cells assessed as stimulation of intracellular calcium levels incubated at room temperature by fluorimetry | 2020 | Journal 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. |
| AID1830051 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581721 | Displacement 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 control | 2020 | Journal 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. |
| AID1809484 | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID1581743 | Competitive antagonist activity at human recombinant adrenergic alpha-1D receptor expressed in rat RBL cells assessed as inhibition of epinephrine-induced intracellular calcium levels incubated at room temperature by fluorimetry | 2020 | Journal 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. |
| AID1581724 | Displacement of radioligand from ORL1 (unknown origin) at 10000 nM incubated for 120 mins relative to control | 2020 | Journal 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. |
| AID1775288 | AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 9.6 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID754488 | Displacement of [3H]DPDPE from delta opoid receptor in Dunkin-Hartley guinea pig brain after 2 hrs by liquid scintillation spectrometry | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID222285 | % maximum inhibition is elicited when the response reaches plateau, calculated regarding electrically induced contraction in guinea pig ileum as 100% | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1581755 | Metabolic stability in human liver microsomes assessed as hepatic clearance in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal 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. |
| AID1809486 | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID1581716 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1872150 | Inhibition of DOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1610015 | Agonist activity at mu opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID754476 | Agonist activity at opioid receptor in guinea pig ileum assessed as inhibition of electrically-induced twitch at 100 pM to 30 uM relative to morphine | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID1581720 | Displacement 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 control | 2020 | Journal 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. |
| AID1581756 | Metabolic stability in human liver microsomes assessed as hepatic extraction ratio in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal 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. |
| AID1581726 | Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1775300 | Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 9.6 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1581717 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1830041 | Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775277 | Stability 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 analysis | 2021 | Journal 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. |
| AID1830053 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581732 | Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1830032 | Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor at 10 uM measured after 120 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581739 | Partial agonist activity at human recombinant adrenergic alpha-1A receptor expressed in CHO cells assessed as stimulation of intracellular calcium levels incubated at room temperature by fluorimetry | 2020 | Journal 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. |
| AID1581754 | Metabolic stability in human liver microsomes assessed as intrinsic clearance in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal 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. |
| AID1775280 | Stability 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 analysis | 2021 | Journal 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. |
| AID1775338 | Dose normalized AUC in rat plasma at 20 mg/kg, po administered as LKT formulation | 2021 | Journal 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. |
| AID1775324 | Drug metabolism in Beagle dog plasma assessed as percentage metabolic ratio at 5 mg/kg, po | 2021 | Journal 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. |
| AID1872152 | Agonist activity at MOP (unknown origin) relative to control | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1749821 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | |||
| AID1872032 | Binding affinity to DOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID754486 | Selectivity ratio of Ki for mu opioid receptor in Dunkin-Hartley guinea pig brain over Ki for delta opioid receptor in Dunkin-Hartley guinea pig brain | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID1610019 | Agonist activity at delta opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1581751 | Metabolic stability in human liver microsomes assessed as half life in presence of NADPH incubated up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal 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. |
| AID1581709 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1581711 | Displacement 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 control | 2020 | Journal 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. |
| AID1830040 | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775304 | Dose normalized Cmax in Sprague-Dawley rat plasma at 5.73 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID222586 | Relative potency expressed as the percentage of the pD2 value against that of morphine | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1830024 | Clearence in Sprague-Dawley rat at 5 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1629767 | Antinociceptive activity in sc dosed CD-1 mouse assessed as increase in reaction time measured 15 mins post dose by radiant heat tail flick assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1809485 | Agonist activity at human MOR expressed in HEK-293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay relative to DAMGO | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID148190 | Relative affinity evaluated for Opioid receptor mu 1 | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1830033 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830046 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775279 | Stability 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 analysis | 2021 | Journal 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. |
| AID1581713 | Displacement 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 control | 2020 | Journal 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. |
| AID1775299 | Ratio of Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 9.6 mg/kg, po administered as OPMS liquid formulation to Dose normalized AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 5.73 mg/kg, po administered as LKT formulation | 2021 | Journal 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. |
| AID1581710 | Displacement 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 control | 2020 | Journal 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. |
| AID1775276 | AUC(0 to 24 hrs) in Sprague-Dawley rat plasma at 5.73 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1581723 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes at 10000 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1581728 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1629756 | Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1610018 | Agonist activity at mu opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1581753 | Fraction unbound in human liver microsomes at 1 uM by equilibrium dialysis | 2020 | Journal 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. |
| AID1872153 | Agonist activity at KOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1775275 | Stability 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 analysis | 2021 | Journal 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. |
| AID1775286 | Tmax in Sprague-Dawley rat plasma at 9.6 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1830042 | Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID149845 | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor kappa 1 using [3H]- U-69,593 as radioligand | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1775303 | Cmax in Sprague-Dawley rat plasma at 5.73 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1775283 | Stability 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 analysis | 2021 | Journal 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. |
| AID1830034 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581718 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes at 10000 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1775281 | Stability 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 analysis | 2021 | Journal 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. |
| AID1581722 | Displacement 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 control | 2020 | Journal 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. |
| AID1581719 | Displacement 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 control | 2020 | Journal 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. |
| AID1775323 | Drug metabolism in Sprague-Dawley rat plasma assessed as 7-HMG metabolite formation by measuring percentage metabolic ratio of AUC(0-24 hrs) of 7-HMG/AUC(0-24hrs) of parent compound at 9.6 mg/kg, po administered as OPMS liquid formulation measured for 24 | 2021 | Journal 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. |
| AID1809487 | Agonist activity at human MOR receptor expressed in HTLA cells co-expressing TEV-fused-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment by Tango assay relative to DAMGO | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects. |
| AID1581731 | Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1775302 | Tmax in Sprague-Dawley rat plasma at 5.73 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1610020 | Agonist activity at kappa opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1775341 | Stability of the compound in rat plasma assessed as drug recovery | 2021 | Journal 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. |
| AID1581733 | Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1581707 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes at 100 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1581749 | Toxicity in Sprague-Dawley rat assessed as induction of hypothermia at 0.0032 to 10 mg/kg, iv | 2020 | Journal 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. |
| AID1872031 | Binding affinity to MOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID754487 | Displacement of [3H]U-69593 from kappa opoid receptor in Dunkin-Hartley guinea pig brain after 1 hr by liquid scintillation spectrometry | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID1581714 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes at 100 nM incubated for 60 mins relative to control | 2020 | Journal 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. |
| AID1830059 | Antinociceptive activity against Sprague-Dawley rats assessed as lower lip retraction at 56 mg/kg, ip measured for 15 mins in presence of WAY100635 | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830052 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830050 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830021 | Elimination rate constant in Sprague-Dawley rat at 5 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1581730 | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes incubated for 60 mins | 2020 | Journal 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. |
| AID1629765 | Activation of mu opioid receptor-1 (unknown origin) expressed in CHO cells assessed as beta-arrestin-2 recruitment at 10 uM after 90 mins by beta-galactosidase complementation assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1581747 | Antinociceptive 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 test | 2020 | Journal 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. |
| AID1629754 | Displacement of [125I]-IBNtxA from mouse kappa opioid receptor-1 expressed in CHO cell membranes incubated for 90 mins | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1830022 | Apparent volume of distributed in Sprague-Dawley rat at 5 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830037 | Antinociceptive activity against ip dosed Sprague-Dawley rats assessed as loser lip retraction measured for 15 mins | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1629752 | Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18 | Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2. |
| AID1581746 | Antinociceptive 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 control | 2020 | Journal 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. |
| AID1581744 | Competitive antagonist activity at human recombinant adrenergic alpha-2C receptor expressed in CHO cells assessed as inhibition of epinephrine-induced intracellular calcium levels incubated at room temperature by fluorimetry | 2020 | Journal 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. |
| AID754481 | Antinociceptive activity in mouse at 92 mg/kg, po by hot plate test | 2013 | Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12 | Orally active opioid compounds from a non-poppy source. |
| AID150051 | Relative affinity evaluated for Opioid receptor delta 1 | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 | Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands. |
| AID1775278 | Stability 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 analysis | 2021 | Journal 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. |
| AID1830049 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1610008 | Inhibition of mu opioid receptor in guinea pig brain membranes | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Progress in the development of more effective and safer analgesics for pain management. |
| AID1872164 | Antinociceptive activity in sc dosed mouse | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1347353 | A2780 Cisplatin Sensitive Ovarian Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347363 | Firefly luciferase counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347352 | COV-362 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347345 | OV-KATE Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347348 | OV-SAHO Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347361 | HEK293 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347364 | KB-8-5-11 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347366 | KB-3-1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347392 | qHTS for activators of dead-cell proteases activity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347370 | qHTS for ATAD5 Antagonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347347 | UWB1.289 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347400 | Viability qHTS for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347355 | HEK-293 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347369 | MCF7 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347378 | qHTS for H2AX Agonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347358 | HPAF-II 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347356 | HPAF-II 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347393 | qHTS for inhibitors of ER calcium dysfunction: SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347360 | HPAF-II 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347388 | qHTS for Activators of p53 Stress Response Pathway screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347394 | Vero-766 cells viability qHTS against the NCATS CANVASS Library: Counterscreen for Zika virus inhibition assay | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347365 | SDT Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347367 | qHTS for ATAD5 Agonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347396 | qHTS for inhibitors of Wild type Zika virus screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347401 | Redox Reaction Profiling qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347377 | DH5-alpha competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347390 | Secretion counterscreen for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347357 | HEK293 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347349 | Panc-1005 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347375 | qHTS for Hypoxia signaling pathway (HIF-1) agonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347372 | qHTS for Constitutive Androstane Receptor (CAR) Antagonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347346 | HPAF-II Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347379 | qHTS for Inflammasome Signaling Inhibitors: IL-1-beta AlphaLISA screen against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347376 | 10-beta competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347391 | qHTS for activators of Nrf2/ARE signaling pathway screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347373 | qHTS for Constitutive Androstane Receptor (CAR) Agonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347350 | SW1088 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347387 | Cytotoxicity qHTS for assessment of Hepg2 cells membrane integrity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347374 | qHTS for Hypoxia signaling pathway (HIF-1) antagonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347354 | UWB1.289-WTBRCA1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347402 | qHTS for inhibitors of Rabies Virus screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347359 | HEK293 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347389 | qHTS assay for small molecule disruptors of mitochondrial membrane potential screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347371 | J3T Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347380 | qHTS for Antimalaria activity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347362 | Diaphorse counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347368 | G06 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347351 | U-118MG Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347381 | Inflammasome Signaling qHTS Counterscreen: IL-1-beta AlphaLISA counterscreen against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1830027 | AUCinfinity in Sprague-Dawley rat at 1.25 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1872031 | Binding affinity to MOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1775334 | Drug uptake in Sprague-Dawley rat plasma at 1.23 mg/kg, po administered as OPMS liquid formulation measured within 1 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1830051 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830039 | Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830037 | Antinociceptive activity against ip dosed Sprague-Dawley rats assessed as loser lip retraction measured for 15 mins | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775278 | Stability 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 analysis | 2021 | Journal 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. |
| AID1775341 | Stability of the compound in rat plasma assessed as drug recovery | 2021 | Journal 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. |
| AID1775280 | Stability 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 analysis | 2021 | Journal 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. |
| AID1830026 | Apparent volume of distributed in Sprague-Dawley rat at 1.25 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830047 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1872151 | Inhibition of KOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1830033 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830061 | Antinociceptive activity against Sprague-Dawley rats assessed as lower lip retraction at 17.8 mg/kg, ip measured for 15 mins | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830044 | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in HEK cells measured after 60 to 90 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830050 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1872149 | Inhibition of MOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1775342 | Stability of the compound in water-methanol mixture (1:1) assessed as drug recovery | 2021 | Journal 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. |
| AID1830045 | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in CHO cells measured after 60 to 90 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830042 | Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1749821 | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | |||
| AID1775326 | Cmax in Sprague-Dawley rat plasma at 0.79 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1775275 | Stability 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 analysis | 2021 | Journal 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. |
| AID1775327 | Tmax in Sprague-Dawley rat plasma at 1.23 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1775283 | Stability 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 analysis | 2021 | Journal 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. |
| AID1830041 | Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830060 | Antinociceptive activity iv dosed Sprague-Dawley rats assessed as hotplate latency for 60 by hot plate test in presence of WAY100635 | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775279 | Stability 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 analysis | 2021 | Journal 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. |
| AID1830056 | Antinociceptive activity iv dosed Sprague-Dawley rats assessed as hotplate latency for 60 by hot plate test | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830038 | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830028 | Clearence in Sprague-Dawley rat at 1.25 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1872033 | Binding affinity to KOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1830040 | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830032 | Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor at 10 uM measured after 120 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775333 | Drug uptake in Sprague-Dawley rat plasma at at 0.79 mg/kg, po administered as LKT formulation measured within 1 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1830049 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830052 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830034 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830053 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830046 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1872032 | Binding affinity to DOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1775328 | Cmax in Sprague-Dawley rat plasma at 1.23 mg/kg, po administered as OPMS liquid formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1830035 | Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor at 100 nM measured after 120 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1830048 | Displacement 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 control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775325 | Tmax in Sprague-Dawley rat plasma at 0.79 mg/kg, po administered as LKT formulation measured for 24 hrs by UPLC-MS/MS analysis | 2021 | Journal 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. |
| AID1775282 | Stability 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 analysis | 2021 | Journal 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. |
| AID1775277 | Stability 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 analysis | 2021 | Journal 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. |
| AID1872150 | Inhibition of DOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1830025 | Elimination rate constant in Sprague-Dawley rat at 1.25 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID1775281 | Stability 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 analysis | 2021 | Journal 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (200)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (1.00) | 18.7374 |
| 1990's | 6 (3.00) | 18.2507 |
| 2000's | 19 (9.50) | 29.6817 |
| 2010's | 105 (52.50) | 24.3611 |
| 2020's | 68 (34.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 68.10
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (68.10) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 24 (11.43%) | 6.00% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 14 (6.67%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 172 (81.90%) | 84.16% |
| Other | 10 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||