speciogynine: structure in first source [MeSH]
Mitragynine : no description available [CHeBI]
ID Source | ID |
---|---|
PubMed CID | 3034396 |
PubMed CID | 15560577 |
CHEMBL ID | 299031 |
CHEMBL ID | 4859858 |
SCHEMBL ID | 875799 |
SCHEMBL ID | 875800 |
SCHEMBL ID | 15979410 |
CHEBI ID | 6956 |
MeSH ID | M0042144 |
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 |
Class | Description |
---|---|
monoterpenoid indole alkaloid | A terpenoid indole alkaloid which is biosynthesised from L-tryptophan and diisoprenoid (usually secolaganin) building blocks. |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Mu-type opioid receptor | Homo sapiens (human) | EC50 | 0.2454 | AID1581734; AID1581748; AID1809484; AID1872142 |
Kappa-type opioid receptor | Homo sapiens (human) | EC50 | 8.5000 | AID1872153 |
Mu-type opioid receptor | Mus musculus (house mouse) | EC50 | 0.2030 | AID1629756 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Mu-type opioid receptor | Homo sapiens (human) | Kb | 0.1792 | AID1581737 |
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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 1091-6490 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 2374-7943 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | Activity of |
AID1872142 | Agonist activity at MOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | Activity of |
AID1610010 | Inhibition of kappa opioid receptor in guinea pig brain membranes | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-6025 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | Activity of |
AID149837 | Relative affinity evaluated for Opioid receptor kappa 1 | 2002 | Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 | 2021 | Journal of natural products, 04-23, Volume: 84, Issue:4 ISSN: 1520-6025 | |
AID1872032 | Binding affinity to DOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | 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: 183ISSN: 1768-3254 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 0022-2623 | 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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | Activity of |
AID1610008 | Inhibition of mu opioid receptor in guinea pig brain membranes | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183ISSN: 1768-3254 | 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 ISSN: 1520-4804 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID1830027 | AUCinfinity in Sprague-Dawley rat at 1.25 mg/kg, iv | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 ISSN: 1520-4804 | Activity of |
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 ISSN: 1520-6025 | 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 ISSN: 1520-4804 | Activity of |
AID1872151 | Inhibition of KOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | Activity of |
AID1872149 | Inhibition of MOP (unknown origin) | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 ISSN: 1520-4804 | Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
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 ISSN: 1520-6025 | 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 ISSN: 1520-6025 | Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats. |
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 ISSN: 1520-4804 | Activity of |
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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-4804 | 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 ISSN: 1520-6025 | Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats. |
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 ISSN: 1520-6025 | Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats. |
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 ISSN: 1520-6025 | Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats. |
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 ISSN: 1520-4804 | Activity of |
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 |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 24 (10.91%) | 6.00% |
Case Studies | 14 (6.36%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 182 (82.73%) | 84.16% |
Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|
2019 Novel Coronavirus Disease | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Absence Seizure | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Ache | 0 | 2004 | 2022 | 7.9 | low | 0 | 0 | 0 | 2 | 4 | 2 | |
Acute Hypercapnic Respiratory Failure | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Acute Liver Injury, Drug-Induced | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Acute Pain | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
Addiction, Opioid | 0 | 2016 | 2023 | 4.5 | low | 0 | 0 | 0 | 0 | 8 | 5 | |
Adverse Drug Event | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Alcohol Abuse | 0 | 2020 | 2021 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 | |
Alcohol Drinking | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Alcoholism | 0 | 2020 | 2021 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 | |
Anxiety | 0 | 2011 | 2014 | 11.5 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Anxiety Disorders | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Anxiety Neuroses | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Aspiration, Respiratory | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Benign Neoplasms, Brain | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Bile Duct Obstruction | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Bile Duct Obstruction, Intrahepatic | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Body Weight | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Brain Hemorrhage, Cerebral | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Brain Neoplasms | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Cancer of Colon | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cardiac Death | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cardiac Toxicity | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cardiotoxicity | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cerebral Hemorrhage | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Chemical and Drug Induced Liver Injury | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Chemical Dependence | 0 | 2005 | 2023 | 8.3 | medium | 0 | 0 | 0 | 3 | 26 | 4 | |
Cholestasis | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cholestasis, Intrahepatic | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cognition Disorders | 0 | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Colonic Neoplasms | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Coma | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Complications, Pregnancy | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Consciousness, Loss of | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Delayed Effects, Prenatal Exposure | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Depression | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Diarrhea | 0 | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Disease Models, Animal | 0 | 2008 | 2021 | 8.4 | low | 0 | 0 | 0 | 1 | 5 | 2 | |
Drug Overdose | 0 | 2011 | 2019 | 8.3 | low | 0 | 0 | 0 | 0 | 6 | 0 | |
Drug Withdrawal Symptoms | 0 | 1997 | 2022 | 6.6 | low | 0 | 0 | 1 | 0 | 12 | 5 | |
Drug-Related Side Effects and Adverse Reactions | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Edema, Pulmonary | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Glial Cell Tumors | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Glioma | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Hemorrhagic Stroke | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Hypoparathyroidism | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Idiopathic Hypoparathyroidism | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Morphine Abuse | 0 | 2021 | 2022 | 2.5 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
Morphine Dependence | 0 | 2021 | 2022 | 2.5 | low | 0 | 0 | 0 | 0 | 0 | 2 | |
Muscle Contraction | 0 | 1997 | 2006 | 21.8 | low | 0 | 0 | 2 | 4 | 0 | 0 | |
Muscle Relaxation | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Nerve Pain | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Neuralgia | 0 | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Neuroblastoma | 0 | 2005 | 2023 | 10.0 | low | 0 | 0 | 0 | 1 | 0 | 1 | |
Neuromuscular Blockade | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Nociceptive Pain | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Opioid-Related Disorders | 0 | 2016 | 2023 | 4.5 | low | 0 | 0 | 0 | 0 | 8 | 5 | |
Pain | 0 | 2004 | 2022 | 7.9 | low | 0 | 0 | 0 | 2 | 4 | 2 | |
Poisoning | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Pregnancy | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Pulmonary Edema | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Respiratory Insufficiency | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Seizures | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Sensitivity and Specificity | 0 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Substance Withdrawal Syndrome | 0 | 1997 | 2022 | 6.6 | low | 0 | 0 | 1 | 0 | 12 | 5 | |
Substance-Related Disorders | 0 | 2005 | 2023 | 8.3 | medium | 0 | 0 | 0 | 3 | 26 | 4 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Ache | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Nociceptive Pain | 0 | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Pain | 0 | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Article | Year |
---|---|
Progress in the development of more effective and safer analgesics for pain management. European journal of medicinal chemistry, , Dec-01, Volume: 183 | 2019 |
Fatality of 33-Year-Old Man Involving Kratom Toxicity. Journal of forensic sciences, , Volume: 64, Issue:6 | 2019 |
Kratom policy: The challenge of balancing therapeutic potential with public safety. The International journal on drug policy, , Volume: 70 | 2019 |
Evaluation of the cardiotoxicity of mitragynine and its analogues using human induced pluripotent stem cell-derived cardiomyocytes. PloS one, , Volume: 9, Issue:12 | 2014 |
A drug toxicity death involving propylhexedrine and mitragynine. Journal of analytical toxicology, , Volume: 35, Issue:1 | 2011 |
Article | Year |
---|---|
Kratom Alkaloids, Natural and Semi-Synthetic, Show Less Physical Dependence and Ameliorate Opioid Withdrawal. Cellular and molecular neurobiology, , Volume: 41, Issue:5 | 2021 |
Pharmacokinetics of mitragynine in man. Drug design, development and therapy, , Volume: 9 | 2015 |
The combination of mitragynine and morphine prevents the development of morphine tolerance in mice. Molecules (Basel, Switzerland), , Jan-04, Volume: 18, Issue:1 | 2013 |
Effects of mitragynine from Mitragyna speciosa Korth leaves on working memory. Journal of ethnopharmacology, , Jun-16, Volume: 129, Issue:3 | 2010 |
Fos-like immunoreactivity in rat dorsal raphe nuclei induced by alkaloid extract of Mitragyna speciosa. Neuroscience letters, , Apr-12, Volume: 416, Issue:2 | 2007 |
Article | Year |
---|---|
Preclinical pharmacokinetic study of speciociliatine, a kratom alkaloid, in rats using an UPLC-MS/MS method. Journal of pharmaceutical and biomedical analysis, , Feb-05, Volume: 194 | 2021 |
Physicochemical Characterization of Mitragyna speciosa Alkaloid Extract and Mitragynine using In Vitro High Throughput Assays. Combinatorial chemistry & high throughput screening, , Volume: 20, Issue:9 | 2017 |
Determination of mitragynine in plasma with solid-phase extraction and rapid HPLC-UV analysis, and its application to a pharmacokinetic study in rat. Analytical and bioanalytical chemistry, , Volume: 397, Issue:5 | 2010 |
Article | Year |
---|---|
Chemical composition and biological effects of kratom (Mitragyna speciosa): In vitro studies with implications for efficacy and drug interactions. Scientific reports, , 11-05, Volume: 10, Issue:1 | 2020 |
Fatal combination of mitragynine and quetiapine - a case report with discussion of a potential herb-drug interaction. Forensic science, medicine, and pathology, , Volume: 15, Issue:1 | 2019 |