Page last updated: 2024-12-06
fluperlapine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
fluperlapine: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 49381 |
| CHEMBL ID | 63756 |
| CHEBI ID | 5122 |
| SCHEMBL ID | 142558 |
| MeSH ID | M0123158 |
Synonyms (52)
| Synonym |
|---|
| 3-fluoro-6-(4-methyl-piperazin-1-yl)-11h-dibenzo[b,e]azepine |
| 3-fluoro-6-(4-methyl-piperazin-1-yl)-11h-dibenzo[b,e]azepine(fluperlapine) |
| bdbm50040241 |
| HMS3394M07 |
| BRD-K15715913-001-01-5 |
| gtpl279 |
| nb-106689 |
| BIOMOL-NT_000093 |
| BPBIO1_001099 |
| PDSP1_000472 |
| MLS001424156 |
| fluperlapine |
| 67121-76-0 |
| C10967 , |
| MLS000758217 |
| smr000449303 |
| NCGC00160388-01 |
| PDSP2_000470 |
| NCGC00160388-02 |
| fluperlapine [inn] |
| 3-fluoro-6-(4-methyl-1-piperazinyl)morphanthridine |
| fluperlapina [inn-spanish] |
| fluperlapinum [inn-latin] |
| HMS2090H12 |
| HMS2052M07 |
| CHEMBL63756 , |
| chebi:5122 , |
| L000256 |
| 3-fluoro-6-(4-methylpiperazin-1-yl)-11h-benzo[c][1]benzazepine |
| FT-0651061 |
| NCGC00160388-03 |
| ewg253m961 , |
| fluperlapinum |
| fluperlapina |
| unii-ewg253m961 |
| dtxsid2046123 , |
| cas-67121-76-0 |
| tox21_111780 |
| dtxcid0026123 |
| CCG-101093 |
| SCHEMBL142558 |
| NC00343 |
| tox21_111780_1 |
| NCGC00160388-04 |
| fluperlapine [mart.] |
| AB00639914-06 |
| OBWGMKKHCLHVIE-UHFFFAOYSA-N |
| SR-01000759288-4 |
| sr-01000759288 |
| 3-fluoro-6-(4-methyl-piperazinyl)-11h-dibenz-(b,e)-azepine |
| (e)-3-fluoro-6-(4-methylpiperazin-1-yl)-11h-dibenzo[b,e]azepine |
| Q855654 |
Research Excerpts
Effects
Fluperlapine has been reported to possess antischizophrenic and antidepressant properties. Low incidence of extrapyramidal side-effects.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Fluperlapine has been reported to possess antischizophrenic and antidepressant properties, with low incidence of extrapyramidal side-effects. " | ( Effects of fluperlapine on dopaminergic systems in rat brain. Burki, HR, 1986) | 2.1 |
| "3. Fluperlapine which has the higher first pass in man and animals was found to be metabolized in vitro more quickly than pindolol." | ( Identification of metabolic pathways of pindolol and fluperlapine in adult human hepatocyte cultures. Bégué, JM; Guillouzo, A; Koch, P; Maurer, G, 1988) | 1.04 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "A large interindividual variability for clozapine bioavailability and plasma steady-state concentrations and clearance exists." | ( The antipsychotic clozapine is metabolized by the polymorphic human microsomal and recombinant cytochrome P450 2D6. Fischer, V; Maurer, G; Tynes, RE; Vogels, B, 1992) | 0.28 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " The possibilities of LC-MS in the pharmaceutical industry for the analysis of drug substances and dosage forms, metabolism studies and the elucidation of the structures of materials of biological origin are discussed." | ( Experience with routine applications of liquid chromatography-mass spectrometry in the pharmaceutical industry. Erni, F; Groeppelin, A; Linder, M; Schellenberg, KH, 1987) | 0.27 |
| " A mean daily dosage of 300-400 mg appeared to be an effective antipsychotic treatment in most cases." | ( Antipsychotic efficacy of fluperlapine. An open multicenter trial. Angst, J; Bartels, M; Heinrich, K; Hippius, H; Koukkou, M; Krebs, E; Küfferle, B; Müller-Oerlinghausen, B; Pöldinger, W; Woggon, B, 1984) | 0.57 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| benzazepine | A group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring. |
| [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 (26)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| TDP1 protein | Homo sapiens (human) | Potency | 26.8890 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 5.9557 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 14.5668 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247 |
| progesterone receptor | Homo sapiens (human) | Potency | 18.8336 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 26.3296 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 15.8465 | 0.0015 | 30.6073 | 15,848.9004 | AID1259401 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 22.3872 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 29.8493 | 0.0002 | 29.3054 | 16,493.5996 | AID743079 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 5.4950 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 19.1220 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 31.6228 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 15.3877 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 11.2202 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
| Interferon beta | Homo sapiens (human) | Potency | 29.6733 | 0.0033 | 9.1582 | 39.8107 | AID1347407 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 8.4127 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Ki | 0.0251 | 0.0001 | 0.5797 | 10.0000 | AID142687 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | Ki | 0.0251 | 0.0001 | 1.4833 | 9.1400 | AID142687 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | Ki | 0.0251 | 0.0001 | 0.6868 | 8.2600 | AID142687 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | Ki | 0.0038 | 0.0002 | 0.6677 | 10.0000 | AID5042; AID5123 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | Ki | 0.0251 | 0.0001 | 0.6661 | 8.2600 | AID142687 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | Ki | 0.0251 | 0.0001 | 0.5890 | 8.2600 | AID142687 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 0.0038 | 0.0001 | 0.6017 | 10.0000 | AID5042; AID5123 |
| D | Rattus norvegicus (Norway rat) | Ki | 0.1412 | 0.0001 | 0.6100 | 10.0000 | AID63371 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | Ki | 0.0038 | 0.0002 | 0.5909 | 10.0000 | AID5042; AID5123 |
| Gastrin/cholecystokinin type B receptor | Mus musculus (house mouse) | Ki | 0.0038 | 0.0003 | 0.0166 | 0.0940 | AID5123 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.1318 | 0.0000 | 0.4375 | 10.0000 | AID61079 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (153)
Molecular Functions (38)
Ceullar Components (21)
Bioassays (79)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347154 | Primary screen GU AMC 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. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID142687 | Binding affinity against muscarinic (M) receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID61079 | Binding affinity against dopamine D2 receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID61521 | In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID231653 | Binding ratio of -log Ki between 5-HT2 and D2 receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID231526 | Ratio of binding affinity towards D2 to D1 receptor was measured | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID231522 | Ratio of binding affinity towards 5-HT2 to D2 receptor was measured | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID231528 | Ratio of binding affinity towards D2 to muscarinic receptor (M) was measured | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID231655 | Binding ratio of -log Ki between D2 and M receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID231654 | Binding ratio of -log Ki between D2 and D1 receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID63371 | Binding affinity against dopamine receptor D1 | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID5123 | In vitro binding affinity against rat 5-hydroxytryptamine 2 receptor. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID5042 | Binding affinity against serotonin 5-hydroxytryptamine 2 receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID516893 | Agonist activity at human TRPA1 expressed in T-REx-HEK293 cells assessed as increase of intracellular calcium level by FDSS assay | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel. |
| AID140974 | In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID64154 | In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1996 | Journal of neurochemistry, Jan, Volume: 66, Issue:1 | Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 2005 | Psychopharmacology, May, Volume: 179, Issue:2 | Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3 | Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3 | Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 2005 | Psychopharmacology, May, Volume: 179, Issue:2 | Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (42)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 18 (42.86) | 18.7374 |
| 1990's | 9 (21.43) | 18.2507 |
| 2000's | 2 (4.76) | 29.6817 |
| 2010's | 7 (16.67) | 24.3611 |
| 2020's | 6 (14.29) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 21.42
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.42) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (13.04%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 40 (86.96%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||