Page last updated: 2024-12-06
halopemide
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
halopemide: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 65490 |
| CHEMBL ID | 245621 |
| SCHEMBL ID | 121267 |
| MeSH ID | M0068079 |
Synonyms (52)
| Synonym |
|---|
| n-[2-[4-(5-chloro-2-oxo-1-benzimidazolinyl)piperidino]ethyl]-p-fluorobenzamide |
| benzamide,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl]ethyl]-4-fluoro- |
| halopemide |
| mls003171133 , |
| 59831-65-1 |
| r 34,301 |
| nsc354856 |
| nsc-354856 |
| D02665 |
| halopemide (usan/inn) |
| r-34301 |
| CHEMBL245621 , |
| n-[2-[4-(5-chloro-2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]ethyl]-4-fluorobenzamide |
| cid_65490 |
| bdbm50206160 |
| halopemide, 8 |
| n-(2-(4-(5-chloro-2-oxo-2,3-dihydro-1h-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-4-fluorobenzamide , |
| n-(2-(4-(5-chloro-2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-4-fluorobenzamide |
| smr001875041 |
| n-(2-(4-(5-chlor-2,3-dihydro-2-oxo-1-benzimidazolyl)piperidino)ethyl)-4-fluorbenzamid |
| r 34301 |
| nsc 354856 |
| halopemidum |
| halopemida [inn-spanish] |
| benzamide, n-(2-(4-(5-chloro-2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl)ethyl)-4-fluoro- |
| 65q28tv0zy , |
| unii-65q28tv0zy |
| halopemida |
| halopemide [usan:inn] |
| halopemidum [inn-latin] |
| n-(2-(4-(5-chloro-2-oxo-1-benzimidazolinyl)piperidino)ethyl)-p-fluorobenzamide |
| VU0155067-2 |
| halopemide [inn] |
| halopemide [usan] |
| SCHEMBL121267 |
| MLS006012046 |
| smr002529688 |
| n-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl]ethyl]-4-fluorobenzamide |
| NBHPRWLFLUBAIE-UHFFFAOYSA-N |
| HMS3648G20 |
| DTXSID20208561 |
| halopemide, >=98% (hplc) |
| MJV , |
| n-{2-[4-(5-chloro-2-oxo-2,3-dihydro-1h-benzimidazol-1-yl)piperidin-1-yl]ethyl}-4-fluorobenzamide |
| HY-119093 |
| CS-0067969 |
| sr-01000946369 |
| SR-01000946369-1 |
| Q27263902 |
| n-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1h-benzimidazol-1-yl)-1-piperidinyl]-ethyl]-4-fluoro-benzamide |
| MS-27272 |
| AKOS040741828 |
Research Excerpts
Overview
Halopemide is a new psychotropic agent. structurally related to the neuroleptics of the butyrophenone type, but with a different phamacological and clinical profile.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Halopemide is a new psychotropic agent, structurally related to the neuroleptics of the butyrophenone type, but with a different phamacological and clinical profile. " | ( Regional localization of halopemide, a new psychotropic agent, in the rat brain. Janssen, PA; Loonen, AJ; Soudijn, W; van Wijngaarden, I, 1978) | 2 |
| "Halopemide is a new psychotropic agent, a structural analogue of the neuroleptics of the butyrophenone type but with different pharmacological and clinical properties. " | ( Halopemide, a new psychotropic agent. Cerebral distribution and receptor interactions. Loonen, AJ; Soudijn, W, 1985) | 3.15 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Repeated early morning trough measures of plasma clozapine and prolactin levels on each subject were studied during the course of a double-blind dose-response clozapine study." | ( Possible individual and gender differences in the small increases in plasma prolactin levels seen during clozapine treatment. de Leon, J; Diaz, FJ; Josiassen, RC; Simpson, GM, 2004) | 0.32 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (8)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| phospholipase D1 isoform b | Homo sapiens (human) | IC50 (µMol) | 0.0080 | 0.0080 | 0.0080 | 0.0080 | AID602151 |
| phospholipase D2 isoform PLD2B | Homo sapiens (human) | IC50 (µMol) | 0.2800 | 0.2800 | 0.2800 | 0.2800 | AID602147 |
| phospholipase D1 isoform a [Homo sapiens] | Homo sapiens (human) | IC50 (µMol) | 0.0080 | 0.0080 | 0.0080 | 0.0080 | AID602151 |
| phospholipase D2 isoform PLD2A | Homo sapiens (human) | IC50 (µMol) | 0.2800 | 0.2800 | 0.2800 | 0.2800 | AID602147 |
| Phospholipase D2 | Homo sapiens (human) | IC50 (µMol) | 1.5367 | 0.0061 | 1.1598 | 10.0000 | AID1532921; AID306650; AID418767; AID498478; AID498482; AID729472 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 0.0070 | 0.0000 | 0.7472 | 8.0000 | AID729471 |
| Phospholipase D1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0110 | 0.0110 | 0.3438 | 1.0000 | AID498481 |
| Phospholipase D1 | Homo sapiens (human) | IC50 (µMol) | 0.1305 | 0.0010 | 1.0656 | 8.5000 | AID1532920; AID1799395; AID1799396; AID1799399; AID418766; AID498477; AID498484; AID729469 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Phospholipase D1 | Homo sapiens (human) | EC50 (µMol) | 0.1605 | 0.0010 | 1.2309 | 8.5000 | AID1799397; AID1799398 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (110)
Molecular Functions (12)
Ceullar Components (35)
Bioassays (38)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1799398 | 293-PLD2 Cell-Based Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\ | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1799397 | Calu-1 Cell-Based Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\ | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1799395 | PLD1 In Vitro Enzymatic Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\ | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1799396 | d.311 Enzymatic Inhibition Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\ | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1799399 | PLD2 In Vitro Enzymatic Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\ | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID498481 | Inhibition of N-terminally truncated rat PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID729472 | Inhibition of PLD2 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| 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] | |||
| 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] | |||
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID418766 | Inhibition of human PLD1 in Calu1 cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID729469 | Inhibition of PLD1 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| 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 | |||
| AID498477 | Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1532920 | Inhibition of PLD1 (unknown origin) | |||
| AID1532921 | Inhibition of PLD2 (unknown origin) | |||
| AID498484 | Inhibition of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID498478 | Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' 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] | |||
| 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] | |||
| 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] | |||
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID306650 | Inhibition of PLD2 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Optimization of halopemide for phospholipase D2 inhibition. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID498482 | Inhibition of human PLD2 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID418767 | Inhibition of GFP-labelled human PLD2 HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. |
| AID729471 | Inhibition of dopamine receptor D2 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID418768 | Selectivity for human PLD1 over human PLD2 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (19)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 12 (63.16) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (26.32) | 29.6817 |
| 2010's | 2 (10.53) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 18.54
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 (18.54) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (10.00%) | 5.53% |
| Reviews | 1 (5.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 17 (85.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||