Page last updated: 2024-12-10
panadiplon
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
panadiplon: structure given in first source; RN from Toxlit [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 3033821 |
| CHEMBL ID | 279867 |
| SCHEMBL ID | 123304 |
| MeSH ID | M0189526 |
Synonyms (34)
| Synonym |
|---|
| bdbm50048837 |
| 3-(5-cyclopropyl-[1,2,4]oxadiazol-3-yl)-5-isopropyl-5h-imidazo[1,5-a]quinoxalin-4-one |
| 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-isopropylimidazo(1,5-a)quinoxalin-4(5h)-one |
| imidazo(1,5-a)quinoxalin-4(5h)-one, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(1-methylethyl)- |
| panadiplon [usan:inn] |
| fg 10571 |
| panadiplonum [inn-latin] |
| panadiplone [inn-french] |
| u-78875 |
| panadiplon |
| fg-10571 |
| 124423-84-3 |
| panadiplon (usan/inn) |
| D05346 |
| CHEMBL279867 , |
| 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-propan-2-ylimidazo[1,5-a]quinoxalin-4-one |
| panadiplone |
| unii-v4pw0s7zp7 |
| panadiplonum |
| v4pw0s7zp7 , |
| AKOS015904452 |
| 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(1-methylethyl)-imidazo(1,5-a)quinoxalin-4(5h)-one |
| panadiplon [inn] |
| panadiplon [usan] |
| SCHEMBL123304 |
| J-523865 |
| 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(propan-2-yl)imidazo[1,5-a]quinoxalin-4(5h)-one |
| DTXSID40869698 |
| panadiplon (u-78875) |
| 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-isopropylimidazo[1,5-a]quinoxalin-4(5h)-one |
| Q7129767 |
| imidazo[1,5-a]quinoxalin-4(5h)-one, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(1-methylethyl)- |
| HY-106851 |
| CS-0026726 |
Research Excerpts
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Panadiplon pretreatment resulted in leftward shifts in the pentobarbital dose-response function but predominantly rightward shifts of the triazolam dose-response function." | ( Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys. Rowlett, JK; Woolverton, WL, 2001) | 1.31 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Investigational toxicology methods, using appropriate models and hypotheses, can often resolve problems, identify toxic chemical substituents and salvage therapeutic discovery programs." | ( Cultured hepatocytes as investigational models for hepatic toxicity: practical applications in drug discovery and development. Bacon, JA; Cramer, CT; Peng, GW; Petrella, DK; Stryd, RP; Sun, EL; Ulrich, RG, 1995) | 0.29 |
| " Idiosyncratic toxic responses are often not detected during this phase in development due to their relative rarity in incidence and differences in species sensitivity." | ( Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon. Bacon, JA; Brass, EP; Cramer, CT; Petrella, DK; Sun, EL; Ulrich, RG, 2001) | 0.53 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Pharmacokinetic analysis of several compounds indicated excellent oral bioavailability and a reasonable half-life in rats." | ( Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. Belonga, KL; Carter, DB; Im, HK; Im, WB; Jacobsen, EJ; Mickelson, JW; Petke, JD; Sethy, VH; Stelzer, LS; Tang, AH; TenBrink, RE; VonVoigtlander, PF; Zhong, WZ, 1999) | 0.3 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Uniquely, a number of these analogues were found to have a bell-shaped dose-response profile in the alpha1 beta2 gamma2 subtype as determined by whole cell patch-clamp technique, where in vitro efficacy was found to decrease with increasing drug concentration." | ( Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. Belonga, KL; Carter, DB; Im, HK; Im, WB; Jacobsen, EJ; Mickelson, JW; Petke, JD; Sethy, VH; Stelzer, LS; Tang, AH; TenBrink, RE; VonVoigtlander, PF; Zhong, WZ, 1999) | 0.3 |
| " Panadiplon pretreatment resulted in leftward shifts in the pentobarbital dose-response function but predominantly rightward shifts of the triazolam dose-response function." | ( Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys. Rowlett, JK; Woolverton, WL, 2001) | 1.5 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (23)
Inhibition Measurements
Biological Processes (21)
Molecular Functions (11)
Ceullar Components (19)
Bioassays (31)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID173445 | Antagonism of metrazole-induced clonic convulsions in rats after ip injection | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID223126 | Compound was tested for ethanol potentiation expressed as loss of righting reflex (anesthesia) | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID35392 | In vitro efficacy calculated by chlorine current assay on alpha-1-beta-2-gamma-2 (GABA-A) receptor subtype | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID124224 | In vivo efficacy is evaluated by percent control of cerebellar GMP levels in (drug+stress) treated mice/mice under stress | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID39931 | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID73539 | Displacement of [3H]-Ro-15-4513 from GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in Sf9 cells | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID196345 | Inhibition of [35S]TBPS binding to GABA-A Benzodiazepine receptor of rat brain membranes | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID112327 | Ethanol potentiation was measured against LORR | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID196364 | In vitro [36Cl]-uptake in rat cerebrocortical synaptoneurosomes | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID72906 | Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID72136 | Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cortical membranes | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID177961 | Antagonistic activity against metrazole-induced clonic convulsions in rat after ip injection | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID112191 | In vivo antagonistic activity against benzodiazepine in mice | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID73226 | Displacement of [3H]flunitrazepam from GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in Sf9 cells | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID112326 | Ethanol potentiation activity was measured as loss of traction response in male CF-1 mice after oral administration | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID222344 | Compound was tested for Acute electroshock physical dependence activity (drug MA50/V122 MA50); No significant activity | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID44593 | In vitro GABA-mediated chloride current in A293 cells expressing GABA-A benzodiazepine receptor alpha-1-beta-2-gamma-2 subunits at 5 uM | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID72305 | In vitro inhibition of [35S]TBPS binding in rat brain membranes, activity expressed as [35S]TBPS shift value | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID123132 | In vivo acute electroshock physical dependence activity in mice; Not active. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID223125 | Antagonism of benzodiazepine traction in mice | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID72779 | In vitro efficacy for GABA-A alpha-1-beta-2-gamma-2 subtype expressed in A293 cells in Cl- current assay | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID73072 | Displacement of [3H]-Ro- 15-4513 from alpha-6 beta2 gamma2 subunits of Rat GABA-A receptor expressed in Sf-9 insect cell membranes | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID39930 | Binding affinity against benzodiazepine receptor (BzR) in rat cortical membranes determined by competition experiments with radiolabeled [3H]flunitrazepam (Fnz) | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID114819 | Ability to antagonize the muscle relaxation effect in mice caused by a benzodiazepine full agonist, triazolam. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID221056 | Ability to antagonize metrazole-induced seizures (clonic and tonic) in mice after intraperitoneal injection | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID40672 | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID223127 | Compound was tested for ethanol potentiation expressed as the loss of traction response (muscle relaxation) | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID72594 | In vitro efficacy by [35S]t-butyl-bicyclophosphorothionate (TBPS) binding to the picrotoxin convulsant site on the GABA-A receptor chloride complex. | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID108875 | Acute electroshock physical dependence activity was evaluated; IA=Inactive | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID72593 | Binding to GABA-A receptor complex relative to TBPS binding to picrotoxin convulsant site | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID177313 | In vivo efficacy evaluated for ability to antagonize metrazole induced clonic convulsions in rat after ip injection | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (20)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 18 (90.00) | 18.2507 |
| 2000's | 2 (10.00) | 29.6817 |
| 2010's | 0 (0.00) | 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: 11.12
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 weak demand-to-supply ratio for research on this compound.
| This Compound (11.12) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (10.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 18 (90.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||