perampanel : A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy. [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]
| ID Source | ID |
|---|---|
| PubMed CID | 9924495 |
| CHEMBL ID | 1214124 |
| CHEBI ID | 71013 |
| SCHEMBL ID | 194370 |
| MeSH ID | M0549034 |
| Synonym |
|---|
| perampanel |
| er-155055-90 |
| CHEMBL1214124 |
| e2007 |
| chebi:71013 , |
| e-2007 , |
| D08964 |
| perampanel (usan) |
| 380917-97-5 |
| perampanel [usan:inn] |
| e 2007 |
| h821664npk , |
| unii-h821664npk |
| benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl(2,3'-bipyridin)-5'-yl)- |
| 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one |
| fycompa |
| AM806751 |
| benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)- |
| HY-14745 |
| CS-1160 |
| perampanelum |
| 2-(6'-oxo-1'-phenyl-1',6'-dihydro-2,3'-bipyridin-5'-yl)benzonitrile |
| AKOS016340421 |
| 2-(2-oxo-1-phenyl-5-pyridin-2-ylpyridin-3-yl)benzonitrile |
| gtpl7050 |
| perampanel [orange book] |
| 5'-(2-cyanophenyl)-1'-phenyl-2,3'-bipyridinyl-6'(1'h)-one |
| perampanel [who-dd] |
| perampanel [inn] |
| perampanel [mi] |
| perampanel [usan] |
| perampanel [vandf] |
| 3-(2-cyanophenyl)-1-phenyl-5-(2-pyridyl)-1,2-dihydropyridin-2-one |
| PRMWGUBFXWROHD-UHFFFAOYSA-N |
| SCHEMBL194370 |
| CH-0056 |
| AC-27375 |
| 2-(6'-oxo-1'-phenyl[1',6'-dihydro[2,3'-bipyridine]]-5'-yl)benzonitrile |
| 6zp , |
| DTXSID80191501 , |
| NCGC00378863-02 |
| bdbm50184410 |
| perampanel(e2007 |
| DB08883 |
| BCP06505 |
| EX-A2128 |
| 1174302-51-2 |
| Q868658 |
| SB16816 |
| dtxcid50113992 |
| n03ax22 |
| ae4 - newer anti-epileptic drug mixtures 4 |
Perampanel (PER) is a new antiepileptic used to treat partial-onset seizures and generalized tonic-clonic seizures in people older than 12 years old. It is a noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonist. Its mechanism of action is not completely clear.
Perampanel has a 2,3'-bipyridin-6'-one core structure, distinguishing it chemically from other AMPA receptor antagonist classes. It has a long mean elimination half-life of 105 hours but may be reduced in the presence of enzyme-inducing antiepileptic drugs.
Perampanel (PER) has been shown to be effective as an adjunctive therapy for controlling refractory focal-onset seizures (FOS) The drug has been associated with relatively more tolerable cognitive effects in patients with epilepsy.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Perampanel was stopped because of inefficacy or paradoxical effects in 28.6% of cases and because of AEs in 7.1%." | ( The impact of perampanel treatment on quality of life and psychiatric symptoms in patients with drug-resistant focal epilepsy: An observational study in Italy. Canevini, MP; Chiesa, V; de Curtis, M; Deleo, F; Didato, G; Pappalardo, I; Pastori, C; Quintas, R; Turner, K; Villani, F; Zambrelli, E, 2019) | 1.6 |
Perampanel and LEV treatments have been associated with the occurrence of similar adverse events (AEs) (sleepiness, irritability, depression, anxiety, aggressiveness). Perampanels was considered effective when seizure frequency had been reduced by more than 50%. More perampanEL-treated patients had ≥ 75% reductions in SG seizure frequency.
This is the first prospective study on the efficacy and safety of perampanel monotherapy in treating Chinese patients with FOS. 11 adverse events (aggression, ataxia, balance disorder, dizziness, fall, fatigue, irritability, rash, somnolence, vertigo, and weight increase) were statistically significantly associated with perampAnel. 4 of them showed a clear dose-response relationship. These analyses suggest that psychiatric adverse effects are associated with use of perampsanel.
Perampanel is metabolized primarily via CYP3A4, yet it has a relatively long half-life of 105h. It is, therefore, recommended that perampsanel be given once daily (preferably at bedtime)
| Excerpt | Reference | Relevance |
|---|---|---|
| " Perampanel is metabolized primarily via CYP3A4, yet it has a relatively long half-life of 105h; it is, therefore, recommended that perampanel be given once daily (preferably at bedtime)." | ( The practical impact of altered dosing on perampanel plasma concentrations: pharmacokinetic modeling from clinical studies. Fain, R; Ferry, J; Gidal, BE; Hussein, Z; Laurenza, A; Majid, O; Yang, H; Zhu, J, 2014) | 1.58 |
| "Pharmacokinetic simulations were performed using validated perampanel pharmacokinetic parameters, derived from 19 phase I studies in 606 subjects, to investigate the effect on perampanel plasma concentration of (1) missing a dose of perampanel followed by delayed replacement of the missed dose, (2) missing a dose followed by resumption of scheduled therapy, and (3) missing a dose in the presence/absence of carbamazepine." | ( The practical impact of altered dosing on perampanel plasma concentrations: pharmacokinetic modeling from clinical studies. Fain, R; Ferry, J; Gidal, BE; Hussein, Z; Laurenza, A; Majid, O; Yang, H; Zhu, J, 2014) | 0.91 |
| "Our results corroborate that given the pharmacokinetic characteristics of perampanel, a missed dose is unlikely to cause as much fluctuation in plasma concentration as would be expected for a drug with a short half-life." | ( The practical impact of altered dosing on perampanel plasma concentrations: pharmacokinetic modeling from clinical studies. Fain, R; Ferry, J; Gidal, BE; Hussein, Z; Laurenza, A; Majid, O; Yang, H; Zhu, J, 2014) | 0.9 |
| "These pharmacokinetic simulations suggest that the long half-life of perampanel may be advantageous in conferring a relatively smooth concentration-time profile with a once-daily or twice-daily dosing, even in the presence of concomitant EIAEDs." | ( The practical impact of altered dosing on perampanel plasma concentrations: pharmacokinetic modeling from clinical studies. Fain, R; Ferry, J; Gidal, BE; Hussein, Z; Laurenza, A; Majid, O; Yang, H; Zhu, J, 2014) | 0.9 |
| "This study explored the pharmacodynamic and pharmacokinetic effects of combining perampanel (PER) with commonly co-administered AEDs." | ( Pharmacodynamic and pharmacokinetic interactions of perampanel and other antiepileptic drugs in a rat amygdala kindling model. Hanada, T; Nagaya, Y; Wu, T, 2014) | 0.88 |
| " Seizure score, electroencephalography (EEG) seizure duration, and motor seizure duration were evaluated, with pharmacodynamic interactions determined by two-way analysis of variance (ANOVA)." | ( Pharmacodynamic and pharmacokinetic interactions of perampanel and other antiepileptic drugs in a rat amygdala kindling model. Hanada, T; Nagaya, Y; Wu, T, 2014) | 0.65 |
| " These pharmacodynamic interactions were statistically significant in some cases, but the same AED combinations were not associated with statistically significant neurotoxic interactions." | ( Pharmacodynamic and pharmacokinetic interactions of perampanel and other antiepileptic drugs in a rat amygdala kindling model. Hanada, T; Nagaya, Y; Wu, T, 2014) | 0.65 |
| "Preclinical and clinical data of the recently released antiepileptic drug perampanel are reviewed based on search in medical databases with special reference to its mechanism of action and to its pharmacokinetic properties relevant for clinical treatment." | ( Perampanel for epilepsy with partial-onset seizures: a pharmacokinetic and pharmacodynamic evaluation. Schulze-Bonhage, A, 2015) | 2.09 |
| "To characterize, in adolescents aged 12-17, the pharmacokinetic (PK) profile of perampanel, the impact of intrinsic and extrinsic factors on PK, and the relationships between perampanel exposure and cognitive function, seizure frequency, and responder status." | ( Pharmacokinetics, exposure-cognition, and exposure-efficacy relationships of perampanel in adolescents with inadequately controlled partial-onset seizures. Ferry, J; Hussein, Z; Laurenza, A; Majid, O; Nabangchang, C; Villanueva, V; Yang, H, 2016) | 0.89 |
| " The elimination was slow, with terminal elimination phase half-life values ranging from 63." | ( Pharmacokinetics of Perampanel in Healthy Korean, White, and Japanese Adult Subjects. Ohnishi, A; Shiba, S; Shin, JG; Tabuchi, H; Yasuda, S, 2018) | 0.8 |
| " It is focused on pharmacokinetic and clinical data of perampanel (PER) for the treatment of epilepsy." | ( Pharmacokinetic and pharmacodynamic considerations for the clinical efficacy of perampanel in focal onset seizures. de Biase, S; Gigli, GL; Nilo, A; Romano, G; Valente, M, 2019) | 0.99 |
| " Pharmacokinetic data were pooled with adolescent pharmacokinetic data from phase II/III studies." | ( Adjunctive Perampanel Oral Suspension in Pediatric Patients From ≥2 to <12 Years of Age With Epilepsy: Pharmacokinetics, Safety, Tolerability, and Efficacy. Davis, R; Dispoto, S; Ferreira, J; Ferry, J; Hussein, Z; Laurenza, A; Majid, O; Mintz, M; Rege, B; Renfroe, JB; Umetsu, Y, 2019) | 0.9 |
| "We present pharmacokinetic data during pregnancy and lactation for brivaracetam, lacosamide and perampanel based on two case studies." | ( Pharmacokinetic data on brivaracetam, lacosamide and perampanel during pregnancy and lactation. Brodtkorb, E; Burns, ML; Johannessen, SI; Landmark, CJ; Rektorli, L; Revdal, E, 2021) | 1.09 |
| " This study aimed to develop a population pharmacokinetic (PPK) model considering the dynamics of enzyme induction and evaluate the effect of CBZ on PER pharmacokinetics." | ( Population Pharmacokinetic Analysis of Drug-Drug Interactions Between Perampanel and Carbamazepine Using Enzyme Induction Model in Epileptic Patients. Fujita, Y; Hirota, T; Ieiri, I; Matsunaga, N; Murai, M; Muraki, S; Suetsugu, K; Tsuchiya, Y, 2023) | 1.14 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model." | ( Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model. Alves, G; Falcão, A; Fortuna, A; Meirinho, S; Rodrigues, M, 2022) | 0.98 |
Perampanel is a potent noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazole propionate receptor (AMPAR) antagonist with good oral bioavailability and favorable pharmacokinetic properties.
Perampanel was given at a maximum dosage of 4-12 mg daily. Simulations demonstrated that twice-daily dosing offered little advantage in further flattening the concentration-time profile of perampsanel in the adherent patient.
| Role | Description |
|---|---|
| AMPA receptor antagonist | An antagonist at the AMPA receptor. |
| anticonvulsant | A drug used to prevent seizures or reduce their severity. |
| [role 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] | |
| Class | Description |
|---|---|
| pyridone | |
| nitrile | A compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it. |
| bipyridines | Compounds containing a bipyridine group. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 13.4504 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 175.0000 | 0.0002 | 2.4585 | 9.9600 | AID1805294 |
| Glutamate receptor 1 | Homo sapiens (human) | IC50 (µMol) | 1.8082 | 0.0190 | 1.7083 | 6.5100 | AID1309746; AID1309747; AID1309748; AID1309749; AID1309750 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1309748 | Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-3 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID496871 | Anticonvulsant activity in po dosed mouse assessed as inhibition of PTZ-induced seizures | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. |
| AID717944 | Ratio of drug level in brain to plasma in Sprague-Dawley rat at 10 mg/kg, po after 30 mins | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID1309746 | Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-8 and human EAAT3 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutam | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID717951 | AUC in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID496870 | Antagonist activity at AMPA receptor in rat cortical membrane assessed as inhibition of AMPA-induced calcium accumulation | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. |
| AID1309750 | Antagonist activity at human iGluA1 receptor flip isoform expressed in CHO-S cells assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 NW dye based fluore | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID717955 | Intrinsic clearance in rat liver microsomes after 15 mins by LC/MS/MS analysis | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717952 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717945 | Ratio of drug level in brain to plasma in ddY mouse at 3 mg/kg, po after 60 mins | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID1309765 | Anticonvulsant activity in po dosed Sprague-Dawley rat assessed as inhibition of pentylenetetrazole-induced clonic convulsions administered 30 mins prior to PTZ dosing measured over 30 mins | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID717943 | Ratio of drug level in CSF to fraction unbound in plasma in ddY mouse at 0.5 mg/kg, ip after 20 mins | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717956 | Intrinsic clearance in mouse liver microsomes after 15 mins by LC/MS/MS analysis | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717950 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717940 | Anticonvulsant activity in ICR mouse pentylenetetrazole-induced seizure model at 0.75 to 3 mg/kg, po after 30 mins | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717948 | Cmax in Sprague-Dawley rat at 1 mg/kg, po | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID496840 | Anticonvulsant activity in ip dosed DBA2 mouse assessed as inhibition of sound-induced clonic seizures | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. |
| AID717949 | Tmax in Sprague-Dawley rat at 1 mg/kg, po | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717939 | Half life in healthy human | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717946 | Oral bioavailability in Sprague-Dawley rat at 1 mg/kg | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID496866 | Anticonvulsant activity in po dosed mouse assessed as inhibition of MES-induced tonic seizures | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. |
| AID1309794 | Toxicity in Sprague-Dawley rat assessed as motor impairment at 30 mg/kg, po by inverted screen test | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID717942 | Anticonvulsant activity in DBA/2J mouse audinogenic seizure model at 0.3 to 3 mg/kg, po after 1 hr | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID717947 | AUC in Sprague-Dawley rat at 1 mg/kg, po | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID1309795 | Protective index, ratio of TD50 for motor impairment to ED50 for inhibition of pentylenetetrazole-induced clonic convulsions in po dosed Sprague-Dawley rat | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID1309749 | Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-4 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID717957 | Intrinsic clearance in human liver microsomes after 15 mins by LC/MS/MS analysis | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID1309747 | Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-2 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. |
| AID1766123 | Inhibition of recombinant SARS-CoV-2 main protease using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay | 2021 | ACS medicinal chemistry letters, Aug-12, Volume: 12, Issue:8 | Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency. |
| AID717941 | Anticonvulsant activity in ddY mouse MES-induced seizure model 0.75 to 2.12 mg/kg, po after 1hr | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID1678478 | Inhibition of recombinant His6-tagged SARS-CoV-2 main protease assessed as residual enzyme activity at 100 uM using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay relative to con | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2. |
| AID717953 | Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID1678479 | Inhibition of recombinant His6-tagged SARS-CoV-2 main protease using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2. |
| AID717954 | Anticonvulsant activity in po dosed ddY mouse AMPA-induced seizure model | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| AID496875 | Antiepileptic activity in human patient assessed as reduction in refractory partial seizures | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. |
| AID717958 | Antagonist activity at AMPA receptor in E18 rat cerebral cortical neurons assessed as inhibition of AMPA-induced intracellular Ca2+ response by fura-2 AM dye based fluorimetry | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel): a novel, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist. |
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| 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. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| AID1805294 | kinetic assay from Article 10.1021/acsmedchemlett.1c00326: \\Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.\\ | 2021 | ACS medicinal chemistry letters, Aug-12, Volume: 12, Issue:8 | Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 261 (51.18) | 24.3611 |
| 2020's | 249 (48.82) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (82.82) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 75 (14.42%) | 5.53% |
| Reviews | 88 (16.92%) | 6.00% |
| Case Studies | 49 (9.42%) | 4.05% |
| Observational | 51 (9.81%) | 0.25% |
| Other | 257 (49.42%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||