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clonazepam

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Description

Clonazepam is a benzodiazepine medication that is used to treat anxiety, seizures, and panic disorders. It works by enhancing the effects of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain. GABA is an inhibitory neurotransmitter that helps to reduce the activity of neurons in the brain, which can have calming effects. The synthesis of clonazepam involves a complex multi-step process starting with the reaction of 2-amino-5-chlorobenzophenone with ethyl chloroformate. This is followed by a series of reactions, including cyclization, halogenation, and dehydrogenation. The effects of clonazepam include sedation, muscle relaxation, and anticonvulsant effects. Its importance lies in its ability to effectively treat a variety of conditions. Clonazepam is studied to understand its mechanisms of action, potential side effects, and its effectiveness in treating different disorders. It is also studied to explore its potential in treating other conditions, such as pain and insomnia.'

Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. [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]

Cross-References

ID SourceID
PubMed CID2802
CHEMBL ID452
CHEBI ID3756
SCHEMBL ID38899
MeSH IDM0004601

Synonyms (130)

Synonym
AC-15733
ro 54023
BIDD:PXR0144
clonazepam [usan:usp:inn:ban:jan]
apetryl
5-24-04-00351 (beilstein handbook reference)
5pe9fde8gb ,
melzap
unii-5pe9fde8gb
106955-87-7
5-(o-chlorophenyl)-1,4-benzodiazepin-2-one
5-(2-chlorophenyl)-1,4-benzodiazepin-2-one
1,4.benzodiazepin-2-one
ro 4-8180
ro 5-4023
2-h-1, 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-
2h-1, 5-(2-chlorophenyl)-1,3-dihydro-7-nitro-
clonopin
ro4023
ro 5-4023/b-7
clonazepam
iktorivil
wln: t67 gmv jn ihj cnw kr bg
2h-1, 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-
1622-61-3
nsc-179913
nsc179913
cloazepam
rivotril
chlonazepam
5-(2-chloro-phenyl)-7-nitro-1,3-dihydro-benzo[e][1,4]diazepin-2-one
OPREA1_168772
ro 4023
klonopin
5-(2-chlorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one
antilepsin
2h-1,4-benzodiazepin-2-one, 5-(2-chlorophenyl)-1,3-dihydro-7-nitro-
landsen
2-h-1,4-benzodiazepin-2-one, 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-
antelepsin
DIVK1C_000973
KBIO1_000973
5-(2-chlorophenyl)-7-nitro-1,3-dihydro-2h-1,4-benzodiazepin-2-one
lktorivil
lonazep
dea no. 2737
rivatril
clonex
5-(2-chlorophenyl)-1,3-dihydro-7-nitro-2h-1,4-benzodiazepin-2-one
klonopin rapidly disintegrating
einecs 216-596-2
clonazepamum [inn-latin]
5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2h-1,4-benzodiazepin-2-one
5-(o-chlorophenyl)-7-nitro-1h-1,4-benzodiazepin-2(3h)-one
clonazepamum
solfidin
ravotril
brn 0759557
hsdb 3265
nsc 179913
kenoket
alti-clonazepam
7-nitro-5-(2-chlorophenyl)-3h-1,4-benzodiazepin-2(1h)-one
paxam
2h-1,4-benzodiazepin-2-one, 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-
IDI1_000973
clonazepam, powder
DB01068
5-(2-chlorophenyl)-7-nitro-1h-benzo[e][1,4]diazepin-2(3h)-one
1,3-dihydro-7-nitro-5-(2-chlorophenyl)-2h-1,4.benzodiazepin-2-one
5-(o-chlorophenyl)-7-nitro-1,3-dihydro-2h-1,4-benzodiazepin-2-one
clonazepam (jp17/usp/inn)
klonopin (tn)
D00280
NINDS_000973
HMS2093H22
clonazepam civ
ro-54023
ro-5-4023
CHEMBL452 ,
CHEBI:3756 ,
HMS503C07
bdbm50019213
A810362
smr000058982
MLS003899214
niosh/df2374250
1,3-dihydro-5-(o-chlorophenyl)-7-nitro-3h-1,4-benzodiazepin-2-one
3h-1,4-benzodiazepin-2-one, 1,3-dihydro-5-(o-chlorophenyl)-7-nitro-
DF23742500 ,
clonazepam [mi]
clonazepam [who-dd]
clonazepam [jan]
clonazepam [usan]
clonazepam [ep monograph]
clonazepam [hsdb]
clonazepam [inn]
clonazepam [usp monograph]
clonazepam [orange book]
clonazepam [mart.]
clonazepam civ [usp-rs]
clonazepam [vandf]
AKOS015902192
gtpl6963
CCG-213669
SCHEMBL38899
7-nitro-1,3-dihydro-5-(o-chlorophenyl)-2h-1,4-benzodiazepin-2-one
5-(2-chlorophenyl)-7-nitro-1,3-dihydro-2h-1,4-benzodiazepin-2-one #
clonazepam--dea schedule iv item
AB01563349_01
DTXSID1022845 ,
5-(2-chlorophenyl)-7-nitro-2,3-dihydro-1h-1,4-benzodiazepin-2-one
clonazepam, european pharmacopoeia (ep) reference standard
sr-01000937610
SR-01000937610-2
clonazepam 0.1 mg/ml in methanol
clonazepam 1.0 mg/ml in methanol
SBI-0206863.P001
Q407988
clonazepam (usp monograph)
n03ae01
clonazepam (usan:usp:inn:ban:jan)
clonazepam (ep monograph)
clonazepam (mart.)
clonazepam civ (usp-rs)
5-(2-chloro-phenyl)-7-nitro-1,3-dihydro-benzo(e)(1,4)diazepin-2-one
clonazepamum (inn-latin)
5-(2-chlorophenyl)-7-nitro-1h-benzo(e)(1,4)diazepin-2(3h)-one
dtxcid002845
clonazepam, 1mg/ml in methanol

Research Excerpts

Overview

Clonazepam is a 1-4 benzodiazepine mainly used to treat epilepsy and epileptiform convulsion state. It is considered to be a first-line treatment for rapid eye movement sleep-related behavior disorder (RBD) in Parkinson's disease.

ExcerptReferenceRelevance
"Clonazepam is a benzodiazepine commonly prescribed to treat panic disorder, epilepsy, anxiety, depression and certain types of seizures. "( A randomized, single-dose, two-sequence, two-period, crossover study to assess the bioequivalence between two formulations of clonazepam tablet in healthy subjects.
Davanço, MG; de Campos, DR; Duarte, FG; Guzmán, MRP; Meulman, J; Palomino, DMH; Tuiran, CMG, 2019
)
2.16
"Oral clonazepam is an effective therapy besides behavioral and safety interventions for hereditary cases."( Hyperekplexia and other startle syndromes.
Pandey, S; Saini, AG, 2020
)
1.01
"Clonazepam is considered to be a first-line treatment for rapid eye movement sleep-related behavior disorder (RBD) in Parkinson's disease (PD). "( Clonazepam for probable REM sleep behavior disorder in Parkinson's disease: A randomized placebo-controlled trial.
Jeon, B; Kim, HJ; Lee, WW; Park, H; Shin, C, 2019
)
3.4
"Clonazepam (CLZ) is a benzodiazepine derivative, whose bioavailability, limited by its very poor water-solubility, could be improved by cyclodextrin complexation. "( Physico-chemical characterization in solution and in the solid state of clonazepam complexes with native and chemically-modified cyclodextrins.
Bragagni, M; Maestrelli, F; Mennini, N; Mura, P, 2014
)
2.08
"Clonazepam is an antimuscarinic, muscle relaxing oral drug."( [Catheter-related bladder discomfort after urological surgery: importance of the type of surgery and efficiency of treatment by clonazepam].
Baron, T; Bourez, S; de la Taille, A; Maro, S; Salomon, L; Zarattin, D, 2014
)
1.33
"Clonazepam (CNZ) is a drug used for insomnia treatment. "( Executive dysfunction in patients with chronic primary insomnia treated with clonazepam.
Contreras-González, N; Haro, R; Jiménez-Correa, U; Poblano, A; Téllez-Alanís, B, 2015
)
2.09
"Clonazepam (CZ) is an anti-epileptic drug used mainly in status epilepticus (SE). "( Intranasal brain-targeted clonazepam polymeric micelles for immediate control of status epilepticus: in vitro optimization, ex vivo determination of cytotoxicity, in vivo biodistribution and pharmacodynamics studies.
Abdelmalak, NS; Ibrahim, AB; Naguib, MJ; Nour, SA; Rashed, HM, 2016
)
2.18
"Clonazepam wafers are an effective acute therapy for prolonged seizures."( Dissolving oral clonazepam wafers in the acute treatment of prolonged seizures.
Hastriter, EV; Ng, YT; Troester, MM, 2010
)
1.43
"Clonazepam is a 1-4 benzodiazepine mainly used to treat epilepsy and epileptiform convulsion state. "( [Therapeutic drug monitoring of clonazepam].
Bentué-Ferrer, D; Coquerel, A; Debruyne, D; Lelong-Boulouard, V; Pailliet-Loilier, M,
)
1.86
"Clonazepam is a benzodiazepine used for the treatment of seizures and panic disorders."( A fatal drug interaction between oxycodone and clonazepam.
Burrows, DL; Ferslew, KE; Hagardorn, AN; Harlan, GC; Wallen, ED, 2003
)
1.3
"Clonazepam, which is a benzodiazepine structurally related to chlordiazepoxide hydrochloride, diazepam and nitrazepam, has been available for the treatment of seizure disorders in the USA since 1976 and in Japan since 1981. "( [Clonazepam as a therapeutic adjunct to improve the management of depression].
Morishita, S, 2004
)
2.68
"Clonazepam (Klonopin) is a benzodiazepine that has been used widely to treat seizures and conditions such as panic attacks and anxiety disorder. "( Clonazepam use in pregnancy and the risk of malformations.
Franz, A; Holmes, LB; Houde, K; Lin, AE; Peller, AJ; Westgate, MN, 2004
)
3.21
"Clonazepam (klonopin) is a popular prescription drug that has been implicated in the field of drug facilitated sexual assaults (DFSA)."( Extraction and analysis of clonazepam and 7-aminoclonazepam in whole blood using a dual internal standard methodology.
Elian, AA; Hackett, J, 2007
)
1.36
"Clonazepam is a safe and effective drug for treatment of RLS; however its long-term efficacy needs confirmation."( Clonazepam and vibration in restless legs syndrome.
Cirignotta, F; Lugaresi, E; Montagna, P; Sassoli de Bianchi, L; Zucconi, M, 1984
)
2.43
"clonazepam is an effective, safe, but slower-acting alternative to I.M."( A double-blind randomized clinical trial of rapid tranquilization with I.M. clonazepam and I.M. haloperidol in agitated psychotic patients with manic symptoms.
Annable, L; Chouinard, G; Holobow, N; Szkrumelak, N; Turnier, L, 1993
)
1.24
"Clonazepam, which is a benzodiazepine structurally related to chlordiazepoxide hydrochloride, diazepam and nitrazepam, has been available for the treatment of seizure disorders in the USA since 1976 and in Japan since 1981. "( Clonazepam as a therapeutic adjunct to improve the management of psychiatric disorders.
Aoki, S; Morishita, S; Watanabe, S, 1998
)
3.19
"Clonazepam appears to be an effective therapeutic alternative in pati"( Efficacy and safety of clonazepam in refractory neurally mediated syncope.
Ashraf, R; Hee, TT; Hilleman, DE; Huebert, V; Kadri, NN; Mohiuddin, SM; Rovang, KS; Ryan, T, 1999
)
1.34
"Clonazepam, which is a benzodiazepine structurally related to chlordiazepoxide hydrochloride, diazepam and nitrazepam, has been available for the treatment of seizure disorders in the USA since 1976 and in Japan since 1981. "( [A trial of clonazepam treatment for manic-depressive psychoses].
Aoki, S; Morishita, S, 1999
)
2.13
"Clonazepam (CLO) is an anticonvulsant benzodiazepine approved by the Food and Drug Administration for use in the treatment of seizures. "( Quantitation of clonazepam and its major metabolite 7-aminoclonazepam in hair.
Janicak, PG; Kern, JL; Levy, NA; Moore, CM; Negrusz, A; Strong, MJ, 2000
)
2.1
"Clonazepam proved to be an efficient contributive factor in the course of a curing process since, in 70% of the cases, it produced quite a visible amelioration."( [Effects of clonazepam taken per os by children with rebellious epileptic encephalopathies].
Brun, JP; Gathier, MC; Gibert, J; Maupetit, F; Maupetit, J; Pechadre, JC, 1977
)
1.36
"Clonazepam is an antiepileptic drug for which a number of analytical procedures have been presented, none of which have been subjected to comparison studies. "( A methods comparison: clonazepam by gas chromatography-electron capture and gas chromatography-mass spectroscopy.
Friel, PN; Raisys, VA; Wilensky, AJ; Wilson, JM, 1979
)
2.02
"Clonazepam is a new benzodiazepine anticonvulsant recently approved by the Food and Drug Administration for the treatment of typical absence, infantile myoclonic, atypical absence, myoclonic, and akinetic seizures. "( Clonazepam. A review of a new anticonvulsant drug.
Browne, TR, 1976
)
3.14
"Clonazepam is an important addition to the therapy of intention myoclonus."( Intention myoclonus: successful treatment with clonazepam.
Dorman, JD; Goldberb, MA, 1976
)
1.23
"Clonazepam seems to be an effective drug in idiopathic trigeminal neuralgia. "( Clonazepam in facial neuralgia and cluster headache. Clinical and electrophysiological study.
Caccia, MR, 1975
)
3.14
"Clonazepam is a potent, long-acting benzodiazepine approved for use in myoclonic and petit mal seizures. "( Mania associated with clonazepam.
Dorevitch, A, 1991
)
2.04
"Clonazepam is a potent anticonvulsant 1,4-benzodiazepine that controls some types of myoclonus. "( Mechanism of action of clonazepam in myoclonus in relation to effects on GABA and 5-HT.
Jenner, P; Marsden, CD; Pratt, JA, 1986
)
2.02
"Clonazepam is a high-potency benzodiazepine labeled for use as an anticonvulsant. "( Clonazepam: new uses and potential problems.
Cohen, LS; Rosenbaum, JF, 1987
)
3.16
"Clonazepam is a high-potency 1,4-benzodiazepine derivative with an intermediate to long elimination half-life that is used mainly in neurology as an antiepileptic."( Clonazepam in the treatment of patients with recurrent panic attacks.
Annable, L; Beaudry, P; Chouinard, G; Fontaine, R, 1986
)
2.44

Effects

Clonazepam has a definite higher capacity, than the other drugs examined to prevent or to reduce the phenomenon of generalization of epilepsy. The drug has a relatively high molar affinity for the benzodiazepine receptor in vitro, and the fractional extent ofBenzodiazepin receptor occupation by clonazapam in vivo is directly and predictably related to the drug's concentration in brain tissue.

Clonazepam (CZP) has rarely been included in treatment guidelines for SE. The drug has been widely used in the treatment of SE patients and has unique advantages. Clonzepam has shown some efficacy in social phobia.

ExcerptReferenceRelevance
"Clonazepam has a definite higher capacity, than the other drugs examined to prevent or to reduce the phenomenon of generalization of epilepsy."( [Experimental comparative study on the antiepileptic effect of clonazepam, sodium dintoine and phenobarbital administered parenterally].
Iannelli, A; Meglio, M,
)
1.09
"Clonazepam, which has a longer half-life, would be expected to have some advantages over the other drugs."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
1.22
"Clonazepam has a relatively high molar affinity for the benzodiazepine receptor in vitro, and the fractional extent of benzodiazepine receptor occupation by clonazepam in vivo is directly and predictably related to the drug's concentration in brain tissue."( Clonazepam pharmacokinetics, brain uptake, and receptor interactions.
Greenblatt, DJ; Miller, LG; Shader, RI, 1987
)
2.44
"Clonazepam has a definite role in the management of parkinsonian dysarthria."( A double-blind trial of clonazepam in the treatment of parkinsonian dysarthria.
Biary, N; Langenberg, PW; Pimental, PA, 1988
)
1.3
"Clonazepam has been widely prescribed and is effective, but it is unclear whether clonazepam also affects the symptoms that accompany BMS, or whether such symptoms affect treatment outcomes."( Therapeutic effects of clonazepam in patients with burning mouth syndrome and various symptoms or psychological conditions.
Bang, JI; Kim, GJ; Kim, MR; Kim, SY; Shin, HI; Sun, DI, 2023
)
1.94
"Clonazepam (CZP) has rarely been included in treatment guidelines for SE; however, this drug has been widely used in the treatment of SE patients and has unique advantages."( Clonazepam in the treatment of status epilepticus.
Liao, H; Shangguan, Y; Wang, X, 2015
)
2.58
"Clonazepam has been used in the treatment of burning mouth syndrome (BMS) for several decades. "( Efficacy evaluation of clonazepam for symptom remission in burning mouth syndrome: a meta-analysis.
Chen, FM; Chen, QM; Cui, Y; Jiang, L; Liu, JL; Xu, H; Zhou, Y, 2016
)
2.19
"Clonazepam has been the first-line therapy for many years, with 2 large case series reporting efficacy with few side effects in the majority of patients."( Drug treatment of REM sleep behavior disorder: the use of drug therapies other than clonazepam.
Anderson, KN; Shneerson, JM, 2009
)
1.3
"Clonazepam has demonstrated effectiveness in several preliminary reports in treating OCD."( A double-blind, placebo-controlled trial of clonazepam in obsessive-compulsive disorder.
Hollander, E; Kaplan, A; Stahl, SM, 2003
)
1.3
"Clonazepam has been considered the treatment of choice for RBD. "( Melatonin for treatment of REM sleep behavior disorder in neurologic disorders: results in 14 patients.
Boeve, BF; Ferman, TJ; Silber, MH, 2003
)
1.76
"Clonazepam has shown some efficacy in social phobia; however, because this evidence is based on few studies, further studies are warranted before definitive conclusions can be drawn."( Clonazepam in the treatment of psychiatric disorders: an update.
Nardi, AE; Perna, G, 2006
)
2.5
"Clonazepam has been shown to be an effective supplementary treatment for depression. "( Possible predictors of response to clonazepam augmentation therapy in patients with protracted depression.
Arita, S; Morishita, S, 2007
)
2.06
"Clonazepam has been reported to be of some value in the treatment of benign essential tremor in open trials. "( A double-blind trial of clonazepam in benign essential tremor.
Lang, A; Marsden, CD; Parkes, JD; Thompson, C, 1984
)
2.02
"Clonazepam, which has low affinity for mBzR, is at least 500 times less potent at both channel activities."( Mitochondrial benzodiazepine receptor linked to inner membrane ion channels by nanomolar actions of ligands.
Antonenko, YN; Kinnally, KW; McEnery, MW; Snyder, SH; Tedeschi, H; Zorov, DB, 1993
)
1.01
"Clonazepam has recently been found by us to selectively diminish RD in BCECT."( Rhythmic slow activity in benign childhood epilepsy with centrotemporal spikes.
Mitsudome, A; Ogawa, A; Ohu, M; Yasumoto, S, 1997
)
1.02
"Clonazepam has several advantages over other benzodiazepines and can be considered a first-line agent for panic disorder."( Use of benzodiazepines in panic disorder.
Davidson, JR, 1997
)
1.02
"Clonazepam has recently been approved for the treatment of panic disorder. "( Pivotal studies of clonazepam in panic disorder.
Davidson, JR; Moroz, G, 1998
)
2.07
"Clonazepam has been found of particular benefit in the treatment of absence and myoclonic seizures."( Recent advances in drug therapy for epilepsy.
Bruni, J, 1979
)
0.98
"Clonazepam has given better results than valproate in temporal lobe and other partial (focal) epilepsies, while valproate has given better results in grand mal seizures and atonic attacks."( Sodium valproate and clonazepam in the treatment of intractable epilepsy.
Anthony, M; Lance, JW, 1977
)
1.3
"Clonazepam has a definite higher capacity, than the other drugs examined to prevent or to reduce the phenomenon of generalization of epilepsy."( [Experimental comparative study on the antiepileptic effect of clonazepam, sodium dintoine and phenobarbital administered parenterally].
Iannelli, A; Meglio, M,
)
1.09
"Clonazepam, which has a longer half-life, would be expected to have some advantages over the other drugs."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
1.22
"Clonazepam has been chosen for further study because in adults it reduced panic attacks and produced few serious side effects."( High anxiety in children.
Graae, F, 1990
)
1
"Clonazepam has a relatively high molar affinity for the benzodiazepine receptor in vitro, and the fractional extent of benzodiazepine receptor occupation by clonazepam in vivo is directly and predictably related to the drug's concentration in brain tissue."( Clonazepam pharmacokinetics, brain uptake, and receptor interactions.
Greenblatt, DJ; Miller, LG; Shader, RI, 1987
)
2.44
"Clonazepam has a definite role in the management of parkinsonian dysarthria."( A double-blind trial of clonazepam in the treatment of parkinsonian dysarthria.
Biary, N; Langenberg, PW; Pimental, PA, 1988
)
1.3

Actions

Clonazepam shows a much slower elimination with a half-life of 20 to 80 hours. It did not produce anaesthesia, at doses up to 1 g kg-1 or when given with nitrendipine.

ExcerptReferenceRelevance
"clonazepam, because of its more prolonged action, could be the drug of choice in controlling status epilepticus."( Intravenous clonazepam in the treatment of status epilepticus in children.
Congdon, PJ; Forsythe, WI, 1980
)
1.36
"Clonazepam shows a much slower elimination with a half-life of 20 to 80 hours."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
1.22
"Clonazepam did not produce anaesthesia, at doses up to 1 g kg-1 or when given with nitrendipine."( Differential interactions between benzodiazepines and the dihydropyridines, nitrendipine and Bay K 8644.
Dolin, SJ; Little, HJ; Patch, TL; Rabbani, M; Taberner, PV, 1991
)
1

Treatment

Clonazepam is useful for treatment-resistant and/or protracted depression, as well as for acceleration of response to conventional antidepressants. Clonazepingam is the treatment of choice for patients with RBD.

ExcerptReferenceRelevance
"Clonazepam and lorazepam treatment was equally effective at similar doses. "( Oral clonazepam versus lorazepam in the treatment of methamphetamine-poisoned children: a pilot clinical trial.
Farnaghi, F; Gachkar, L; Gholami, N; Hassanian-Moghaddam, H; McDonald, R; Rahmani, R; Zamani, N, 2020
)
2.51
"Clonazepam is useful for treatment-resistant and/or protracted depression, as well as for acceleration of response to conventional antidepressants."( Clonazepam as a therapeutic adjunct to improve the management of depression: a brief review.
Morishita, S, 2009
)
2.52
"Clonazepam is the treatment of choice for patients with RBD. "( Rapid eye movement sleep behavior disorder.
Gugger, JJ; Wagner, ML, 2007
)
1.78
"Clonazepam treatment decreased the paroxysms two times and more in 58.1% patients."( [New facts about pathogenesis of atrial fibrillation: correlation between changes in bioelectric brain activity and recurrence of atrial fibrillation paroxysms].
Fedorova, VI; Gordeev, SA; Nedostup, AV; Vasiukov, SS, 2007
)
1.06
"Clonazepam treatment led to a decrease in agitation and logorrhea, without the side effects associated with neuroleptics."( Use of clonazepam in mania and schizoaffective disorders.
Bell, IR; Binder, RL; Link, NA; Victor, BS, 1984
)
1.44
"Clonazepam-treated animals manifest a higher number of conditioned-reflex avoidance responses compared with the controls throughout the entire 5-day period."( Effect of clonazepam and electrolesions of the dorsal and medial raphe nuclei on learning.
Petkov, VV, 1980
)
1.38
"Clonazepam treatment resolved the see-saw nystagmus."( [Intermittent sea-saw nystagmus successfully treated with clonazepam].
Augustin, P; Cochin, JP; Didier, T; Do Marcolino, C; Hannequin, D, 1995
)
1.26
"Clonazepam-treated patients experienced significantly fewer panic attacks, and these were of lesser intensity and short duration than those in placebo-treated patients (p < 0.001)."( Clonazepam in the treatment of panic disorder: a double-blind, placebo-controlled trial investigating the correlation between clonazepam concentrations in plasma and clinical response.
Annable, L; Beauclair, L; Chouinard, G; Fontaine, R; Holobow, N, 1994
)
2.45
"Clonazepam treatment of RBD was completely or partially successful in 87% of the patients who used the drug."( Rapid eye movement sleep behaviour disorder: demographic, clinical and laboratory findings in 93 cases.
Boeve, BF; Olson, EJ; Silber, MH, 2000
)
1.03
"Clonazepam treatment in a dose 1-2 mg/day brought about a significant stabilization of blood pressure in 82.0% of patients with LHE."( [Labile hypertension in elderly: clinical features, autonomic regulation of circulation, approaches to treatment].
Dmitriev, KV; Fedorova, VI; Nedostup, AV, 2000
)
1.03
"The clonazepam treatment significantly decreased the total numbers of leg movements and the numbers of leg movements per hour without affecting the mean intermovement interval."( Periodic leg movements in sleep with restless legs syndrome: effect of clonazepam treatment.
Horiguchi, J; Inami, Y; Nishimatsu, O; Sasaki, A; Sukegawa, T, 1992
)
1
"Clonazepam treatment gave rise to beta-waves and prevented the increase in alpha and theta activity that was found in placebo subjects during the recording period; this was only true, however, for low to moderate plasma concentrations of clonazepam."( Hyperventilation-induced EEG changes in humans and their modulation by an anticonvulsant drug.
Rockstroh, B, 1990
)
1
"Clonazepam pretreatment inhibited both picrotoxin and allylglycine-induced myoelonus whereas AOAA was effective in inhibiting only picrotoxin-induced myoclonus."( The antimyoclonic action of clonazepam through a GABA--independent mechanism.
Krishnamoorthy, MS; Paul, V,
)
1.15
"Treatment with clonazepam predicts lower relapse when compared with paroxetine."( A 6-Year Posttreatment Follow-up of Panic Disorder Patients: Treatment With Clonazepam Predicts Lower Recurrence Than Treatment With Paroxetine.
Amrein, R; Arias-Carrión, O; Carta, MG; Dias, GP; Freire, RC; Machado, S; Mochcovitch, MD; Nardi, AE; Versiani, M, 2017
)
1.02
"Treatment with clonazepam markedly reduced the threshold and intensity of the startle response, enabling him to recover independence."( Sporadic hyperekplexia presenting with an ataxic gait.
Bilbao, I; Losada, J; Maestro, I; Rouco, I; Zarranz, JJ, 2014
)
0.74
"Treatment with clonazepam versus paroxetine resulted in fewer weekly panic attacks at week 4 (0.1 vs 0.5, respectively; P < 0.01), and greater clinical improvements at week 8 (CGI-I: 1.6 vs 2.9; P = 0.04)."( Psychopharmacotherapy of panic disorder: 8-week randomized trial with clonazepam and paroxetine.
Amrein, R; Crippa, JA; da Costa, RT; de Carvalho, MR; de Cerqueira, AC; de O E Silva, AC; de-Melo-Neto, VL; Dias, GP; Freire, RC; Hallak, JE; King, AL; Levitan, MN; Mezzasalma, MA; Mochcovitch, MD; Nardi, AE; Nascimento, I; Sardinha, A; Soares-Filho, GL; Valença, AM; Veras, AB; Versiani, M, 2011
)
0.94
"Treatment with clonazepam and propylthiouracil resulted in resolution of the myoclonic jerks within the next 3 weeks."( Graves' disease associated with spasmodic truncal flexion.
Hum, AY; Lim, EC; Loh, LM; Teoh, HL, 2005
)
0.67
"Treatment with clonazepam, frequent hospitalizations (drug-resistancy) and lack of occupational activity were revealed to be additional significant contributing factors."( Risk factors for depression in patients with epilepsy.
Fiszer, U; Grabowska-Grzyb, A; Jedrzejczak, J; Nagańska, E, 2006
)
0.67
"Treatment with clonazepam was very effective; it completely ameliorated the symptom of tongue biting but had no effect on chin trembling."( Recurrent nocturnal tongue biting in a child with hereditary chin trembling.
Goraya, JS; Parmar, V; Virdi, V, 2006
)
0.67
"Treatment with clonazepam 0.25mg nightly resulted in the disappearance of nocturnal events."( REM sleep behavior disorder in a patient with pontine stroke.
Luning, W; Xi, Z, 2009
)
0.69
"Treatment with clonazepam has abolished the nocturnal behavioural disturbance."( Conversion disorder revisited: severe parasomnia discovered.
Bokey, K, 1993
)
0.63
"Treatment with clonazepam."( Clonazepam for the treatment of lancinating phantom limb pain.
Bartusch, SL; D'Alessio, JG; Jernigan, JR; Sanders, BJ, 1996
)
2.09
"Treatment with clonazepam (CZP) (0.5 and 2.0 mg/kg), a GABA-benzodiazepine agonist, prior to MA administration prevented the acquisition of sensitization."( The role of gamma-aminobutyric acid (GABA)-benzodiazepine neurotransmission in an animal model of methamphetamine-induced psychosis.
Ito, K, 1999
)
0.64
"Treatment with clonazepam reduced the symptoms in case 2, and when combined with lithium, the disorder went into remission after 6 months."( Lithium and clonazepam treatment of two cases with cluster headache.
Fujikawa, T; Horiguchi, J; Kagaya, A; Takebayashi, M; Yamawaki, S, 1999
)
1.02
"Treatment with clonazepam 1 mg resulted in the striking disappearance of nystagmus."( [Acquired pendular nystagmus after pontine hemorrhage].
Amakusa, T; Kosaka, K; Yokota, J; Yoshimoto, Y, 1999
)
0.64
"Treatment with clonazepam in addition to sodium valproate resulted in a remarkable improvement of clinical symptoms (i.e."( A case of temporal lobe epilepsy with improvement of clinical symptoms and single photon emission computed tomography findings after treatment with clonazepam.
Ide, M; Mizukami, K; Shiraishi, H; Suzuki, T, 2000
)
0.85
"Treatment with clonazepam was effective in relieving these manifestations in the affected infants and children."( Hyperekplexia: pedigree studies in two families.
Hayashi, T; Kajii, T; Tachibana, H, 1991
)
0.62
"Treatment with clonazepam produced an initial depression in levels of most of the amino acids analyised."( The effects of two anticonvulsants on amino acid levels in the developing rat cerebellum.
Hannah, RS; Roth, SH; Spira, AW, 1989
)
0.62
"Treatment with clonazepam was studied in a group of 20 patients suffering from periodic movements in sleep, in a double-blind parallel group design. "( Double-blind evaluation of clonazepam on periodic leg movements in sleep.
Lavie, P; Peled, R, 1987
)
0.92
"Treatment with clonazepam, tetrabenazine hydrochloride, or other medications provides a satisfactory control in most patients."( Segmental myoclonus. Clinical and pharmacologic study.
Jankovic, J; Pardo, R, 1986
)
0.61

Toxicity

The adverse drug reactions (ADRs) related to clonazepam are mild, and only two cases of myotoxicity induced by the drug have been reported. Somnolence was the main adverse event associated with clonAZepam therapy.

ExcerptReferenceRelevance
" Safe discontinuation rates of CZP were estimated by comparing these patients with 23 patients without CZP discontinuation seizures."( Seizures with clonazepam: discontinuation and suggestions for safe discontinuation rates in children.
Sugai, K,
)
0.49
" Somnolence was the main adverse event associated with clonazepam therapy."( Efficacy, safety, and gradual discontinuation of clonazepam in panic disorder: a placebo-controlled, multicenter study using optimized dosages.
Moroz, G; Rosenbaum, JF, 1999
)
0.81
"In this placebo-controlled trial, clonazepam was an efficacious and safe shortterm treatment of the symptoms of panic disorder."( Efficacy, safety, and gradual discontinuation of clonazepam in panic disorder: a placebo-controlled, multicenter study using optimized dosages.
Moroz, G; Rosenbaum, JF, 1999
)
0.84
" On account of several experimental and clinical studies reporting effectiveness against the toxic effects of heroin and methamphetamine, chlormethiazole was systematically tested in the present study for its effectiveness against cocaine-induced seizures and lethality in mice."( Chlormethiazole: effectiveness against toxic effects of cocaine in mice.
Gasior, M; Ungard, JT; Witkin, JM, 2000
)
0.31
"Cardiac glycosides, which inhibit the plasma membrane Na(+) pump, are one of the four categories of drug recommended for routine use to treat heart failure, yet their therapeutic window is limited by toxic effects."( Role of mitochondrial dysfunction in cardiac glycoside toxicity.
Brown, DA; Liu, T; O'Rourke, B, 2010
)
0.36
" However, a complete reversal of encephalopathy, on withdrawal of the drug, strongly suggested an adverse drug reaction (ADR) due to valproic acid."( Encephalopathy in an infant with infantile spasms: possible role of valproate toxicity.
Sampath, S; Sivathanu, S; Sunderkumar, S; Veerasamy, M, 2014
)
0.4
" The relative safety of the 2 concentrations was evaluated in terms of occurrence of adverse drug reactions (ADRs) and occurrence of change to treatment plan secondary to ADRs."( Safety and tolerability of topical clonazepam solution for management of oral dysesthesia.
Ji, YD; Kelley, JM; Kuten-Shorrer, M; Lerman, MA; Palmason, S; Sonis, ST; Stock, S; Treister, NS; Villa, A; Woo, SB, 2017
)
0.73
"1 mg/mL concentration appears to be safe and well-tolerated."( Safety and tolerability of topical clonazepam solution for management of oral dysesthesia.
Ji, YD; Kelley, JM; Kuten-Shorrer, M; Lerman, MA; Palmason, S; Sonis, ST; Stock, S; Treister, NS; Villa, A; Woo, SB, 2017
)
0.73
" The goal of this study is to evaluate the potential of micelle-like nanoparticles (MNP) for providing safe drug usage in pregnancy and protect both foetus and mother from medication side effects."( Investigations on clonazepam-loaded polymeric micelle-like nanoparticles for safe drug administration during pregnancy.
Elcin, AE; Elcin, YM; Parmaksiz, M; Sezgin-Bayindir, Z; Yuksel, N, 2018
)
0.81
"The adverse drug reactions (ADRs) related to clonazepam are mild, and only two cases of myotoxicity induced by clonazepam have been reported, with both patients recovering well."( A serious adverse drug reaction probably induced by clonazepam: a case report of myotoxicity.
Han, X; Wang, J, 2019
)
1.02
" Mild adverse events were reported in three patients in the clonazepam, two patients in the trazodone group, and none in the melatonin group."( Safety and efficacy of melatonin, clonazepam, and trazodone in patients with Parkinson's disease and sleep disorders: a randomized, double-blind trial.
Agah, E; Aghamollaii, V; Hadi, F; Mirsepassi, Z; Mousavi, SV; Tafakhori, A; Talachi, N; Tavanbakhsh, S, 2022
)
1.24
" In the safety analysis, only mild or no serious adverse events were observed."( Safety and efficacy of clonazepam in patients with hemifacial spasm: A double-blind, randomized, placebo-controlled trial.
Ahn, SH; Baek, SH; Choi, K; Hong, YH; Kim, B; Kim, JS; Park, KH; Shin, JY; Sohn, SY; Sung, JJ, 2022
)
1.03
" The review included patients diagnosed with chorea and NKX2-1-RD genetic diagnosis, drug therapy as intervention, no comparator, and outcomes of chorea improvement and adverse events."( Systematic review of drug therapy for chorea in NXK2-1-related disorders: Efficacy and safety evidence from case studies and series.
Bachoud-Lévi, AC; Blasco-Amaro, JA; Capuano, A; Isabel-Gómez, R; Martín-Gómez, C; Nou-Fontanet, L; Ortigoza-Escobar, JD; Zorzi, G, 2023
)
0.91
" No clinical improvements were observed with carbidopa/levodopa, tetrabenazine, or clonazepam, and various adverse effects were reported."( Systematic review of drug therapy for chorea in NXK2-1-related disorders: Efficacy and safety evidence from case studies and series.
Bachoud-Lévi, AC; Blasco-Amaro, JA; Capuano, A; Isabel-Gómez, R; Martín-Gómez, C; Nou-Fontanet, L; Ortigoza-Escobar, JD; Zorzi, G, 2023
)
1.14

Pharmacokinetics

Clonazepam elimination half-life falls in the range of 20 to 80 hours, but means within the population and variance are not well defined. A population pharmacokinetic model was developed describing the PK of clonazapam in plasma and the relationship between plasma and saliva concentrations.

ExcerptReferenceRelevance
" The method was applied to pharmacokinetic and bioavailability studies of nitrazepam in humans."( Assay of underivatized intrazepam and clonazepam in plasma by capillary gas chromatography applied to pharmacokinetic and bioavailability studies in humans.
Bracht, H; Breimer, DD; de Boer, AG; Röst-Kaiser, J, 1978
)
0.53
"Anticonvulsant therapy was among the first areas to benefit from clinical pharmacokinetic studies."( Clinical pharmacokinetics of anticonvulsants.
Dam, M; Hvidberg, EF, 1976
)
0.26
"4 l/kg and the plasma half-life (t1/2) between 19 and 60 hours."( Pharmacokinetics of the anticonvulsant drug clonazepam evaluated from single oral and intravenous doses and by repeated oral administration.
Berlin, A; Dahlström, H, 1975
)
0.52
" Pharmacokinetic parameters were calculated using R-Strip for each age group."( Pharmacokinetics of clonazepam in developing rats.
Edge, JH; Ono, J; Walson, PD; Wang, L, 1992
)
0.61
" When the sequence of trials was placebo first and fluoxetine second, fluoxetine coadministration significantly prolonged alprazolam half-life (20 versus 17 hours) and reduced clearance (48 versus 61 ml/min)."( Fluoxetine impairs clearance of alprazolam but not of clonazepam.
Cotreau, MM; Greenblatt, DJ; Harmatz, JS; Horst, WD; Preskorn, SH, 1992
)
0.53
"Alprazolam, adinazolam, and clonazepam share the typical pharmacological effects of benzodiazepines yet are diverse in their pharmacokinetic properties."( Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam.
DeVane, CL; Lydiard, RB; Ware, MR, 1991
)
0.79
" Differences in pharmacokinetic parameters, therefore, will influence the choice of drug."( Pharmacokinetics and clinical use of benzodiazepines in the management of status epilepticus.
Treiman, DM, 1989
)
0.28
" Clonazepam elimination half-life falls in the range of 20 to 80 hours, but means within the population and variance are not well defined."( Clonazepam pharmacokinetics, brain uptake, and receptor interactions.
Greenblatt, DJ; Miller, LG; Shader, RI, 1987
)
2.63
" The correlation between receptor occupancy and the pharmacodynamic actions of these drugs in blocking pentylenetetrazol seizures and inducing rotarod ataxia indicated that ED50 for these effects occurred at receptor occupancy of 30 to 60% for both drugs."( Benzodiazepine receptor occupancy in vivo: correlation with brain concentrations and pharmacodynamic actions.
Greenblatt, DJ; Miller, LG; Paul, SM; Shader, RI, 1987
)
0.27
" The median elimination half-life (t1/2) in patients receiving concomitant valproate (VPA) was 43."( Pharmacokinetic interactions between lamotrigine and other antiepileptic drugs in children with intractable epilepsy.
Boreus, L; Eriksson, AS; Hoppu, K; Nergårdh, A, 1996
)
0.29
" diazepam (DZ), clonazepam (CZ), and a monocarbamate-based new compound (MCA) were studied in rabbits for the pharmacokinetics (PK) and pharmacodynamic (PD) response following intravenous (IV) and IN administrations."( Rapid-onset intranasal delivery of anticonvulsants: pharmacokinetic and pharmacodynamic evaluation in rabbits.
Choi, YM; Gorukanti, S; Kim, KH; Li, L, 2000
)
0.65
" The peak concentration (Cmax) of CZP and the time intervals from dosing to Cmax (Tmax) were 20."( Pharmacokinetic and pharmacodynamic effects of clonazepam in children with epilepsy treated with valproate: a preliminary study.
Wang, L; Wang, XD, 2002
)
0.57
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
" Any pharmacokinetic contribution was ascertained by measurement of brain antiepileptic drug (AED) concentrations."( Pharmacodynamic and/or pharmacokinetic characteristics of interactions between loreclezole and four conventional antiepileptic drugs in pentylenetetrazole-induced seizures in mice: an isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2005
)
0.33
"Nine healthy volunteers participated in a 3-phase clinical pharmacokinetic study of the benzodiazepine derivative clonazepam."( Clonazepam pharmacokinetics: comparison of subcutaneous microsphere injection with multiple-dose oral administration.
Blaskovich, PD; Chen, G; Greenblatt, DJ; Harmatz, JS; Nuwayser, ES; Zinny, MA, 2005
)
1.98
" Brain AED concentrations were also measured so as to ascertain any pharmacokinetic contribution to the pharmacodynamic interactions."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.54
" However, these interactions were complicated by changes in brain AED concentrations consequent to pharmacokinetic interactions."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.54
" However, these conclusions are confounded by the fact that STP is associated with significant pharmacokinetic interactions."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.54
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Pharmacokinetic (PK) data were compared with those previously collected in patients (n=127) treated with phenytoin for seizure prophylaxis."( Influence on Busilvex pharmacokinetics of clonazepam compared to previous phenytoin historical data.
Bacigalupo, A; Buzyn, A; Cahn, JY; Carreras, E; Kröger, N; Puozzo, C; Sanz, G; Vernant, JP, 2010
)
0.62
" Informed by these measurements, we built a pharmacokinetic model that quantitatively predicts microbiome contributions to systemic drug and metabolite exposure, as a function of bioavailability, host and microbial drug-metabolizing activity, drug and metabolite absorption, and intestinal transit kinetics."( Separating host and microbiome contributions to drug pharmacokinetics and toxicity.
Goodman, AL; Wegmann, R; Zimmermann, M; Zimmermann-Kogadeeva, M, 2019
)
0.51
" A population pharmacokinetic model was developed describing the PK of clonazepam in plasma and the relationship between plasma and saliva concentrations."( Population pharmacokinetics of clonazepam in saliva and plasma: Steps towards noninvasive pharmacokinetic studies in vulnerable populations.
Bergmann, KR; Cohen, AF; Egas, AC; Kruizinga, MD; Santen, GWE; van Esdonk, MJ; Zuiker, RGJA, 2022
)
1.24

Compound-Compound Interactions

The aim of this study was to investigate the repurposing of escitalopram oxalate and clonazepam drugs individually, and in combination with the antibiotics ciprofloxacin and sulfamethoxazole-trimethoprim.

ExcerptReferenceRelevance
" Phenytoin in combination with other drugs (anticonvulsives, antibiotics etc."( [Effects of drug interaction in infancy (author's transl)].
Alterthum, K; Bauer, P; Stünkel, S; Windorfer, A, 1980
)
0.26
"The effects of the benzodiazepines clonazepam (CLZ) and diazepam (DZ), introduced independently and in combination with cyproheptadine (CY) upon single and repeated application on apomorphine stereotypy in rats were studied."( Effects of single and repeated application of clonazepam and diazepam independently and in combination with cyproheptadine on apomorphine stereotypy in rats.
Georgiev, VP; Petkov, VV, 1984
)
0.8
"Valproic acid undergoes drug-drug interactions with most of the commonly used anticonvulsants."( Drug interactions with valproic acid.
Koch, KM; Levy, RH, 1982
)
0.26
" The present study aimed to compare nCPAP alone (n), nCPAP combined with clonazepam (n+c) and clonazepam alone (c) in patients with mild to moderate SAHS associated with high leg activity."( High leg motor activity in sleep apnea hypopnea patients: efficacy of clonazepam combined with nasal CPAP on polysomnographic variables.
De Maertelaer, V; Kempenaers, Ch; Kerkhofs, M; Lanquart, JR; Linkowski, R; Noseda, A; Nouvelle, M, 2002
)
0.78
"The anticonvulsant and acute adverse (neurotoxic) effects of STP in combination with the various conventional antiepileptic drugs (AEDs), at fixed ratios of 1:3, 1:1, and 3:1, were evaluated in the PTZ and chimney tests in mice using the isobolographic analysis."( Characterization of the anticonvulsant, behavioral and pharmacokinetic interaction profiles of stiripentol in combination with clonazepam, ethosuximide, phenobarbital, and valproate using isobolographic analysis.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.54
" Adverse-effect profiles of the drugs in combination were determined and brain AED concentrations were measured."( Isobolographic characterization of the anticonvulsant interaction profiles of levetiracetam in combination with clonazepam, ethosuximide, phenobarbital and valproate in the mouse pentylenetetrazole-induced seizure model.
Andres-Mach, MM; Czuczwar, SJ; Dudra-Jastrzebska, M; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2009
)
0.56
"To study the efficacy of levetiracetam (LEV) combined with short-term clonazepam (CZP) in the treatment of electrical status epilepticus during sleep (ESES) in children with benign childhood epilepsy with centrotemporal spikes (BECCT)."( [Efficacy of levetiracetam combined with short-term clonazepam in treatment of electrical status epilepticus during sleep in children with benign childhood epilepsy with centrotemporal spikes].
Chen, L; Su, TF; Xu, SQ, 2014
)
0.89
" Then, they received LEV in combination with short-term CZP."( [Efficacy of levetiracetam combined with short-term clonazepam in treatment of electrical status epilepticus during sleep in children with benign childhood epilepsy with centrotemporal spikes].
Chen, L; Su, TF; Xu, SQ, 2014
)
0.65
"LEV combined with short-term CZP is effective and has few side effects in treating ESES syndrome among children with BECCT."( [Efficacy of levetiracetam combined with short-term clonazepam in treatment of electrical status epilepticus during sleep in children with benign childhood epilepsy with centrotemporal spikes].
Chen, L; Su, TF; Xu, SQ, 2014
)
0.65
" The aim of this study was to investigate the repurposing of escitalopram oxalate and clonazepam drugs individually, and in combination with the antibiotics ciprofloxacin and sulfamethoxazole-trimethoprim, to treat multidrug-resistant (MDR) microorganisms and to evaluate the potential chemical nuclease activity."( Repurposing of escitalopram oxalate and clonazepam in combination with ciprofloxacin and sulfamethoxazole-trimethoprim for treatment of multidrug-resistant microorganisms and evaluation of the cleavage capacity of plasmid DNA.
Bottega, A; Coelho, SS; Foletto, VS; Hörner, R; Lorenzoni, VV; Machado, CS; Mainardi, A; Rampelotto, RF; Rosa, TFD; Serafin, MB, 2021
)
1.11

Bioavailability

A two-compartment distribution model best characterized clonazepam plasma kinetics with a mixture component on the absorption rate constants. The study was conducted in 24 fasting healthy male volunteers of Indian origin.

ExcerptReferenceRelevance
" It is suitable for investigations on pharmacokinetics and bioavailability as well as for monitoring the correlation between plasma level and therapeutic efficacy and toxicology."( Determination of flunitrazepam, desmethylflunitrazepam and clonazepam in plasma by gas liquid chromatography with an internal standard.
Aubert, C; Cano, JP; Guintrand, J; Viala, A, 1977
)
0.5
" They appear to be well absorbed when given by mouth, but their patterns of distribution within the body are different."( Pharmacokinetics of drugs used for petit mal 'absence' epilepsy.
Eadie, MJ; McKauge, L; Smith, GA; Tyrer, JH, 1977
)
0.26
" New knowledge of the pharmacokinetics of phenytoin has led to a better understanding of the drug's bioavailability and uses."( Recent advances in drug therapy for epilepsy.
Bruni, J, 1979
)
0.26
" The method was applied to pharmacokinetic and bioavailability studies of nitrazepam in humans."( Assay of underivatized intrazepam and clonazepam in plasma by capillary gas chromatography applied to pharmacokinetic and bioavailability studies in humans.
Bracht, H; Breimer, DD; de Boer, AG; Röst-Kaiser, J, 1978
)
0.53
" The absorption rate and fraction are very much dependent on the pharmaceutical preparation, and changes of brand may alter the plasma level of phenytoin in spite of unaltered dose."( Clinical pharmacokinetics of anticonvulsants.
Dam, M; Hvidberg, EF, 1976
)
0.26
" The bioavailability of CZP from the gel ointment was 47."( Percutaneous absorption of clonazepam in rabbit.
Ito, Y; Iwaki, M; Ogiso, T; Yamamoto, Y, 1989
)
0.57
" After oral administration absorption was rapid, but bioavailability poor and highly variable (20-60%)."( Pharmacokinetics of clonazepam in the dog.
Al-Tahan, F; Frey, HH; Löscher, W, 1984
)
0.59
" The absorption rate of MCA was relatively slower with the peak time of 13-32 min."( Rapid-onset intranasal delivery of anticonvulsants: pharmacokinetic and pharmacodynamic evaluation in rabbits.
Choi, YM; Gorukanti, S; Kim, KH; Li, L, 2000
)
0.31
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"To assess the bioavailability of clonazepam from two brands of 2 mg tablet formulations--Epitril and reference brand."( Comparative bioavailability study of clonazepam after oral administration of two tablet formulations.
Bhate, VR; Bhatt, AD; Chauhan, BL; Doshi, B; Kulkarni, RD; Rammamurthy, L; Revankar, SN; Sane, SP, 2000
)
0.86
"A two-way randomised cross-over bioavailability study was carried out in 12 healthy male volunteers."( Comparative bioavailability study of clonazepam after oral administration of two tablet formulations.
Bhate, VR; Bhatt, AD; Chauhan, BL; Doshi, B; Kulkarni, RD; Rammamurthy, L; Revankar, SN; Sane, SP, 2000
)
0.58
" administration, as shown by the mean absolute bioavailability of 93 and 90%, respectively."( Comparative single-dose pharmacokinetics of clonazepam following intravenous, intramuscular and oral administration to healthy volunteers.
Crevoisier, C; Delisle, MC; Foletti, G; Joseph, I, 2003
)
0.58
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" Considering the effective role of Klonopin (KNP) in the treatment of epilepsy, KNP quantification in its production process for dose adjustments and checking the purity and also after its usage by patents for bioavailability testing and effectiveness assay is vital."( Klonopin assay using modified electrode with multiwalled carbon nanotubes and poly melamine nanocomposite.
Ghalkhani, M; Khaloo, SS; Mirzaie, RA, 2019
)
0.51
"A two-compartment distribution model best characterized clonazepam plasma kinetics with a mixture component on the absorption rate constants."( Population pharmacokinetics of clonazepam in saliva and plasma: Steps towards noninvasive pharmacokinetic studies in vulnerable populations.
Bergmann, KR; Cohen, AF; Egas, AC; Kruizinga, MD; Santen, GWE; van Esdonk, MJ; Zuiker, RGJA, 2022
)
1.25

Dosage Studied

Plasma clonazepam and its metabolite were measured during a single dosing interval in 10 pediatric epilepsy patients (2-18 years, 11-102 kg) who had been receiving CZP therapeutically from 2 weeks to 4 years. The 3 drugs also show differences in elimination rate, which make it desirable to give valproate 3 times a day and clonzepam twice a day.

ExcerptRelevanceReference
" The 3 drugs also show differences in elimination rate, which make it desirable to give valproate 3 times a day and clonazepam twice a day, whereas ethosuximide could reasonably be given once daily without undesirably wide fluctuations in plasma drug level over the dosage interval."( Pharmacokinetics of drugs used for petit mal 'absence' epilepsy.
Eadie, MJ; McKauge, L; Smith, GA; Tyrer, JH, 1977
)
0.47
" The "specific" use of each drug on the various forms of epileptic seizures is determined and the possibility of crisis control with reduction of the drugs dosage is verified."( [Effect of drugs on electroclinical types of epileptic seizures in Lennox-Gastaut syndrome].
Lison, MP; Speciali, GG, 1977
)
0.26
"The applicability of a pharmacokinetic model for drug interactions by enzyme induction was tested by chronic dosing situation using carbamazepine (Tegretol) as the inducer and clonazepam (Clonopin) as the drug affected."( Time-course of interaction between carbamazepine and clonazepam in normal man.
Cutler, RE; Lai, AA; Levy, RH, 1978
)
0.7
" Combined treatment with other anticonvulsant drugs decreases the half-life and more frequent dosing may be necessary."( Clinical pharmacokinetics of anticonvulsants.
Dam, M; Hvidberg, EF, 1976
)
0.26
" Accordingly, the dosage is begun at a low level and increased slowly."( Clonazepam. A review of a new anticonvulsant drug.
Browne, TR, 1976
)
1.7
" The effective dosage was 7 to 12 mg a day in divided doses."( Intention myoclonus: successful treatment with clonazepam.
Dorman, JD; Goldberb, MA, 1976
)
0.51
" The plasma half-lives after cessation of the subchronic dosing were of the same magnitude as after single doses."( Pharmacokinetics of the anticonvulsant drug clonazepam evaluated from single oral and intravenous doses and by repeated oral administration.
Berlin, A; Dahlström, H, 1975
)
0.52
" If this is true in human, it is implicated in dosing of neonatal or pediatric patients."( Pharmacokinetics of clonazepam in developing rats.
Edge, JH; Ono, J; Walson, PD; Wang, L, 1992
)
0.61
" For treatment, the dosage and way of administration of diazepam should be judged according to the severeness of the disease; nitrazepam and clonazepam are effective, too."( [Clinical analysis of 30 cases of stiff-man syndrome].
Chen, BJ, 1992
)
0.49
" On the basis of these considerations and clinical reports describing the use of these drugs, we make dosage recommendations to enable the practitioner to individualize therapeutic regimens."( Drugs used in the management of trigeminal neuralgia.
Patsalos, PN; Zakrzewska, JM, 1992
)
0.28
" A significant improvement was found in the symptomatology of these patients, but relapses occurred when CLZ dosage was reduced."( Sodium valproate and clonazepam for treatment-resistant panic disorder.
Fontaine, R; Ontiveros, A, 1992
)
0.6
" High-performance liquid chromatographic analyses were performed on routinely ordered blood samples collected from chronically dosed outpatients during regular clinic visits."( Clonazepam and 7-aminoclonazepam in human plasma.
Edge, JH; Rane, A; Walson, PD, 1991
)
1.72
"We describe the case of a 26 years old woman in chronic therapy with phenobarbital, carbamazepine, valproic acid (VPA) and clonazepam who showed a hyperammonemic encephalopathy after an increase in dosage of VPA."( State of stupor from valproic acid during chronic treatment: case report.
Buffa, C; Gentile, S; Ravetti, C; Sacerdote, I, 1991
)
0.49
" Clonazepam, with its relatively long half-life, permits less frequent dosing than possible with benzodiazepines with shorter half-lives and more continuous control of anxiety, although around 20% of patients experience unacceptable sedative effects or no reduction in anxiety."( High-potency benzodiazepines for short-term management of panic disorder: the U.S. experience.
Tesar, GE, 1990
)
1.19
" After intravenous dosage with either drug, the area under the serum concentration curve (AUC) for the intact drug, as well as for the principal metabolites (lorazepam glucuronide and 7-aminoclonazepam, respectively), was nearly identical between portal and systemic serum."( Contribution of the gastrointestinal tract to lorazepam conjugation and clonazepam nitroreduction.
Eichelkraut, W; Greenblatt, DJ; Hahn, N; LeDuc, BW; Ochs, HR; Powers, JF, 1991
)
0.7
"Pigeons were trained in a cumulative dosing procedure to emit one response in the presence of 15 mg/kg phenytoin and another response in the absence of phenytoin."( Discriminative stimulus properties of phenytoin in the pigeon: determination via a cumulative dosing procedure.
Clark, R; Poling, A; Schlinger, H, 1990
)
0.28
" Fully kindled rats were dosed three times daily for 2 or 4 weeks."( Tolerance to anticonvulsant effects of diazepam, clonazepam, and clobazam in amygdala-kindled rats.
Chiu, TH; Rosenberg, HC; Tietz, EI,
)
0.39
"A trial transdermal dosage form designed to sustain a suitable plasma concentration of clonazepam (CZP) was produced using a porous membrane (Hipore 2100 or 4050) and applied to rabbits and rats for pharmacokinetic and pharmacodynamic evaluations."( Membrane-controlled transdermal therapeutic system containing clonazepam and anticonvulsant activity after its application.
Ito, Y; Iwaki, M; Ogiso, T; Yamamoto, Y, 1989
)
0.74
" Eighty-two percent (39) of the patients rated clonazepam as being "better" than alprazolam due to decreased dosing frequency and lack of interdose anxiety."( Rebound anxiety in panic disorder patients treated with shorter-acting benzodiazepines.
Brotman, AW; Herman, JB; Rosenbaum, JF, 1987
)
0.53
" The anticonvulsant and motor impairment effects of clobazam and 2 1,4-benzodiazepine, diazepam and clonazepam, were compared by dose-response analysis in amygdala-kindled rats and on 3 tests of motor function: gross motor impairment, a vertical screen test, and muscle tone."( A comparison of the anticonvulsant effects of 1,4- and 1,5-benzodiazepines in the amygdala-kindled rat and their effects on motor function.
Chiu, TH; Rosenberg, HC; Tietz, EI,
)
0.35
" Dosage of both drugs was within the usual range."( Carbamazepine and benzodiazepines in combination--a possibility to improve the efficacy of treatment of patients with 'intractable' infantile spasms?
Groh, C; Lischka, A; Müller, R; Tatzer, E, 1987
)
0.27
" Tremorolytic potency (ED50) was calculated from dose-response curves."( Cholecystokinin octapeptide (CCK-8), ceruletide and analogues of ceruletide: effects on tremors induced by oxotremorine, harmine and ibogaine. A comparison with prolyl-leucylglycine amide (MIF), anti-Parkinsonian drugs and clonazepam.
Zetler, G, 1983
)
0.45
" Though both blepharospasm and OMD are thought to represent focal dystonia at different body sites, the extent of improvement achieved with these drugs at the dosage employed differed markedly."( Meige's syndrome: acute and chronic responses to clonazepan and anticholinergics.
Giménez-Roldán, S; Hípola, D; Mateo, D, 1984
)
0.27
") administered in combination with naloxone and picrotoxin shifted dose-response curves for both naloxone and picrotoxin to the right."( Comparison of the effects of naloxone and picrotoxin on schedule-controlled responding in the pigeon: possible GABA-antagonistic effects of naloxone.
Carter, RB; Leander, JD, 1984
)
0.27
" New antiepileptic drugs have improved medical management, and technical and theoretical advances in pharmacokinetics have permitted physicians to design balanced dosing for individual patients."( Recent developments in the diagnosis and therapy of epilepsy.
Crandall, PH; Engel, J; Sterman, MB; Troupin, AS; Wasterlain, CG, 1982
)
0.26
" However, displacement alone, unlike induced metabolism, should not affect the drug's dose-response relationship."( Drug interactions with valproic acid.
Koch, KM; Levy, RH, 1982
)
0.26
" The following were taken as evaluation criteria: age, sex, performance status, duration and dosage of previous systemic and current spinal morphine therapy, concomitant analgesic and co-analgesic medication, pretreatment of the dorsal column and neurological dysfunction due to damage either of the nerval plexus or of the medulla spinalis."( Complications of spinal opioid therapy: myoclonus, spastic muscle tone and spinal jerking.
Bingel, U; Kloke, M; Seeber, S, 1994
)
0.29
"5 years, 78% of patients remained on medication and the mean dosage of alprazolam and clonazepam did not increase."( Long-term outcome after acute treatment with alprazolam or clonazepam for panic disorder.
Cohen, LS; Meltzer-Brody, S; Otto, MW; Pollack, MH; Rosenbaum, JF; Tesar, GE, 1993
)
0.75
"1 mg/kg) reduced by 54% the emotional stress-induced increase of colonic spike burst frequency, while a higher dosage (1 mg/kg) of methysergide had no effect."( Comparative involvement of 5-HT1, 5-HT2 and 5-HT3 receptors in stress-induced colonic motor alterations in rats.
Alary, C; Buéno, L; Gué, M; Junien, JL; Rio-Lacheze, CD, 1993
)
0.29
"In an attempt to investigate whether benzodiazepines at low dosage have a significant effect in reducing spasticity among children with cerebral palsy, we carried out a double-blind, placebo-controlled, cross-over study."( Treatment of spasticity in children with low dose benzodiazepine.
Dahlin, M; Knutsson, E; Nergårdh, A, 1993
)
0.29
"Long-term, nightly benzodiazepine treatment of injurious parasomnias and other disorders of disrupted nocturnal sleep resulted in sustained efficacy in most cases, with low risk of dosage tolerance, adverse effects, or abuse."( Long-term, nightly benzodiazepine treatment of injurious parasomnias and other disorders of disrupted nocturnal sleep in 170 adults.
Mahowald, MW; Schenck, CH, 1996
)
0.29
"Plasma clonazepam (CZP) and its metabolite [7-aminoclonazepam (7ACZP) and 7-acetamidoclonazepam (7AACZP)] concentrations were measured during a single dosing interval in 10 pediatric epilepsy patients (2-18 years, 11-102 kg) who had been receiving CZP therapeutically from 2 weeks to 4 years."( Clonazepam disposition in pediatric patients.
Edge, JH; Walson, PD, 1996
)
2.19
"The stability of drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied."( Stability of acetazolamide, allopurinol, azathioprine, clonazepam, and flucytosine in extemporaneously compounded oral liquids.
Allen, LV; Erickson, MA, 1996
)
0.54
" Pharmacokinetic study did not show induction mechanism at this dosage and with this type of administration."( [High dose ifosfamide at 15 g/m2/cycle: a feasibility study in 10 patients].
Baranzelli, MC; Deligny, N; Demaille, MC; Gourmel, B; N'Guyen, M; Pichon, F, 1997
)
0.3
"In this multicenter, parallel-group, placebo-controlled, fixed-dose study, the efficacy, safety, dosing characteristics, and discontinuation of clonazepam were analyzed in patients with panic disorder."( Clonazepam in the treatment of panic disorder with or without agoraphobia: a dose-response study of efficacy, safety, and discontinuance. Clonazepam Panic Disorder Dose-Response Study Group.
Bowden, CL; Moroz, G; Rosenbaum, JF, 1997
)
1.94
"A stability indicating, reversed phase high-performance liquid chromatographic method utilizing a smallbore HPLC column has been developed for the determination of clonazepam in a commercial tablet dosage form."( Analysis of clonazepam in a tablet dosage form using smallbore HPLC.
Spell, JC; Stewart, JT, 1998
)
0.87
" Clonazepam should, at the time, be considered only as an alternative treatment for patients nonresponsive to conventional therapy, and should be used at a dosage of 3-6 mg/day for depressive state and 10 mg/day for acute manic state in combination with other psychotropic drugs."( [A trial of clonazepam treatment for manic-depressive psychoses].
Aoki, S; Morishita, S, 1999
)
1.59
" The animals were intranasally dosed with DZ (1 mg/kg), CZ (0."( Rapid-onset intranasal delivery of anticonvulsants: pharmacokinetic and pharmacodynamic evaluation in rabbits.
Choi, YM; Gorukanti, S; Kim, KH; Li, L, 2000
)
0.31
" We investigated the effect of piracetam and clonazepam, an anti-epileptic drug, on high dosage urea-induced myoclonus using an electromyogram in rats."( [A pharmacological profile of piracetam (Myocalm), a drug for myoclonus].
Nanri, M; Tajima, K, 2000
)
0.57
" Fortunately, inpatient treatment was not necessary due to an increase of topiramate dosage and addition of risperidone and clonazepam."( Topiramate as a mood stabilizer.
Kasper, S; Letmaier, M; Schreinzer, D; Wolf, R, 2001
)
0.52
"The aims of the present study were (1) to investigate and quantify the pharmacokinetics, including inter-occasion variability and covariate relationships, of busulphan in BMT patients and (2) to develop a user-friendly initial dosing and therapeutic drug monitoring (TDM) strategy for the treatment of those patients with busulphan."( Population pharmacokinetic analysis resulting in a tool for dose individualization of busulphan in bone marrow transplantation recipients.
Bekassy, A; Hassan, M; Hassan, Z; Jonsson, EN; Karlsson, MO; Ljungman, P; Nilsson, C; Oberg, G; Ringden, O; Sandström, M, 2001
)
0.31
"Current dosing regimens of psychotropic drugs are based on plasma kinetic considerations, although it is unclear whether plasma levels faithfully reflect brain kinetics of drugs."( Significant dissociation of brain and plasma kinetics with antipsychotics.
Jones, C; Kapur, S; Remington, G; Tauscher, J; Zipursky, RB, 2002
)
0.31
" The peak concentration (Cmax) of CZP and the time intervals from dosing to Cmax (Tmax) were 20."( Pharmacokinetic and pharmacodynamic effects of clonazepam in children with epilepsy treated with valproate: a preliminary study.
Wang, L; Wang, XD, 2002
)
0.57
" Oral administration of high dosage of anticholinergic drugs is firstly recommended for the treatment of dystonia."( [Medical treatment of dystonia].
Kachi, T, 2001
)
0.31
"To evaluate the clinical efficacy of clonazepam in a fixed dosage (2 mg/day), compared to placebo, in the treatment of panic disorder patients and to verify whether there are any differences in the responses to clonazepam between panic disorder patients with the respiratory and non-respiratory subtypes."( Therapeutic response to benzodiazepine in panic disorder subtypes.
Lopes, FL; Mezzasalma, MA; Nardi, AE; Nascimento, I; Valença, AM; Versiani, M; Zin, WA, 2003
)
0.59
" Axis I and II psychiatric diagnosis was assessed and methadone dosage and history of abuse was recorded."( Treatment of benzodiazepine dependence in methadone maintenance treatment patients: a comparison of two therapeutic modalities and the role of psychiatric comorbidity.
Adelson, M; Bleich, A; Gelkopf, M; Melamed, Y; Weizman, T, 2003
)
0.32
"0-mg daily dosage of oral clonazepam during 60-180 days."( Clonazepam in the pharmacological treatment of vertigo and tinnitus.
Caovilla, HH; da Silva, ML; Ganança, CF; Ganança, FF; Ganança, MM; Munhoz, MS; Serafini, F, 2002
)
2.06
" The dosage of lamotrigine was increased and the patient received clonazepam intravenously, but a new seizure quickly occurred."( [Epileptic seizures during childbirth in a patient with idiopathic generalised epilepsy].
Bloem, BR; Renier, WO; Voermans, NC; Zwarts, MJ, 2005
)
0.57
" The dosage of clonazepam is higher (10."( [Misuse of clonazepam (Rivotril): recent trends].
Frauger, E; Micallef, J; Natali, F; Pradel, V; Reggio, P; Thirion, X,
)
0.87
" The steady-state plasma concentrations of AEDs at the experimental dosage were coincided with the range of clinical therapeutic concentrations."( [Experimental study on the possibility of brain damage induced by chronic treatment with phenobarbital, clonazepam, valproic acid and topiramate in immature rats].
Cai, FC; Zhang, XP; Zhu, HX, 2007
)
0.55
"Simple, accurate, precise, and sensitive ultraviolet spectrophotometric and reversed-phase high-performance liquid chromatographic (RP-HPLC) methods for simultaneous estimation of escitalopram oxalate (ESC) and clonazepam (CLO) in combined tablet dosage form have been developed and validated."( Spectrophotometric and reversed-phase high-performance liquid chromatographic methods for simultaneous determination of escitalopram oxalate and clonazepam in combined tablet dosage form.
Dhavale, ND; Gandhi, SV; Jadhav, VY; Sabnis, SS,
)
0.52
" Information for health professionals and workers in forensic structures as well as education of the general population associated with preventive measures such as drug dosage form changes should contribute to improved care management of victims and decreased risk."( Chemical submission: results of 4-year French inquiry.
Burin, E; Dally, S; Djezzar, S; Questel, F, 2009
)
0.35
" Limbic (psychomotor) seizure activity was evoked in albino Swiss mice by a current (32 mA, 6 Hz, 3s stimulus duration) delivered via ocular electrodes and isobolographic analysis for parallel and non-parallel dose-response effects was used to characterize the consequent anticonvulsant interactions between the various drug combinations."( Isobolographic characterization of interactions of levetiracetam with the various antiepileptic drugs in the mouse 6 Hz psychomotor seizure model.
Luszczki, JJ; Patsalos, PN; Wlaz, A; Wojda, E, 2009
)
0.35
" Phase 1 was a 6-week lead-in with open-label sertraline flexibly dosed to 100 mg (or escitalopram equivalent) to prospectively define treatment refractoriness (lack of remission)."( Next-step strategies for panic disorder refractory to initial pharmacotherapy: a 3-phase randomized clinical trial.
Hoge, EA; Lebeau, RT; Moshier, SJ; Otto, MW; Pollack, MH; Simon, NM; Thompson, EH; Worthington, JJ; Zalta, AK, 2009
)
0.35
"A semisolid dosage form of clonazepam (CZP), administered to the oral cavity between the lower gum and bottom lip with small volume of saline, was developed to obtain the stable dosage which can replace the injection dosage form."( [Development of semisolid dosage form of clonazepam for oral cavity administration].
Machida, Y; Onishi, H; Sakata, O, 2010
)
0.92
" Bu dosing and continued until 24 hours after the last dose."( Influence on Busilvex pharmacokinetics of clonazepam compared to previous phenytoin historical data.
Bacigalupo, A; Buzyn, A; Cahn, JY; Carreras, E; Kröger, N; Puozzo, C; Sanz, G; Vernant, JP, 2010
)
0.62
") dosage form of clonazepam (CZ), an oral droplet formulation of CZ was developed previously; however, the droplet was physically unstable."( Semi-solid dosage form of clonazepam for rapid oral mucosal absorption.
Machida, Y; Onishi, H; Sakata, O, 2011
)
1.01
"A semi-solid dosage form, composed of polyethylene glycol 1500 (PEG), CZ, and oleic acid (OA) at 37/1/2 (w/w) and named PEG/CZ/OA, and a semi-solid dosage form containing PEG and CZ at 39/1 (w/w), called PEG/CZ, were prepared."( Semi-solid dosage form of clonazepam for rapid oral mucosal absorption.
Machida, Y; Onishi, H; Sakata, O, 2011
)
0.67
"The semi-solid dosage forms were much more stable physically than the droplet, that is, no recrystallization of CZ was observed for at least 8 days."( Semi-solid dosage form of clonazepam for rapid oral mucosal absorption.
Machida, Y; Onishi, H; Sakata, O, 2011
)
0.67
"The objective of the current study was to develop a validated, specific stability-indicating reversed-phase liquid chromatographic (LC) method for the quantitative determination of escitalopram oxalate and clonazepam and their related substances in bulk drugs and pharmaceutical dosage forms in the presence of degradation products."( Stability-indicating RP-HPLC method for the simultaneous determination of escitalopram oxalate and clonazepam.
Gadapayale, KK; Kakde, MG; Kakde, RB; Satone, DD, 2013
)
0.79
"From these cases, we observe that a rough estimate of final clobazam dosage for each mg of clonazepam under substitution is likely to be at least 10-fold, probably closer to 15-fold for many patients, and as high as 20-fold for a few."( Clinical considerations in transitioning patients with epilepsy from clonazepam to clobazam: a case series.
Chung, S; Kuzniecky, R; Perry, MS; Sankar, R; Sinha, S, 2014
)
0.86
" In one case, a reduction in the dosage of clonazepam was also suggested."( Using venlafaxine to treat behavioral disorders in patients with autism spectrum disorder.
Bertschy, G; Carminati, F; Carminati, GG; Chabert, J; Darbellay, B; Deriaz, N; Fathi, M; Ferrero, F; Gerber, F; Kosel, MM, 2016
)
0.7
" Supra-therapeutic dosing of loperamide is promoted on multiple drug-use websites and online forums as a treatment for opioid withdrawal, as well as for euphoric effects."( Not your regular high: cardiac dysrhythmias caused by loperamide.
Biary, R; Hoffman, RS; Howland, MA; Lugassy, D; Rice, B; Wightman, RS, 2016
)
0.43
" The median CLB dosage did not change from baseline to last follow-up, while median CZP dosage increased 25% in adults and 50% in children."( Clobazam and clonazepam use in epilepsy: Results from a UK database incident user cohort study.
Brodie, MJ; Chung, S; François, C; Guiraud-Diawara, A; Isojarvi, J; Quelen, C; Shen, V; Verpillat, P; Wade, A, 2016
)
0.8
" The median CLB dosage used by both adults and children remained stable over the 16-year study period, while the median CZP dosage increased in both adults and children."( Clobazam and clonazepam use in epilepsy: Results from a UK database incident user cohort study.
Brodie, MJ; Chung, S; François, C; Guiraud-Diawara, A; Isojarvi, J; Quelen, C; Shen, V; Verpillat, P; Wade, A, 2016
)
0.8
" The exposure date, dose-response relationship, and class of BZRAs were comprehensively assessed."( The Use of Benzodiazepine Receptor Agonists and the Risk of Hospitalization for Pneumonia: A Nationwide Population-Based Nested Case-Control Study.
Chen, TY; Hsu, CY; Liu, CL; Mao, WC; Winkelman, JW; Wu, CS, 2018
)
0.48
"This study suggests that there is a dose-response relationship between current BZRA use and the risk of hospitalization for pneumonia."( The Use of Benzodiazepine Receptor Agonists and the Risk of Hospitalization for Pneumonia: A Nationwide Population-Based Nested Case-Control Study.
Chen, TY; Hsu, CY; Liu, CL; Mao, WC; Winkelman, JW; Wu, CS, 2018
)
0.48
"To infer the frequency of dosage and medication history investigate of the victims in drug facilitated cases by the segmental analysis of clonazepam in hair."( [The Role of Segmental Analysis of Clonazepam in Hair in Drug Facilitated Cases].
Chen, H; Shen, M; Xiang, P, 2017
)
0.93
"Segmental analysis of hair can provide the information of frequency of dosage and intake timing, which shows an unique evidential value in drug facilitated crimes."( [The Role of Segmental Analysis of Clonazepam in Hair in Drug Facilitated Cases].
Chen, H; Shen, M; Xiang, P, 2017
)
0.73
" Subsequently, the dosage was doubled (1mg twice daily), and complete cessation of seizures was achieved 20 days later."( Early onset epileptic encephalopathy with a novel GABRB3 mutation treated effectively with clonazepam: A case report.
Lian, Y; Xie, N; Zhang, Y, 2017
)
0.68
" Medication dosing generally followed standard dosing guidelines with very few exceptions."( Seizure Rescue Medication Use among US Pediatric Epilepsy Providers: A Survey of the Pediatric Epilepsy Research Consortium.
Payne, E; Wallace, A; Wirrell, E, 2019
)
0.51
"The scoping review identified 57 studies with most data available on their tolerability (68% local, 54% systemic), clinical effects (82%), details on dosage (96%) and routes of application (100%)."( Subcutaneous Drugs and Off-label Use in Hospice and Palliative Care: A Scoping Review.
Dürr, F; Jean-Petit-Matile, S; Kobleder, A; Meyer-Massetti, C; Wernli, U, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anticonvulsantA drug used to prevent seizures or reduce their severity.
GABA modulatorA substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor-ionophore complex. GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of gamma-aminobutyric acid-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act.
anxiolytic drugAnxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions.
[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]

Drug Classes (2)

ClassDescription
1,4-benzodiazepinone
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
[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 (44)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki0.00090.00090.89545.6234AID239299
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki0.00090.00090.89545.6234AID239299
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)Ki0.00090.00010.04380.1630AID41853; AID41871
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)Ki0.00090.00010.04380.1630AID41853; AID41871
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.00090.00000.12345.5000AID239299
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)Ki0.00090.00010.04530.1630AID41853; AID41871
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)Ki0.00090.00010.04530.1630AID41853; AID41871
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.00090.00000.10825.5000AID239299
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50 (µMol)555,904.00000.00011.14948.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.00090.00000.21085.6234AID239299
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50 (µMol)555,904.00000.00011.03936.0000AID40995
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.00090.00090.83985.6234AID239299
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50 (µMol)555,904.00000.00011.29158.0000AID40995
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.00090.00000.18819.0000AID239299
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.505710.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.497310.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)Ki0.00090.00010.04530.1630AID41853; AID41871
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)Ki0.00090.00010.04530.1630AID41853; AID41871
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.498810.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.504610.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50 (µMol)555,904.00000.00011.30188.0000AID40995
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.00090.00010.20769.0000AID239299
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Translocator proteinBos taurus (cattle)Ki0.00090.00090.00090.0009AID1894694
Translocator proteinHomo sapiens (human)IC50 (µMol)555,904.00000.00030.13020.4900AID40987
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)100.00000.00000.43624.3000AID52410; AID52413
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00010.24801.4000AID52410
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50 (µMol)555,904.00000.00010.98006.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.00090.00010.24425.6234AID239299
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50 (µMol)555,904.00000.00011.19936.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.00090.00010.25155.6234AID239299
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.00090.00010.24015.6234AID239299
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50 (µMol)555,904.00000.00010.93746.0000AID40995
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.00090.00000.28325.6234AID239299
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)555,904.00000.00011.01936.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki0.00090.00020.37095.6234AID239299
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.506510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.505710.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki0.00090.00090.89545.6234AID239299
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.00090.00020.41199.0000AID239299
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki0.00090.00090.89545.6234AID239299
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki0.00090.00090.89545.6234AID239299
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.00170.00010.507510.0000AID40817; AID40826
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50 (µMol)555,904.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki0.00090.00090.89545.6234AID239299
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (64)

Processvia Protein(s)Taxonomy
chloride transmembrane transportGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
monoatomic ion transportGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
monoatomic ion transportGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
response to toxic substanceGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
central nervous system neuron developmentGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
response to progesteroneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ovulation cycleGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
signal transductionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
roof of mouth developmentGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
lipid transportTranslocator proteinBos taurus (cattle)
protein targeting to mitochondrionTranslocator proteinHomo sapiens (human)
C21-steroid hormone biosynthetic processTranslocator proteinHomo sapiens (human)
heme biosynthetic processTranslocator proteinHomo sapiens (human)
monoatomic anion transportTranslocator proteinHomo sapiens (human)
chloride transportTranslocator proteinHomo sapiens (human)
steroid metabolic processTranslocator proteinHomo sapiens (human)
glial cell migrationTranslocator proteinHomo sapiens (human)
response to xenobiotic stimulusTranslocator proteinHomo sapiens (human)
response to manganese ionTranslocator proteinHomo sapiens (human)
response to vitamin B1Translocator proteinHomo sapiens (human)
peripheral nervous system axon regenerationTranslocator proteinHomo sapiens (human)
sterol transportTranslocator proteinHomo sapiens (human)
adrenal gland developmentTranslocator proteinHomo sapiens (human)
negative regulation of protein ubiquitinationTranslocator proteinHomo sapiens (human)
regulation of cholesterol transportTranslocator proteinHomo sapiens (human)
response to progesteroneTranslocator proteinHomo sapiens (human)
negative regulation of tumor necrosis factor productionTranslocator proteinHomo sapiens (human)
response to testosteroneTranslocator proteinHomo sapiens (human)
regulation of cell population proliferationTranslocator proteinHomo sapiens (human)
cholesterol homeostasisTranslocator proteinHomo sapiens (human)
positive regulation of apoptotic processTranslocator proteinHomo sapiens (human)
negative regulation of nitric oxide biosynthetic processTranslocator proteinHomo sapiens (human)
behavioral response to painTranslocator proteinHomo sapiens (human)
regulation of steroid biosynthetic processTranslocator proteinHomo sapiens (human)
positive regulation of mitochondrial depolarizationTranslocator proteinHomo sapiens (human)
positive regulation of calcium ion transportTranslocator proteinHomo sapiens (human)
contact inhibitionTranslocator proteinHomo sapiens (human)
positive regulation of glial cell proliferationTranslocator proteinHomo sapiens (human)
negative regulation of glial cell proliferationTranslocator proteinHomo sapiens (human)
positive regulation of programmed necrotic cell deathTranslocator proteinHomo sapiens (human)
cellular response to lipopolysaccharideTranslocator proteinHomo sapiens (human)
cellular response to zinc ionTranslocator proteinHomo sapiens (human)
cellular hypotonic responseTranslocator proteinHomo sapiens (human)
maintenance of protein location in mitochondrionTranslocator proteinHomo sapiens (human)
negative regulation of mitophagyTranslocator proteinHomo sapiens (human)
negative regulation of ATP metabolic processTranslocator proteinHomo sapiens (human)
response to acetylcholineTranslocator proteinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processTranslocator proteinHomo sapiens (human)
negative regulation of corticosterone secretionTranslocator proteinHomo sapiens (human)
behavioral fear responseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
associative learningGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
negative regulation of chloride transportGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
response to xenobiotic stimulusGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
neurotransmitter transportGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
GABA-A receptor activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
ligand-gated monoatomic ion channel activityGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ligand-gated monoatomic ion channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
identical protein bindingGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
androgen bindingTranslocator proteinHomo sapiens (human)
protein bindingTranslocator proteinHomo sapiens (human)
benzodiazepine receptor activityTranslocator proteinHomo sapiens (human)
cholesterol bindingTranslocator proteinHomo sapiens (human)
transmembrane transporter bindingTranslocator proteinHomo sapiens (human)
cholesterol transfer activityTranslocator proteinHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signaling receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmembrane signaling receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neurotransmitter transmembrane transporter activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
apical plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
axonGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
dendriteGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
postsynaptic membraneGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
nuclear envelopeGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
dendriteGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
presynaptic active zone membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
Schaffer collateral - CA1 synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
mitochondrial membraneTranslocator proteinBos taurus (cattle)
mitochondrionTranslocator proteinHomo sapiens (human)
mitochondrial outer membraneTranslocator proteinHomo sapiens (human)
cytosolTranslocator proteinHomo sapiens (human)
intracellular membrane-bounded organelleTranslocator proteinHomo sapiens (human)
extracellular exosomeTranslocator proteinHomo sapiens (human)
endoplasmic reticulumTranslocator proteinHomo sapiens (human)
membraneTranslocator proteinHomo sapiens (human)
nucleoplasmGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cytosolGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuronal cell body membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
postsynaptic membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
cerebellar Golgi cell to granule cell synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
nucleolusGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
microtubule cytoskeletonGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
receptor complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (145)

Assay IDTitleYearJournalArticle
AID40826Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain1988Journal of medicinal chemistry, Dec, Volume: 31, Issue:12
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID418134Anticonvulsant activity in po dosed rat assessed as protection against maximal electroshock-induced seizure2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1150165Muscle relaxant activity in cat suspended by scruff of neck assessed as relaxation of body and hind legs1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID23479Partition coefficient (logP)1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID1150162Muscle relaxant activity in mouse1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID418131Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizure2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1128799Binding affinity to human serum albumin at 30 uM by HPLC analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID1256681Neurotoxicity in Chinese Kun Ming mouse assessed as locomotor activity by measuring total distance traveled at 10 mg/kg, po administered 1 hr before test measured for 10 mins (Rvb = 13881.4 +/- 8595.8 millimeter)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID1704779Effect on spontaneous locomotor activity in Kunming mouse assessed as total distance traveled at 1 mg/kg, ig measured after 1 hr (Rvb = 13579 +/- 8864 millimeter)
AID131927Tested for inhibition of quinoline-induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID131925Tested for inhibition of pentylenetetrazole induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID604742Displacement of radiolabeled dansylsarcosine from fatty acid-free human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID540230Dose normalised AUC in rat after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID306152Induction of reactive oxygen species response in Jurkat cells after 1 hr2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID306149Inhibition of F1F0-ATPase hydrolysis activity in bovine submitochondrial particles2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID291617Displacement of [3H]flunitrazepam from BZ-site of GABAA receptor in Sprague-Dawley rat cortex membrane2007Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
Enaminone amides as novel orally active GABAA receptor modulators.
AID1150164Anticonvulsion activity in mouse assessed as protection against pentylenetetrazole-induced convulsion1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID52280Half-maximal inhibition of [125I]-CCK-8(+) binding to cholecystokinin receptor from guinea pig brain tissue1988Journal of medicinal chemistry, Dec, Volume: 31, Issue:12
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
AID1150163Taming activity in mouse assessed as suppression of electrical current-induced aggressive behavior by foot-shock test1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID227700Anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1128800Binding affinity to rat serum albumin at 30 uM by HPLC analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID418136Toxicity in po dosed rat assessed as minimal muscular or neurological impairment by rotarod paradigm test2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID1079933Acute 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
AID226431Relative binding to GABA-A receptor in the presence and absence of GABA (GABA shift), Ki(-GABA)/Ki(+GABA)1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID40995Binding affinity towards benzodiazepine/GABA A receptor.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID40817Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1704781Effect on spontaneous locomotor activity in Kunming mouse assessed as total distance traveled at 10 mg/kg, ig measured after 1 hr (Rvb = 13579 +/- 8864 millimeter)
AID225156Dose reducing the seizure severity in rat cornea 1 hr after peroral administration1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID227697Compound was evaluated for the Anti-fighting behavior.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID131913Tested for inhibition of maximal electroshock -induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID418133Toxicity in ip dosed mouse assessed as minimal muscular or neurological impairment by rotarod paradigm test2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID1150161Sedative activity in mouse1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID239299Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1256679Neurotoxicity in Chinese Kun Ming mouse assessed as locomotor activity by measuring total distance traveled at 1 mg/kg, po administered 1 hr before test measured for 10 mins (Rvb = 13881.4 +/- 8595.8 millimeter)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID40987Binding affinity of compound towards Benzodiazepine receptor in a competition assay1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID72312Relative binding to GABA-A receptor in the presence and absence of GABA (GABA shift), Ki(-GABA)/Ki(+GABA)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis, structure-activity relationships, and molecular modeling studies of N-(indol-3-ylglyoxylyl)benzylamine derivatives acting at the benzodiazepine receptor.
AID306151Induction of reactive oxygen species response in Ramos cells after 1 hr2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID41871Inhibition of [3H]- flumazenil binding to benzodiazepine receptor in bovine brain membranes2001Journal of medicinal chemistry, Jul-05, Volume: 44, Issue:14
Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID219916Stimulation of steroid (pregnenolone) biosynthesis in mouse Y-1 adrenocortical cells at 40 uM1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID604744Displacement of radiolabeled dansylsarcosine from fatty acid containing human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID227698Evaluation for the Anti-pentylenetetrazole effect.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID226275Relative binding to GABA-A receptor in the presence and absence of GABA (GABA shift), Ki(-GABA)/Ki(+GABA)2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands.
AID338175Displacement of [3H]flunitrazepam from benzodiazepine receptor assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID306150Inhibition of F1F0-ATPase synthesis activity in bovine submitochondrial particles2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID41988Displacement of [3H]- Ro.15-1788 from GABA-A central Benzodiazepine receptor (BzR) of Bovine cerebral cortex membrane2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands.
AID131776Tested for inhibition of 3-mercaptopropanoic acid induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID539470Solubility of the compound in water2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079936Choleostatic 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]
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID41741Inhibition of [35S]-TBPS binding to GABA-A central Benzodiazepine Receptor of bovine cerebral cortex membranes2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands.
AID71572Inhibition of TBPS binding to GABA-A receptor of bovine brain membranes at 0.5 uM relative to clonazepam1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.
AID52413Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue1988Journal of medicinal chemistry, Dec, Volume: 31, Issue:12
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
AID29360Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID418137Therapeutic index, ratio of TD50 for ip dosed mouse to ED50 for protection against subcutaneous metrazole-induced seizure in ip dosed mouse2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID418138Therapeutic index, ratio of TD50 for po dosed rat to ED50 for protection against subcutaneous metrazole-induced seizure in po dosed rat2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID418135Anticonvulsant activity in po dosed rat assessed as protection against subcutaneous metrazole-induced seizure2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID1894694Binding affinity to bovine brain membrane BzR assessed as inhibition constant2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID41853In vitro inhibition of [3H]-Ro- 15-1788 binding to GABA-A Benzodiazepine receptor of bovine brain membranes1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.
AID1128801Binding affinity to human serum albumin2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID102218Stimulatory effect on progesterone biosynthesis in MA10 leydig cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR).
AID1079931Moderate 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]
AID306153Induction of cell death in Ramos cells after 24 hrs2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID1079938Chronic 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]
AID1079935Cytolytic 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]
AID229422Selectivity of binding to pancreatic CCK and brain benzodiazepine receptors, ratio of IC501987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
AID232605Ratio of IC50 CCK(pancreas)/ IC50BZD (brain)1988Journal of medicinal chemistry, Dec, Volume: 31, Issue:12
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
AID131910Tested for inhibition of bicuculline induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID604741Displacement of radiolabeled warfarin from fatty acid-free human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID1660982Inhibition of Escherichia coli Stx2 in human HeLa cells assessed as stimulation of protein synthesis by measuring increase in [14C]-leucine incorporation at 30 uM incubated with cells for 4 hrs prior to Stx2 addition and further incubated for 20 hrs and s2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin.
AID540232Dose normalised AUC in monkey after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID41873Ratio of Ki with out GABA and with GABA2001Journal of medicinal chemistry, Jul-05, Volume: 44, Issue:14
Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID280839Displacement of [3H]flumazenil from benzodiazepine receptor in bovine brain membranes2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
AID1256680Neurotoxicity in Chinese Kun Ming mouse assessed as locomotor activity by measuring total distance traveled at 3 mg/kg, po administered 1 hr before test measured for 10 mins (Rvb = 13881.4 +/- 8595.8 millimeter)2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID52410Half-maximal inhibition of [125I]-CCK-33 binding to rat pancreas cholecystokinin receptor1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID337891Displacement of [3H]flunitrazepam from benzodiazepine receptor1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID72591Specific [35S]- TBPS binding at high affinity site loated near chloride channel of GABA-A receptor chloride complex1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis, structure-activity relationships, and molecular modeling studies of N-(indol-3-ylglyoxylyl)benzylamine derivatives acting at the benzodiazepine receptor.
AID418132Anticonvulsant activity in ip dosed mouse assessed as protection against subcutaneous metrazole-induced seizure2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models.
AID1704780Effect on spontaneous locomotor activity in Kunming mouse assessed as total distance traveled at 3 mg/kg, ig measured after 1 hr (Rvb = 13579 +/- 8864 millimeter)
AID306154Induction of cell death in Jurkat cells after 24 hrs2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540233Dose normalised AUC in human after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID52275Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
AID604743Displacement of radiolabeled warfarin from fatty acid containing human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID540231Dose normalised AUC in dog after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID131932Tested for inhibition of strychnine-induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID1346520Human GABAA receptor alpha1 subunit (GABAA receptors)1989Science (New York, N.Y.), Sep-22, Volume: 245, Issue:4924
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
AID1346504Human GABAA receptor alpha2 subunit (GABAA receptors)1989Science (New York, N.Y.), Sep-22, Volume: 245, Issue:4924
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
AID1346496Human GABAA receptor alpha3 subunit (GABAA receptors)1989Science (New York, N.Y.), Sep-22, Volume: 245, Issue:4924
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,501)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990826 (33.03)18.7374
1990's600 (23.99)18.2507
2000's490 (19.59)29.6817
2010's453 (18.11)24.3611
2020's132 (5.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 132.43

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.

MetricThis Compound (vs All)
Research Demand Index132.43 (24.57)
Research Supply Index7.99 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index251.42 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (132.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials239 (8.79%)5.53%
Reviews227 (8.35%)6.00%
Case Studies811 (29.83%)4.05%
Observational6 (0.22%)0.25%
Other1,436 (52.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (35)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT01291316]Phase 1/Phase 225 participants (Actual)Interventional2010-04-30Completed
Neurochemical,Metabonomics and Neuroimaging Characterization of TCM Diagnostic Subtypes of Major Depression Disorder [NCT02346682]Phase 475 participants (Anticipated)Interventional2015-02-28Recruiting
A Phase III, Randomized, Open Label, Single Center, Study on the Effects of Treatment of Epilepsia Partialis Continua With Clobazam Compared to Treatment With or in Addition to Lorazepam and/or Clonazepam [NCT02134366]Phase 37 participants (Actual)Interventional2014-07-31Terminated(stopped due to Recruitment Issues - Lack of target population)
An Open Label Benzodiazepine Study for the Treatment of Seizure Clusters in a Third Level Mexican Neurological Center [NCT06056349]150 participants (Anticipated)Interventional2023-05-01Recruiting
Effect of Clonazepam on REM Sleep Behavior Disorder in Patients With Parkinsonism: a Prospective, Randomized, Double-blind and Placebo-controlled Trial [NCT02312908]Phase 240 participants (Actual)Interventional2015-03-31Completed
Efficiency of Levetiracetam Intravenous in Association With Clonazepam Versus Clonazepam Alone in Prehospital Care of Generalised Tonicoclonic Status Epilepticus [NCT01150331]Phase 3203 participants (Actual)Interventional2009-07-31Completed
Exploring the Role of the GABAergic Modulation in Pain Transmission in Human. Effects of the GABAA Agonist N-desmethylclobazam on Central Sensitization: a Pharmacodynamic and Pharmacokinetic Study in Healthy Volunteers [NCT03375034]Phase 156 participants (Actual)Interventional2017-03-30Completed
Efficacy of Intravenous Clonazepam According to the Dosage in Children Status Epilepticus [NCT04287361]310 participants (Actual)Observational2019-08-30Completed
A Randomized Double-Blind, Double-Dummy, Crossover Study to Evaluate the Efficacy and Safety of Prolonged-Release Melatonin and Clonazepam in Patients With Rapid Eye Movement (REM) Sleep Behavior Disorder in Parkinson Disease [NCT02789592]Phase 230 participants (Anticipated)Interventional2016-07-31Not yet recruiting
A Randomised Controlled Trial of the Ketogenic Diet in the Treatment of Epilepsy in Children Under the Age of Two Years [NCT02205931]Phase 4160 participants (Anticipated)Interventional2015-01-31Recruiting
Burning Mouth Syndrome - Optimized Diagnostic Criteria and Treatment [NCT05059418]40 participants (Anticipated)Interventional2021-11-01Not yet recruiting
Clonazepam Effects on Brain Oscillations and Cognition in Schizophrenia [NCT03061136]Phase 40 participants (Actual)Interventional2016-10-31Withdrawn(stopped due to Delays in equipment procurement prevented the start of the study in time)
Treatment Refractory Panic Disorder [NCT00118417]Phase 2/Phase 346 participants (Actual)Interventional1999-03-31Completed
Effectiveness of Mucolox® and Clonazepam in Treatment of Burning Mouth Syndrome [NCT02690844]Phase 40 participants (Actual)Interventional2016-04-30Withdrawn
Effects of Gaba-a-Agonists on Pain Mechanisms: An Experimental Study in Healthy Volunteers [NCT01011036]Phase 317 participants (Actual)Interventional2009-12-31Completed
Evaluate The Pharmacokinetics Of Two Alprazolam Formulations (Immediate Release And Extended Release Tablets) And A Clonazepam Tablet In A Healthy Mexican Population [NCT00810316]Phase 124 participants (Actual)Interventional2008-10-31Completed
Long-term, Open, Naturalistic, Randomized Clinical Trial With Clonazepam and Paroxetine in Panic Disorder With or Without Agoraphobia [NCT02852577]Phase 4120 participants (Actual)Interventional2000-01-31Completed
The Benefit of Prophylactic Anticonvulsant in Post Cardiac Arrest Syndrome With Induced Mild Hypothermia [NCT01083784]Phase 460 participants (Anticipated)Interventional2010-03-31Enrolling by invitation
Use of Low Intensity Laser Combined With Topical Clonazepam for the Treatment of Burning Mouth Syndrome [NCT04313907]Phase 427 participants (Anticipated)Interventional2019-08-16Recruiting
Comparative, Randomized, Single-Dose, 2 Way Cross Over Bioavailability Study of Kali's Clonazepam Tablets 1 mg With That of Klonopin Tablets 1 mg in Healthy Adult Subjects Under Fasting Conditions. [NCT00652639]Phase 132 participants (Actual)Interventional2004-02-29Completed
Comparative, Randomized, Single-Dose, Bioavailability Study of Kali's Clonazepam ODT 1 mg With That of Klonopin Wafers 1 mg ODT in Healthy Adult Subjects Under Fasting Conditions. [NCT00652912]Phase 132 participants (Actual)Interventional2004-03-31Completed
Comparison Between Lorazepam, Clonazepam and Clonazepam + Fosphenytoin for the Treatment of Out-of-hospital Generalized Status Epilepticus in Adults Patients [NCT01870024]Phase 3434 participants (Actual)Interventional2013-06-26Completed
Improving Outcomes in Pharmacotherapy of Social Phobia [NCT00282828]Phase 4397 participants (Actual)Interventional2006-03-31Completed
Effect of Clonazepam on Cannabis Withdrawal and Relapse in Treatment-seeking Patients: Combined Inpatient/Outpatient Study [NCT02913924]Phase 268 participants (Actual)Interventional2016-12-31Completed
Combined Treatment With a Benzodiazepine (Clonazepam) and a Selective Serotonin Reuptake Inhibitor (Paroxetine) for Rapid Treatment of Posttraumatic Stress Disorder (PTSD) [NCT00025740]Phase 478 participants Interventional2001-10-31Completed
Assessment of the Effectiveness of the Selected Treatment Method and Psychological Disorders of Primary Burning Mouth Syndrome [NCT04884503]Phase 258 participants (Actual)Interventional2019-01-12Completed
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
Psychopharmacological Treatment of Emotional Distress: A Randomized Controlled Trial [NCT06133114]Phase 480 participants (Anticipated)Interventional2023-12-31Not yet recruiting
Evaluation of the Effect of Different Treatments on Pain Scores and Self-reported Oral Health-related Quality of Life in Individuals With Burning Mouth Syndrome: a Randomized Controlled Clinical Trial [NCT06040190]Phase 4150 participants (Anticipated)Interventional2023-11-01Not yet recruiting
The Efficacy of A Single Dose Clonazepam Compared With the Intermittent Diazepam to Prevent Recurrent Febrile Seizures in Queen Sirikit National Institute of Child Health [NCT04364321]74 participants (Anticipated)Interventional2020-05-13Recruiting
The Effectiveness of Acupuncture Versus Clonazepam in the Patients With Burning Mouth Syndrome [NCT02382029]Early Phase 14 participants (Actual)Interventional2014-03-31Completed
Efficacy of Hydroxyzine Versus Treatment as Usual for Panic Disorder: An Eight-Week, Open Label, Pilot, Randomized Controlled Trial. [NCT05737511]Phase 480 participants (Anticipated)Interventional2023-12-30Not yet recruiting
A Phase 2a, Open-label,Proof -Of-Concept Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of Intranasal Clonazepam in Adult Subjects With Epileptic Seizures [NCT00594945]Phase 245 participants (Actual)Interventional2007-12-31Completed
Excessive Crying in Children With Cerebral Palsy and Communication Deficits -a Fixed-sequence, Crossover Clinical Trial [NCT04523935]Phase 4131 participants (Actual)Interventional2005-12-07Completed
Efficacy and Safety of Melatonin and Rivotril Treatment for Idiopathic Rapid Eye Movement Sleep Disorder: Prospective Randomized Study. [NCT03255642]34 participants (Actual)Interventional2017-11-09Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00118417 (3) [back to overview]Change in Panic Disorder Symptoms, Phase 1 (Week 0 - Week 6)
NCT00118417 (3) [back to overview]Change in Panic Disorder Symptoms, Phase 2 (Week 6 - Week 12)
NCT00118417 (3) [back to overview]Change in Panic Disorder Symptoms, Phase 3 (Week 12 - Week 24)
NCT00282828 (2) [back to overview]Post-treatment Social Phobia Severity as Defined by Endpoint LSAS Scores
NCT00282828 (2) [back to overview]Rates of Remission (LSAS≤30) After 12 Weeks of Randomized Treatment During Phase II, Among Phase I Non-responders
NCT00594945 (1) [back to overview]Number of Spikes and Sharp Waves, Relative Change From Baseline to Treatment Day (%).
NCT02913924 (2) [back to overview]Time to Cannabis Use Relapse
NCT02913924 (2) [back to overview]Proportion of Cannabis Use Days Per Week

Change in Panic Disorder Symptoms, Phase 1 (Week 0 - Week 6)

This measure is the change in points between baseline and endpoint scores on the Panic Disorder Severity Scale (PDSS). The PDSS is a 7-item scale with each item rated from 0 (none) to 4 (extreme), for a total score range of 0 to 28 points, and an established interrater reliability of 0.87. (NCT00118417)
Timeframe: Measured at baseline and after Phase 1 (6 weeks)

InterventionPoints on a scale (Mean)
Moderate Sertraline Treatment4.3

[back to top]

Change in Panic Disorder Symptoms, Phase 2 (Week 6 - Week 12)

This measure is the change in points between baseline and endpoint scores on the Panic Disorder Severity Scale (PDSS). The PDSS is a 7-item scale with each item rated from 0 (none) to 4 (extreme), for a total score range of 0 to 28 points, and an established interrater reliability of 0.87. (NCT00118417)
Timeframe: Measured after Phase 1 (Week 6) and Phase 2 (Week 12)

InterventionPoints on a scale (Mean)
Increased Sertraline2.36
Sertraline Plus Placebo2.31

[back to top]

Change in Panic Disorder Symptoms, Phase 3 (Week 12 - Week 24)

This measure is the change in points between baseline and endpoint scores on the Panic Disorder Severity Scale (PDSS). The PDSS is a 7-item scale with each item rated from 0 (none) to 4 (extreme), for a total score range of 0 to 28 points, and an established interrater reliability of 0.87. (NCT00118417)
Timeframe: Measured after Phase 2 (Week 12) and Phase 3 (Week 24)

InterventionPoints on a scale (Mean)
Medication Optimization3.78
Augmented Cognitive Behavior Therapy2.9

[back to top]

Post-treatment Social Phobia Severity as Defined by Endpoint LSAS Scores

The Liebowitz Social Anxiety Scale (LSAS) is a 24-item scale assessing fear and avoidance in social and performance situations; it is widely used in studies of pharmacological treatment of Generalized Social Anxiety Disorder (GSAD). We analyzed the overall change in LSAS (last Phase II LSAS minus Week 10 LSAS). Higher numbers reflect greater drops in social anxiety disorder severity. Scores on the LSAS range from 0 to 144, with higher scores indicating greater pathology. (NCT00282828)
Timeframe: Change from Week 10 to Week 22

Interventionunits on a scale (Mean)
Sertraline and Clonazepam27
Venlafaxine18
Sertraline and Placebo16

[back to top]

Rates of Remission (LSAS≤30) After 12 Weeks of Randomized Treatment During Phase II, Among Phase I Non-responders

The Liebowitz Social Anxiety Scale (LSAS) is a 24-item scale assessing fear and avoidance in social and performance situations; it is widely used in studies of pharmacological treatment of Generalized Social Anxiety Disorder (GSAD). Scores on the LSAS range from 0 to 144, with higher scores indicating greater pathology. (NCT00282828)
Timeframe: Measured at Week 22 (Endpoint)

Interventionparticipants (Number)
Sertraline and Clonazepam17
Venlafaxine11
Sertraline and Placebo10

[back to top]

Number of Spikes and Sharp Waves, Relative Change From Baseline to Treatment Day (%).

Summary of video EEG number of spikes and sharp waves. Over a 24 hour period. (NCT00594945)
Timeframe: Change from baseline to treatment day

Interventionpercentage of baseline (Mean)
Intranasal Clonazepam 2 mg-7.4
Intranasal Clonazepam 3 mg-26.1

[back to top]

Time to Cannabis Use Relapse

for inpatient participants the number of days till relapse to cannabis use, post inpatient discharge, as recorded on the time line follow-back and confirmed by urine toxicology. (NCT02913924)
Timeframe: Number of days during 12 weeks of study participation

Interventiondays (Median)
Clonazepam1
Placebo1

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Proportion of Cannabis Use Days Per Week

for outpatient participants the proportion of cannabis use days per week as recorded by the Timeline Followback method (NCT02913924)
Timeframe: the 7 weeks of study participation or length of participants participation during the medication maintenance phase

,
Interventionproportion of use days (Mean)
week 1week 2week 3week 4week 5week 6week 7
Clonazepam0.740.780.710.670.670.580.58
Placebo0.790.750.700.640.640.650.67

[back to top]