Page last updated: 2024-12-05

loxapine

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Description

Loxapine: An antipsychotic agent used in SCHIZOPHRENIA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3964
CHEMBL ID831
CHEBI ID50841
SCHEMBL ID94146
MeSH IDM0012711

Synonyms (132)

Synonym
8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,5]benzoxazepine
BRD-K39915878-036-05-3
BRD-K39915878-036-04-6
gtpl205
DIVK1C_006919
az-004
loxitane
adasuve
2-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine
chembl831 ,
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,9,12,14-heptaene
8-chloro-6-(4-methylpiperazino)benzo[b][1,4]benzoxazepine;succinic acid
bdbm22871
cl71,563
cloxazepine
dibenzacepin
loxapine [usan:inn:ban]
2-chloro-11-(4-methylpiperazino)dibenzo(b,f)(1,4)oxazepine
dibenzoazepine
2-chloro-11-(4-methyl-1-piperazinyl)-dibenz(b,f)(1,4)oxazepine
hydrofluoride 3170
cl-62362
2-chloro-11-(4-methyl-1-piperazinyl)dibenz(b,f)(1,4)oxazepine
loxapin
hf 3170
brn 0626753
hf3170
hsdb 3111
loxapinum [inn-latin]
s 805
s-805
lw 3170
einecs 217-835-3
loxapina [inn-spanish]
cl 62362
dibenz(b,f)(1,4)oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-
sum 3170
lossapina [dcit]
SPECTRUM_000355
BPBIO1_000226
dibenz[b,f][1,4]oxazepine, 2-chloro-11-(4-methyl-1-piperazinyl)-
BSPBIO_000204
BSPBIO_003479
PRESTWICK2_000132
PRESTWICK3_000132
PDSP1_001058
LOPAC0_000720
QTL1_000050
SPECTRUM5_001857
loxapinum
loxapina
CHEBI:50841 ,
1977-10-2
C07104
loxapine
2-chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine
DB00408
oxilapine
loxapine (usan/inn)
adasuve (tn)
D02340
KBIOSS_000835
KBIO2_003403
KBIO1_001863
KBIO2_000835
KBIO2_005971
KBIO3_002983
SPECTRUM2_001737
PRESTWICK1_000132
SPECTRUM3_001830
SPBIO_002143
PRESTWICK0_000132
SPECPLUS_000823
SPBIO_001814
PDSP2_001042
NCGC00022279-04
NCGC00022279-05
NCGC00021145-01
NCGC00022279-03
8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine
NCGC00021145-07
sum-3170
cl 62,362
L001085
NCGC00021145-08
NCGC00021145-03
NCGC00021145-06
NCGC00021145-04
NCGC00021145-05
NCGC00021145-02
loxitane intramuscular
loxitane-c oral suspension
lossapina
staccato loxapine
unii-ler583670j
ler583670j ,
CCG-204805
HY-17390
CS-1105
loxapine [mart.]
loxapine [orange book]
loxapine [mi]
loxapine [hsdb]
loxapine [usan]
loxapine [inn]
loxapine [who-dd]
loxapine [vandf]
S5197
SCHEMBL94146
XJGVXQDUIWGIRW-UHFFFAOYSA-N
2-chloro-11-(4-methylpiperazino)dibenz[b,f][1,4]oxazepine
AB00053735_15
AB00053735_16
DTXSID7023229 ,
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaene
AKOS030526111
Q58614
BRD-K39915878-036-15-2
SDCCGSBI-0050698.P003
NCGC00021145-23
LOXAPINE (WATER)
LOXAPINE (DMSO)
F84888
MS-24900
EN300-6479125
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0,3,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaene
n05ah01
loxapina (inn-spanish)
dtxcid903229
2-chloro-11-(4-methylpiperazin-1-yl)dibenzo(b,f)(1,4)oxazepine
loxapine (mart.)
loxapinum (inn-latin)

Research Excerpts

Overview

Loxapine substitution is a promising option for patients with autism spectrum disorder (ASD) who develop antipsychotic-induced metabolic illness. Loxapin is a dibenzoxazepine neuroleptic that is metabolized by the liver in humans.

ExcerptReferenceRelevance
"Loxapine is a first-generation antipsychotic medication available in the United States in oral form for more than three decades."( Safety and efficacy review of inhaled loxapine for treatment of agitation.
Currier, G; Walsh, P, 2013
)
1.38
"Loxapine is a well-established, first-generation antipsychotic agent. "( Loxapine inhalation powder: a review of its use in the acute treatment of agitation in patients with bipolar disorder or schizophrenia.
Keating, GM, 2013
)
3.28
"Loxapine substitution is a promising option for patients with autism spectrum disorder (ASD) who develop antipsychotic-induced metabolic illness. "( Loxapine for Reversal of Antipsychotic-Induced Metabolic Disturbances: A Chart Review.
Andridge, R; Hellings, JA; Jain, S, 2016
)
3.32
"Loxapine is a first generation antipsychotic, belonging to the dibenzoxazepine class. "( The Role of Inhaled Loxapine in the Treatment of Acute Agitation in Patients with Psychiatric Disorders: A Clinical Review.
Carano, A; de Bartolomeis, A; de Berardis, D; Di Giannantonio, M; Fornaro, M; Iasevoli, F; Marini, S; Martinotti, G; Orsolini, L; Perna, G; Piersanti, M; Serroni, N; Tomasetti, C; Valchera, A; Vellante, F, 2017
)
2.22
"Loxapine is an older first-generation antipsychotic drug that is approved for the treatment of schizophrenia."( Now take a deep breath: inhaled loxapine for the treatment of acute agitation.
Howland, RH, 2012
)
1.38
"Loxapine is an atypical antipsychotic, with a lower risk of neurological side effects than first generation of antipsychotics. "( [Dysphagia or dysphagias during neuroleptic medication?].
Chaumartin, N; Lachaux, B; Monville, M, 2012
)
1.82
"Loxapine is a dibenzoxazepine neuroleptic that is metabolized by the liver in humans. "( Interspecies variability and drug interactions of loxapine metabolism in liver microsomes.
Bun, H; Bun, SS; Voeurng, V,
)
1.83
"Loxapine is a typical antipsychotic while isoloxapine, its 8Cl-isomer, shows atypicality in some animal models. "( Contrasting loxapine to its isomer isoloxapine--the critical role of in vivo D2 blockade in determining atypicality.
Kapur, S; McClelland, RA; Natesan, S; Nobrega, JN; Vanderspek, S, 2005
)
2.15
"Loxapine is a tricyclic antipsychotic drug with sedating properties."( Effect of loxapine on electrical brain activity, intracranial pressure, and middle cerebral artery flow velocity in traumatic brain-injured patients.
Abdennour, L; Coriat, P; Lescot, T; Naccache, L; Pereira, AR; Puybasset, L; Sanchez-Pena, P, 2007
)
1.46
"Loxapine is an antipsychotic which is not clearly distinct from typical or atypical drugs in terms of its effects on global or mental state. "( Loxapine for schizophrenia.
Bagnall, A; Chakrabarti, A; Chue, P; Fenton, M; Palaniswamy, V; Wong, W; Xia, J, 2007
)
3.23
"Loxapine is a tricyclic antipsychotic drug of the dibenzoxapine class. "( Parenteral loxapine in severely disturbed schizophrenic patients.
Cottereau, MJ; Deniker, P; Loo, H, 1980
)
2.09
"Loxapine is a neuroleptic of the dibenzoxazepine class; it is metabolized in vivo to desmethylloxapine (amoxapine) and 8-hydroxyamoxapine, two compounds with antidepressant activity."( Loxapine in the treatment of psychotic-depressive disorders: Measurement of antidepressant metabolites.
Burch, EA; Goldschmidt, TJ, 1983
)
2.43
"Loxapine is a drug which is used in the treatment of psychotic disorders. "( The role of metabolites in a bioequivalence study 1: loxapine, 7-hydroxyloxapine and 8-hydroxyloxapine.
Hawes, EM; Hsia, D; Hubbard, JW; McKay, G; Midha, KK, 1993
)
1.98
"Loxapine is a typical neuroleptic that shows great structural and functional homology to the atypical antipsychotic clozapine. "( A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes.
Barlas, C; Franks, P; Mishra, RK; Singh, AN; Singh, S, 1996
)
1.98
"Loxapine is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. "( Loxapine for schizophrenia.
Bagnall, A; Chue, P; Fenton, M; Leitner, M; Murphy, B; Wood, J, 2000
)
3.19
"Loxapine is a dibenzoxazepine tricyclic compound used to treat schizophrenia in the United States since 1976. "( Loxapine intoxication: case report and literature review.
Jenkins, AJ; Mazzola, CD; Miron, S, 2000
)
3.19
"Loxapine is a dibenzoxazepine, tricyclic compound recommended for the treatment of acute and chronic schizophrenia. "( Loxapine: a review of its pharmacological properties and therapeutic efficacy as an antipsychotic agent.
Avery, GS; Brogden, RN; Heel, RC; Speight, TM, 1978
)
3.14

Effects

Loxapine has the ability to control agitation without affecting spontaneous ventilation. It has effects on cortical and NAC DA and ACh release which are comparable to those of known atypical APDs.

ExcerptReferenceRelevance
"Loxapine has been adopted in the management of a wide range of acute disturbances, such as agitation in psychosis."( Fifty years of experience with loxapine for the rapid non-coercive tranquilization of acute behavioral disturbances in schizophrenia patients, and beyond.
Baloche, E; Corruble, E; Llorca, PM; Nuss, P; P Garay, R, 2022
)
1.73
"Loxapine has the ability to control agitation without affecting spontaneous ventilation."( Loxapine to control agitation during weaning from mechanical ventilation.
Cohen, Y; Dreyfuss, D; Gaudry, S; Hajage, D; Megarbane, B; Ricard, JD; Salomon, L; Sonneville, R; Sztrymf, B; Van Der Meersch, G; Vodovar, D, 2017
)
2.62
"Loxapine has effects on cortical and NAC DA and ACh release which are comparable to those of known atypical APDs. "( A comparison of the effects of loxapine with ziprasidone and thioridazine on the release of dopamine and acetylcholine in the prefrontal cortex and nucleus accumbens.
Ichikawa, J; Li, Z; Meltzer, HY, 2003
)
2.05

Actions

ExcerptReferenceRelevance
"Loxapine didn't inhibit bacterial growth in broth at concentration up to 500 μM and has no effect on Salmonella's type III secretion system genes' expression."( Loxapine, an antipsychotic drug, suppresses intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages.
Chen, CS; Chiu, HC; Fang, CS; Hsu, CY; Shiau, CW; Yang, CY, 2019
)
2.68

Treatment

Loxapine treatment shortens the agitation episode and attenuates the impact on the patient, facilitating ambulance transfer. Treatment is then stopped, resulting in a very rapid clinical improvement.

ExcerptReferenceRelevance
"Loxapine treatment shortens the agitation episode and attenuates the impact on the patient, facilitating ambulance transfer."( [New medical approach to out-of-hospital treatment of psychomotor agitation in psychiatric patients: a report of 14 cases].
Borraz-Clares, D; Cester-Martínez, A; Cortés-Ramas, JA; Pellicer-Gayarre, M, 2017
)
1.18
"Treatment with loxapine is then stopped, resulting in a very rapid clinical improvement."( [Dysphagia or dysphagias during neuroleptic medication?].
Chaumartin, N; Lachaux, B; Monville, M, 2012
)
0.72

Toxicity

Inhaled loxapine was generally safe and well tolerated and produced rapid improvement in agitated patients with psychotic disorders. The primary endpoint is incidence of serious adverse events (AEs) and respiratory AEs of special interest related to use of inhaled l Roxapine outside the hospital setting.

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Three serious adverse events occurred at least 6 days after treatment, but none were judged related to study treatment."( Efficacy and safety of loxapine for inhalation in the treatment of agitation in patients with schizophrenia: a randomized, double-blind, placebo-controlled trial.
Allen, MH; Cassella, JV; Feifel, D; Lesem, MD; Munzar, P; Ross, R; Spyker, DA; Zimbroff, DL, 2011
)
0.68
"Inhaled loxapine was generally safe and well tolerated and produced rapid improvement in agitated patients with psychotic disorders."( Efficacy and safety of loxapine for inhalation in the treatment of agitation in patients with schizophrenia: a randomized, double-blind, placebo-controlled trial.
Allen, MH; Cassella, JV; Feifel, D; Lesem, MD; Munzar, P; Ross, R; Spyker, DA; Zimbroff, DL, 2011
)
1.11
"All airway adverse events (AEs) were of mild or moderate severity."( Safety and tolerability of inhaled loxapine in subjects with asthma and chronic obstructive pulmonary disease--two randomized controlled trials.
Cassella, JV; Fishman, RS; Greos, LS; Gross, N; Meltzer, EO; Spangenthal, S; Spyker, DA, 2014
)
0.68
"Neuroleptic malignant syndrome (NMS) is a rare but severe adverse effect of antipsychotic drugs."( Pharmacist intervention to detect drug adverse events on admission to the emergency department: Two case reports of neuroleptic malignant syndrome.
Breuker, C; Castet-Nicolas, A; Giraud, I; Gourhant, V; Leenhardt, F; Perier, D; Pinzani, V; Villiet, M, 2017
)
0.46
" Safety was assessed using adverse event (AE), laboratory value, physical/neurologic examination, vital sign, electrocardiogram, suicidality, and extrapyramidal symptom assessment."( Pharmacokinetics and Safety of Single-Dose Inhaled Loxapine in Children and Adolescents.
Cassella, J; Hellriegel, E; Kunta, J; Rabinovich-Guilatt, L; Riesenberg, R; Selim, S; Smith, MA; Vinks, AA, 2017
)
0.71
" The primary endpoint is incidence of serious adverse events (AEs) and respiratory AEs of special interest related to use of inhaled loxapine outside the hospital setting."( Safety and efficacy of self-administered inhaled loxapine (ADASUVE) in agitated patients outside the hospital setting: protocol for a phase IV, single-arm, open-label trial.
Baleeiro Teixeira, T; Boldeanu, A; Garcia-Alonso, F; Gil, E, 2018
)
0.94

Pharmacokinetics

Loxapine Cmax was similar in smokers and nonsmokers with a GMR of 99. Pharmacokinetic parameters assessed included Cmax, Tmax, AUCinf, and T1/2.

ExcerptReferenceRelevance
"The objective of this randomized, double-blind, placebo-controlled, dose escalation study was to determine the pharmacokinetic characteristics, safety, and tolerability of single doses of inhaled loxapine aerosol in healthy volunteers."( Pharmacokinetics of loxapine following inhalation of a thermally generated aerosol in healthy volunteers.
Cassella, JV; Munzar, P; Spyker, DA, 2010
)
0.87
"To investigate the pharmacokinetic differences between the common nasal delivery models."( Pharmacokinetic comparison between the long-term anesthetized, short-term anesthetized and conscious rat models in nasal drug delivery.
Qian, S; Wong, YC; Zuo, Z, 2014
)
0.4
" Regarding the pharmacokinetic parameters (Cmax, Tmax, AUC, bioavailability) of tacrine and its metabolites, short-term anesthetized model resembled closer to conscious model than long-term anesthetized model."( Pharmacokinetic comparison between the long-term anesthetized, short-term anesthetized and conscious rat models in nasal drug delivery.
Qian, S; Wong, YC; Zuo, Z, 2014
)
0.4
" Pharmacokinetic parameters assessed included Cmax, Tmax, AUCinf, and T1/2 for loxapine and 8-OH-loxapine."( Effect of smoking on the pharmacokinetics of inhaled loxapine.
Cassella, JV; Fishman, RS; Huie, K; Spyker, DA; Takahashi, LH, 2014
)
0.88
"Loxapine Cmax was similar in smokers and nonsmokers with a GMR of 99."( Effect of smoking on the pharmacokinetics of inhaled loxapine.
Cassella, JV; Fishman, RS; Huie, K; Spyker, DA; Takahashi, LH, 2014
)
2.09
"This randomized, double-blind, placebo-controlled, parallel-group study was to determine the pharmacokinetic characteristics, safety, and tolerability of multiple doses of inhaled loxapine aerosol in subjects on a stable, oral, chronic antipsychotic regimen."( Multiple dose pharmacokinetics of inhaled loxapine in subjects on chronic, stable antipsychotic regimens.
Cassella, JV; Riesenberg, RA; Spyker, DA, 2015
)
0.87

Compound-Compound Interactions

ExcerptReferenceRelevance
" This enables us to choose between species to further validate drug-drug interaction studies."( Interspecies variability and drug interactions of loxapine metabolism in liver microsomes.
Bun, H; Bun, SS; Voeurng, V,
)
0.38
" These results further support the previous suggestion that the cortical dopamine system plays an important role in the effects of antipsychotic drugs administered in combination with fluvoxamine."( Lack of enhanced effect of antipsychotics combined with fluvoxamine on acetylcholine release in rat prefrontal cortex.
Ago, Y; Baba, A; Matsuda, T; Nakamura, S; Sato, M, 2006
)
0.33

Bioavailability

ExcerptReferenceRelevance
" Estimates of average bioavailability (AUC- infinity, AUC0t and Cmax) were obtained by the difference of the least squares means of log test and log reference."( The role of metabolites in a bioequivalence study 1: loxapine, 7-hydroxyloxapine and 8-hydroxyloxapine.
Hawes, EM; Hsia, D; Hubbard, JW; McKay, G; Midha, KK, 1993
)
0.54
" Comparison of the plasma AUC for the parent drugs following administration of the parent drugs and prodrugs allowed estimation of the apparent bioavailability of parent drug from prodrug dosing."( A novel prodrug approach for tertiary amines. 3. In vivo evaluation of two N-phosphonooxymethyl prodrugs in rats and dogs.
Charman, SA; Charman, WN; Krise, JP; Stella, VJ, 1999
)
0.3

Dosage Studied

Loxapine was often associated with psychotropic medications (anxiolytic, antidepressant, normothymic) In the present randomized crossover study to evaluate the bioequivalence of two dosage forms containing loxapin, the parent drug and its 7-hydroxy and 8-Hydroxy metabolites were monitored.

ExcerptRelevanceReference
" schedule) had demonstrable anti-psychotic activity in 14 of 25 chronic schizophrenic patients (56%), while TFP treatment in appropriate dosage showed a similar activity in 9 of 23 patients (39%)."( A double-blind comparison of loxitane--loxapine succinate and trifluoperazine hydrochloride in chronic schizophrenic patients.
Moyano, CZ, 1975
)
0.52
" Optimal dosage levels achieved with the concentrate proved satisfactory with the capsules."( Evaluation of loxapine hydrochloride oral concentrate (loxitane C) in acute schizophrenia.
Wittkopp, TA, 1978
)
0.62
" The average daily dosage was 81."( Loxapine versus perphenazine in psychotic patients. A double-blind, randomized, multicentre trial.
Fensbo, C; Fruensgaard, K; Hansen, KM; Sihm, F; Wollenberg, J, 1978
)
1.7
" Continuous administration of the two forms using the individualized sedation threshold dosage also failed to indicate any clinical or side effect differences in the two forms."( Clinical and plasma level characteristics of intramuscular and oral loxapine.
Cooper, TB; Lee, JH; Simpson, GM; Young, MA, 1978
)
0.49
" The therapeutic dosage range was found to be from 10 to 80 mg daily--about half that used for younger patients."( Loxapine succinate as a neuroleptic agent: evaluation in two populations of elderly psychiatric patients.
Branchey, MH; Elgart, B; Lee, JH; Simpson, GM; Vicencio, A, 1978
)
1.7
"The authors report a case of unequivocal Neuroleptic Malignant Syndrome, in which the patient was successfully rechallenged with a different potent neuroleptic in substantial dosage during the recovery phase."( Use of neuroleptics after an episode of neuroleptic malignant syndrome.
Lipman, E; Padgett, R, 1989
)
0.28
" During the four-week study, dosage was flexible to a maximum of 250 mg daily (mean daily dose, 176 mg)."( Acutely ill schizophrenic patients treated with loxapine. A clinical study in a community mental health center.
Rasul, M, 1980
)
0.52
" Using an optimizing dosage regime, the outcome variables studied were aggression frequency and the number and nature of emergent side effects."( Aggression in the demented patient: a double-blind study of loxapine versus haloperidol.
Ancill, RJ; Carlyle, W; Sheldon, L, 1993
)
0.53
" In the present randomized crossover study to evaluate the bioequivalence of two dosage forms containing loxapine, the parent drug and its 7-hydroxy and 8-hydroxy metabolites were monitored for up to 96 hours after the administration of the test or reference formulations."( The role of metabolites in a bioequivalence study 1: loxapine, 7-hydroxyloxapine and 8-hydroxyloxapine.
Hawes, EM; Hsia, D; Hubbard, JW; McKay, G; Midha, KK, 1993
)
0.75
" Dosing implications for drugs with a more even serotonin-2A (5-HT2A) receptor and dopamine-2 (D2) receptor blocking effect are discussed."( Pharmacologic and pharmacokinetic considerations in choosing an antipsychotic.
Ereshefsky, L, 1999
)
0.3
" Further study of the dose-response curve for loxapine and its usefulness in treating neuroleptic-resistant schizophrenia is indicated."( Low-dose loxapine in the treatment of schizophrenia: is it more effective and more "atypical" than standard-dose loxapine?
Jayathilake, K; Meltzer, HY, 1999
)
0.98
" The mean AUCs following iv and im dosing of parent drugs were not statistically different from the parent drug AUCs obtained after prodrug dosing."( A novel prodrug approach for tertiary amines. 3. In vivo evaluation of two N-phosphonooxymethyl prodrugs in rats and dogs.
Charman, SA; Charman, WN; Krise, JP; Stella, VJ, 1999
)
0.3
" The syndrome often develops after a sudden increase in dosage of the neuroleptic medication or in states of dehydration."( Neuroleptic malignant syndrome: case report and discussion.
Chandran, GJ; Keegan, DL; Mikler, JR, 2003
)
0.32
"Individuals in the extended dosing group were not at greater risk of symptom exacerbation, relapse, or rehospitalization; indeed, more rehospitalizations occurred in those receiving regular dosing."( "Extended" antipsychotic dosing in the maintenance treatment of schizophrenia: a double-blind, placebo-controlled trial.
Feingold, A; Kapur, S; Mann, S; Remington, G; Seeman, P; Shammi, C, 2011
)
0.37
" When plotting the PEC responders over time NNT becomes more robust as time after dosing elapses, with the 10 mg dose reaching a NNT of 4 by 20 min."( Inhaled loxapine for agitation revisited: focus on effect sizes from 2 Phase III randomised controlled trials in persons with schizophrenia or bipolar disorder.
Citrome, L, 2012
)
0.81
" The daily mean dosage of loxapine was 168,4 mg/d, in antipsychotic loxapine monotherapy (27%) or in combination with other antipsychotics (63%); it was often associated with psychotropic medications (anxiolytic [72%], antidepressant [21%], normothymic [19%])."( [RÉALITÉ LT, a pharmacoepidemiological study of semiology and therapeutic strategy of patients with schizophrenia treated by antipsychotic loxapine in routine clinical practice].
Augendre, J; Cousin, FR; Pascal, JC; Samuelian, JC; Saoud, M; Schmitt, L; Tonelli, I; Vacheron, MN; Vidailhet, P; Walter, M, 2012
)
0.88
" It was concluded that inhaled loxapine does not require dosage adjustment based on smoking behavior."( Effect of smoking on the pharmacokinetics of inhaled loxapine.
Cassella, JV; Fishman, RS; Huie, K; Spyker, DA; Takahashi, LH, 2014
)
0.94
" Loxapine was dosed flexibly up to 15 mg daily, starting with 5 mg on alternate days."( Loxapine add-on for adolescents and adults with autism spectrum disorders and irritability.
Aman, MG; Andridge, R; Barth, FX; Butler, MG; Cain, SE; Han, JC; Hellings, JA; Logan, M; Mikhnev, D; Palaguachi, GI; Reed, G; Teng, R; Zhou, X, 2015
)
2.77
" Data were also then retrospectively extracted from clinic charts regarding age, gender, diagnoses, LOX doses, treatment duration, concomitant medications, and LOX dosage reductions."( Low Dose Loxapine: Neuromotor Side Effects and Tolerability in Autism Spectrum Disorders.
Genovese, A; Hellings, JA; Jadhav, M; Jadhav, S; Jain, S, 2015
)
0.83
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antipsychotic agentAntipsychotic drugs are agents that control agitated psychotic behaviour, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect.
dopaminergic antagonistA drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists.
[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 (1)

ClassDescription
dibenzooxazepineAn organic heterotricyclic compound consisting of two benzene rings fused to a seven-membered ring containing one oxygen and one nitrogen atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency0.05800.00521.30228.1995AID624455
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency29.93490.035520.977089.1251AID504332
D(1A) dopamine receptorHomo sapiens (human)Potency0.24000.02245.944922.3872AID488982; AID488983
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency23.93410.134610.395030.1313AID1347049
chromobox protein homolog 1Homo sapiens (human)Potency4.46680.006026.168889.1251AID488953
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.48160.00669.809418.4927AID1347050
flap endonuclease 1Homo sapiens (human)Potency26.67950.133725.412989.1251AID588795
Ataxin-2Homo sapiens (human)Potency28.18380.011912.222168.7989AID588378
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium channel subfamily K member 2Homo sapiens (human)IC50 (µMol)20.00000.40003.92279.0000AID1307728
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00040.629810.0000AID5704
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)5.50000.00001.403910.0000AID141053
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.05400.00000.74728.0000AID61306
D(2) dopamine receptorHomo sapiens (human)Ki0.02100.00000.651810.0000AID64197; AID64327
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01800.00021.874210.0000AID36855
D(4) dopamine receptorHomo sapiens (human)IC50 (µMol)0.01400.00011.14239.3280AID63865
D(4) dopamine receptorHomo sapiens (human)Ki0.00630.00000.436210.0000AID64202; AID65954; AID659851
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01800.00021.270410.0000AID36855
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.01500.00030.37088.1600AID6563
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.00240.00000.385510.0000AID659850
Histamine H1 receptorRattus norvegicus (Norway rat)IC50 (µMol)1.00000.00000.32271.2589AID87514
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.02100.00000.705610.0000AID64197
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.04300.00000.14803.1800AID6648
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)0.02200.00011.01788.7960AID64825
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01800.00001.819410.0000AID36855
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.03250.00020.522910.0000AID238747; AID6563
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.00490.00021.11158.0280AID64202
Histamine H4 receptorHomo sapiens (human)Ki4.27590.00060.478710.0000AID1798265; AID266654
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium channel subfamily K member 2Homo sapiens (human)EC50 (µMol)19.70000.18702.72248.1800AID1802150
Histamine H4 receptorHomo sapiens (human)EC50 (µMol)0.21880.00740.601610.0000AID266655
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km27.00007.00007.00007.0000AID214939
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (203)

Processvia Protein(s)Taxonomy
cardiac ventricle developmentPotassium channel subfamily K member 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayPotassium channel subfamily K member 2Homo sapiens (human)
memoryPotassium channel subfamily K member 2Homo sapiens (human)
response to mechanical stimulusPotassium channel subfamily K member 2Homo sapiens (human)
response to axon injuryPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationPotassium channel subfamily K member 2Homo sapiens (human)
cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium channel subfamily K member 2Homo sapiens (human)
cochlea developmentPotassium channel subfamily K member 2Homo sapiens (human)
positive regulation of cellular response to hypoxiaPotassium channel subfamily K member 2Homo sapiens (human)
negative regulation of DNA biosynthetic processPotassium channel subfamily K member 2Homo sapiens (human)
stabilization of membrane potentialPotassium channel subfamily K member 2Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
heme catabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (44)

Processvia Protein(s)Taxonomy
outward rectifier potassium channel activityPotassium channel subfamily K member 2Homo sapiens (human)
potassium ion leak channel activityPotassium channel subfamily K member 2Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (53)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membranePotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
cell surfacePotassium channel subfamily K member 2Homo sapiens (human)
apical plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
neuronal cell bodyPotassium channel subfamily K member 2Homo sapiens (human)
calyx of HeldPotassium channel subfamily K member 2Homo sapiens (human)
astrocyte projectionPotassium channel subfamily K member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium channel subfamily K member 2Homo sapiens (human)
plasma membranePotassium channel subfamily K member 2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (139)

Assay IDTitleYearJournalArticle
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID230009Ratio of Ki value towards dopamine D2L receptor to that of D-4 receptor.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID659853Lipophilicity, log K of the compound in IAM-PC-DD2 HPLC column by UV method2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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).
AID235776Therapeutic ratio by subcutaneous dose of administration (quotient ED50 catalepsy/ED50 climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
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).
AID65733In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
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).
AID61306Compound was tested in vitro for its binding affinity towards human Dopamine receptor D21999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID23708Partition coefficient (logP)1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID65954Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
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).
AID1414679Induction ROS accumulation in human MDA-MB-231 cells by DCFH-DA-based assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Tanshinone-IIA-Based Analogues of Imidazole Alkaloid Act as Potent Inhibitors To Block Breast Cancer Invasion and Metastasis in Vivo.
AID458779Activity at HCMV US28 receptor assessed as receptor-mediated inositol phosphate response at 10 uM2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.
AID64327Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.
AID266668Agonist activity at human histamine H4 receptor transfected in SK-N-MC cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID624607Specific activity of expressed human recombinant UGT1A32000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
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).
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID458778Displacement of [125I]CCL5 from HCMV US28 receptor at 10 uM2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.
AID176501Compound is measured for inhibition of catalepsy in rats by peroral administration of compound1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID87514Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID659850Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
AID36855In vitro binding affinity towards Alpha-1 adrenergic receptor by the displacement of [3H]prazosin radioligand in rat cortical homogenates1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
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).
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID5483Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID228675Antipsychotic activity was determined from peroral administration of compound in mice (ED50 catalepsy-ED50 Climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
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).
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]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID64202Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
AID64270Compound was tested in vitro for its binding affinity towards CNS Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand; Not tested1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
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).
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]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' 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]
AID184473Reduction in motor activity in rats following p.o. administration.1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID25866Protonation constant of the compound.1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID5704Compound was tested in vitro for its binding affinity towards 5-hydroxytryptamine 2C receptor from rat using [3H]mesulergine as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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.
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).
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID176502Compound is measured for inhibition of catalepsy in rats by subcutaneous administration of compound1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
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).
AID235775Therapeutic ratio by peroral dose of administration (quotient ED50 catalepsy/ED50 climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID395326Fraction unbound in rat brain2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID141053Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID266654Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
AID214939Binding affinity against human UDP Glucuronosyltransferase 1A4 (UGT1A4)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Pharmacophore and quantitative structure-activity relationship modeling: complementary approaches for the rationalization and prediction of UDP-glucuronosyltransferase 1A4 substrate selectivity.
AID26538log K was measured potentiometrically in Brij35 medium1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
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.
AID63865Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.21999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
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]
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).
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID624608Specific activity of expressed human recombinant UGT1A42000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID112988Compound was tested for the neuroleptic activity as measured by it's antagonism of d-amphetamine induced lethality in grouped mice(GAL) when administered perorally; 0.09-0.241981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents.
AID6648Binding affinity towards rat 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID266655Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
AID231681Ratio between Ki values of D2 and D4 receptors1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID228676Antipsychotic activity was determined from subcutaneous administration of compound in mice (ED50 catalepsy-ED50 Climbing)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID1307728Inhibition of of human TREK1 expressed in whole COS cells assessed as reduction in channel currents2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
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]
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).
AID64825Binding affinity towards human Dopamine receptor D31999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID23695Partition coefficient (logP)1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID112271Inhibition of apomorphine induced climbing affects in mice by administering the compound perorally in mice1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
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
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID395329Dissociation constant, pKa by mass spectrometry2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID659855Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells at 10'-6 M after 60 mins by liquid scintillation counting2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
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).
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID26300log P values determined at pH 7.41999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID115620Inhibition of tetrabenazine induced depression in mice was following p.o. administration; Inactive.1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents.
AID6563Binding affinity towards human 5-hydroxytryptamine 6 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID64197Affinity was evaluated by inhibition of [3H]spiperone binding to COS cells transfected with human dopamine D-2(long) receptor1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
AID659857Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 cells at 10'-6 M after 60 mins by liquid scintillation counting2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
AID659851Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
AID61175Compound was tested in vitro for its binding affinity towards CNS Dopamine receptor D1 of rat corpus striatum using [3H]SCH-23390 as radioligand; Not tested1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
AID238747Binding affinity for human 5-hydroxytryptamine 6 receptor2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
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).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1345788Human D2 receptor (Dopamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345788Human D2 receptor (Dopamine receptors)1997Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Feb, Volume: 16, Issue:2
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Jan, Volume: 66, Issue:1
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
AID1346037Human H1 receptor (Histamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2000The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1
Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)2005Psychopharmacology, May, Volume: 179, Issue:2
Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1993The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24
Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.
AID1346445Human KNa1.1 (Calcium- and sodium-activated potassium channels)2012The Journal of pharmacology and experimental therapeutics, Mar, Volume: 340, Issue:3
The antipsychotic drug loxapine is an opener of the sodium-activated potassium channel slack (Slo2.2).
AID1345814Human D4 receptor (Dopamine receptors)1997Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Feb, Volume: 16, Issue:2
Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors.
AID1798265H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1802150TREK1 Assay from Article 10.1111/cbdd.12810: \\Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently.\\2016Chemical biology & drug design, Dec, Volume: 88, Issue:6
Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (342)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990127 (37.13)18.7374
1990's66 (19.30)18.2507
2000's37 (10.82)29.6817
2010's98 (28.65)24.3611
2020's14 (4.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 73.62

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 Index73.62 (24.57)
Research Supply Index6.08 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index128.69 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (73.62)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials71 (19.56%)5.53%
Reviews38 (10.47%)6.00%
Case Studies71 (19.56%)4.05%
Observational3 (0.83%)0.25%
Other180 (49.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (29)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Assessment of Loxapine in the Management of Restlessness During Mechanical Ventilation Weaning [NCT01193816]Phase 4100 participants (Actual)Interventional2011-05-31Completed
Pulmonary Safety of Staccato® Loxapine for Inhalation in Subjects With Chronic Obstructive Pulmonary Disease [NCT00889837]Phase 153 participants (Actual)Interventional2009-06-30Completed
A Phase IV, Open-label, Non-randomized, Clinical Trial to Evaluate the Safety of Self-administered ADASUVE® (Staccato Loxapine for Inhalation) in Agitated Patients Outside the Hospital Setting [NCT02525991]Phase 4323 participants (Actual)Interventional2016-09-08Completed
Tolerability and Analgesic Efficacy of Loxapine in Patients With Refractory, Chemotherapy-induced Neuropathic Pain [NCT02820519]Phase 24 participants (Actual)Interventional2016-06-07Terminated(stopped due to Intolerable high amount of adverse events)
Pulmonary Safety of Repeat Doses of Staccato® Loxapine for Inhalation in Healthy Volunteers [NCT00789360]Phase 130 participants (Actual)Interventional2008-11-30Completed
Outcomes of Antipsychotic Medication Use in the Emergency Department: A Retrospective Comparison Study [NCT02504450]93 participants (Actual)Observational2015-04-30Completed
A Postmarketing Observational Study to Evaluate the Safety of ADASUVE® (STACCATO® Loxapine for Inhalation) in Patients With Agitation Associated With Schizophrenia or Bipolar I Disorder [NCT03513549]10,000 participants (Anticipated)Observational2014-11-04Recruiting
A Randomized Double-blind Multicenter Double-dummy Non-inferiority Trial of Inhaled Loxapine and Intramuscular Haloperidol + Lorazepam for the Reduction of Agitation [NCT03110900]Phase 42 participants (Actual)Interventional2017-09-30Terminated(stopped due to Sponsor Withdrawal)
Pharmacokinetics of Staccato® Loxapine for Inhalation in Smokers Compared to Nonsmokers [NCT00873769]Phase 135 participants (Actual)Interventional2009-04-30Completed
Thorough QT/QTc Study of Staccato® Prochlorperazine for Inhalation in Healthy Volunteers [NCT00543062]Phase 148 participants (Actual)Interventional2007-10-31Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Single Dose Efficacy and Safety Study of Staccato® Loxapine for Inhalation in Patients With Migraine Headache [NCT00489476]Phase 2168 participants (Actual)Interventional2007-06-30Completed
Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736]725,489 participants (Actual)Observational2012-04-30Completed
Thorough QT/QTc Study of Staccato® Loxapine for Inhalation in Healthy Volunteers [NCT00874237]Phase 148 participants (Actual)Interventional2009-04-30Completed
A Multi-center, Randomized, Double-blind, Placebo-controlled, Single Dose Efficacy and Safety Study of StaccatoTM Loxapine for Inhalation in Schizophrenic Patients With Agitation. [NCT00369577]Phase 2129 participants (Actual)Interventional2006-08-31Completed
Pulmonary Safety of Staccato® Loxapine for Inhalation in Subjects With Asthma [NCT00890175]Phase 152 participants (Actual)Interventional2009-05-31Completed
A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic [NCT02600741]296 participants (Actual)Observational2015-07-24Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Multi-Dose Efficacy and Safety Study of Staccato® Loxapine for Inhalation in Patients With Bipolar I Disorder and Acute Agitation [NCT00721955]Phase 3314 participants (Actual)Interventional2008-07-31Completed
Facilitation of Weaning From Ventilator by Loxapine [NCT00122733]9 participants (Actual)Interventional2005-12-31Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Loxapine Succinate Capsules (25 mg; Mylan) and Loxitane® Capsules (25 mg; Watson) in Healthy Volunteers [NCT00648778]Phase 153 participants (Actual)Interventional2003-01-31Completed
Safety, Tolerability, and Pharmacokinetics of Multiple Doses of Staccato® Loxapine for Inhalation in Subjects on Chronic, Stable Antipsychotic Regimens [NCT00555412]Phase 140 participants (Actual)Interventional2007-10-31Completed
A Multi-center, Randomized, Double-blind, Placebo-controlled Efficacy and Safety Study of Staccato Loxapine (ADASUVE®) for Inhalation in Acutely Agitated Patients With Schizophrenia or Bipolar Disorder [NCT04148963]Phase 3150 participants (Anticipated)Interventional2019-12-01Not yet recruiting
Thorough QT/QTc Study of 2 Doses of ADASUVE® in Healthy Volunteers [NCT01854710]Phase 460 participants (Actual)Interventional2013-05-31Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Multi-Dose Efficacy and Safety Study of Staccato® Loxapine for Inhalation in Schizophrenic Patients With Agitation [NCT00628589]Phase 3344 participants (Actual)Interventional2008-02-29Completed
Comparison Between Midazolam and Loxapine in the Treatment of Agitated Patients in the Emergency Department [NCT00290082]Phase 3120 participants (Anticipated)Interventional2005-12-31Terminated(stopped due to 2 complications with midazolam)
ADASUVE®-Lorazepam Drug-Drug Interaction Study [NCT01877642]Phase 422 participants (Actual)Interventional2013-06-30Completed
A Nonrandomized, Open-Label, Multicenter, Phase 1 Study to Assess the Safety and Pharmacokinetics of ADASUVE® (STACCATO® Loxapine for Inhalation) at Doses of 2.5, 5, or 10 mg in Children and Adolescents (10 Through 17 Years of Age) With Any Condition Warr [NCT02184767]Phase 130 participants (Actual)Interventional2014-07-31Completed
AGItated Patients Management: intraNASAL Midazolam vs Intramuscular Loxapine, a Randomized Non Inferiority Trial [NCT05324852]Phase 3830 participants (Anticipated)Interventional2023-04-14Recruiting
Safety, Tolerability, and Pharmacokinetics of a Single Dose of Staccato™ Loxapine for Inhalation in Normal, Healthy Volunteers [NCT00444028]Phase 150 participants (Actual)Interventional2005-09-30Completed
A Multi-center, Randomized, Double-Blind, Placebo-Controlled, Single Dose Efficacy and Safety Study of Staccato® Loxapine for Inhalation in Outpatients With Migraine Headache [NCT00825500]Phase 2366 participants (Actual)Interventional2009-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00369577 (4) [back to overview]BARS Change From Baseline After Drug Treatment
NCT00369577 (4) [back to overview]CGI-I Responders
NCT00369577 (4) [back to overview]Clinical Global Impressions-Improvement Scale (CGI-I) After Drug Administration
NCT00369577 (4) [back to overview]PANSS-EC Change From Baseline
NCT00444028 (6) [back to overview]Half-life
NCT00444028 (6) [back to overview]Dose Proportionality (AUCinf) by Power Analysis
NCT00444028 (6) [back to overview]Clearance
NCT00444028 (6) [back to overview]Cmax
NCT00444028 (6) [back to overview]ke
NCT00444028 (6) [back to overview]Tmax
NCT00489476 (3) [back to overview]Pain-free at 2 Hours
NCT00489476 (3) [back to overview]Pain-relief Response (Pain Severity of NONE or MILD) at 2 Hours
NCT00489476 (3) [back to overview]Responders, Sustained Freedom From Pain
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 30 ms
NCT00543062 (7) [back to overview]Maximum Effect of Inhaled Prochlorperazine on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo
NCT00543062 (7) [back to overview]Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI > 450 ms
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI > 480 ms
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 60 ms
NCT00543062 (7) [back to overview]QTcI Versus Prochlorperazine Concentration
NCT00628589 (3) [back to overview]Clinical Global Impression-Improvement (CGI-I) Score
NCT00628589 (3) [back to overview]Change in PANSS-EC From Baseline
NCT00628589 (3) [back to overview]CGI-I Responders
NCT00721955 (3) [back to overview]CGI-I Responders
NCT00721955 (3) [back to overview]Change in PANSS Excited Component (PEC) Score From Baseline Following Dose #1 of Staccato Loxapine, Compared With Placebo
NCT00721955 (3) [back to overview]Clinical Global Impression-Improvement (CGI-I) Score Following Dose #1 of Staccato Loxapine, Compared With Placebo
NCT00789360 (2) [back to overview]The Largest Treatment Difference (Loxapine - Placebo) in Change in FVC From Baseline by Spirometry
NCT00789360 (2) [back to overview]The Largest Treatment Difference (Loxapine - Placebo) in Change in FEV1 From Baseline by Spirometry
NCT00825500 (2) [back to overview]Photophobia Free
NCT00825500 (2) [back to overview]Pain-Relief at 2 Hours Post-treatment
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 60 ms
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 30 ms
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI > 480 ms
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI > 450 ms
NCT00874237 (7) [back to overview]Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)
NCT00874237 (7) [back to overview]Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo
NCT00874237 (7) [back to overview]Cardiac Repolarization Change (QTcI) Versus Loxapine Concentration Relationship Following Treatment With Staccato Loxapine in Healthy Volunteers.
NCT01854710 (7) [back to overview]Subjects With QTcI > 480 ms
NCT01854710 (7) [back to overview]Subjects With QTcI Increase > 30 ms From Baseline
NCT01854710 (7) [back to overview]Subjects With QTcI Increase > 60 ms From Baseline
NCT01854710 (7) [back to overview]Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo
NCT01854710 (7) [back to overview]Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)
NCT01854710 (7) [back to overview]QTc Versus Loxapine Concentration
NCT01854710 (7) [back to overview]Subjects With QTcI > 450 ms
NCT01877642 (8) [back to overview]Maximum Level of Sedation for Lorazepam 1 mg IM + ADASUVE 10 mg
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Cogscreen Pathfinder Response for Combined vs Individual (Lorazepam, Loxapine)
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Diastolic Blood Pressure for Combined vs Individual (Lorazepam, Loxapine)
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Pulse Oximetry for Combined vs Individual (Lorazepam, Loxapine)
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Respiration Rate for Combined vs Individual (Lorazepam, Loxapine)
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Sedation for Combined vs Individual (Lorazepam, Loxapine)
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Systolic Blood Pressure for Combined vs Individual (Lorazepam, Loxapine)
NCT01877642 (8) [back to overview]Relative Pharmacodynamic Effect on Heart Rate for Combined vs Individual (Lorazepam, Loxapine)

BARS Change From Baseline After Drug Treatment

Change from baseline on the Behavioral Activity Rating Scale (BARS) ranging from 1 to 7 where: 1 = difficult or unable to rouse, 2 = asleep but responds normally to verbal or physical contact, 3 = drowsy, appears sedated, 4 = quiet, and awake (normal level of activity), 5 = signs of overt (physical or verbal) activity, calms down with instructions, 6 = extremely or continuously active, not requiring restraint, 7 = violent, requires restraint. (NCT00369577)
Timeframe: 2 hours

InterventionBARS Score, Change from Baseline, units (Mean)
Inhaled Placebo-0.930
Inhaled Loxapine 5 mg-1.53
Inhaled Loxapine 10 mg-2.02

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CGI-I Responders

Frequency of response based on the CGI-I (defined as achieving a CGI-I score of 1 or 2 at 2 hours after administration of the inhalation) (NCT00369577)
Timeframe: 2 hours

InterventionParticipants (Count of Participants)
Inhaled Placebo9
Inhaled Loxapine 5 mg22
Inhaled Loxapine 10 mg25

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Clinical Global Impressions-Improvement Scale (CGI-I) After Drug Administration

Clinical Global Impression- Improvement (CGI-I) scores ranged from 1 to 7: 0=not assessed (missing), 1=very much improved, 2=much improved, 3=minimally improved, 4=no change, 5=minimally worse, 6=much worse, 7=very much worse. (NCT00369577)
Timeframe: 2 hours

InterventionCGI-I Units (7=worse, 1=better) (Mean)
Inhaled Placebo3.19
Inhaled Loxapine 5 mg2.53
Inhaled Loxapine 10 mg2.28

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PANSS-EC Change From Baseline

The Positive and Negative Syndrome Scale-Excited Component (PANSS-EC) comprises 5 items associated with agitation: poor impulse control, tension, hostility, uncooperativeness, and excitement; each scored 1 (min) to 7 (max). The PANSS-EC, the sum of these 5 subscales, thus ranges from 5 to 35. Individuals were eligible if they had a PANSS-EC of ≥14 (out of 35) and a score ≥4 (out of 7) on at least 1 of the 5 items. (NCT00369577)
Timeframe: 2 hours

InterventionPANSS units (Mean)
Inhaled Placebo-4.98
Inhaled Loxapine 5 mg-6.71
Inhaled Loxapine 10 mg-8.56

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Half-life

Half-life of the terminal elimination phase of loxapine concentrations (NCT00444028)
Timeframe: predose, 0.5, 1, 2, 3, 5, 10, 30 and 45 min, 1, 2, 4, 6, 12, and 24 hours

Interventionhours (Mean)
Staccato Loxapine 0.625 mg5.2
Staccato Loxapine 1.25 mg6.56
Staccato Loxapine 2.5 mg6.92
Staccato Loxapine 5 mg6.2
Staccato Loxapine 10 mg6.14

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Dose Proportionality (AUCinf) by Power Analysis

"Dose proportionality by power analysis examines the linear regression of the log-AUC versus log-Dose on a by-patient basis across all doses administered. The slope and 90% confidence interval (CI) provide a clear, quantitative (best practices) assessment of the relationship of drug delivered to dose administered. The units on such analyses are generally those of slope (rise over run), with 1.000 being perfect. Although any positive slope might be considered clinically useful, a 90% CI within the criteria of 0.800-1.250 may be considered a delivery system which is as good as it gets." (NCT00444028)
Timeframe: predose, 0.5, 1, 2, 3, 5, 10, 30 and 45 min, 1, 2, 4, 6, 12, and 24 hours

Interventionhr*mcg/L (Mean)
Staccato Loxapine 0.625 mg11.9
Staccato Loxapine 1.25 mg23.4
Staccato Loxapine 2.5 mg44.6
Staccato Loxapine 5 mg95.5
Staccato Loxapine 10 mg140.6

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Clearance

clearance (CL/F) of lozxapine (NCT00444028)
Timeframe: predose, 0.5, 1, 2, 3, 5, 10, 30 and 45 min, 1, 2, 4, 6, 12, and 24 hours

InterventionL/hour (Mean)
Staccato Loxapine 0.625 mg56.2
Staccato Loxapine 1.25 mg55.9
Staccato Loxapine 2.5 mg61.1
Staccato Loxapine 5 mg53.8
Staccato Loxapine 10 mg78

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Cmax

maximum concentration of loxapine observed (NCT00444028)
Timeframe: predose, 0.5, 1, 2, 3, 5, 10, 30 and 45 min, 1, 2, 4, 6, 12, and 24 hours

Interventionng/mL (Mean)
Staccato Loxapine 0.625 mg6.5
Staccato Loxapine 1.25 mg9.7
Staccato Loxapine 2.5 mg62.9
Staccato Loxapine 5 mg105
Staccato Loxapine 10 mg134

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ke

elimination rate constant (NCT00444028)
Timeframe: predose, 0.5, 1, 2, 3, 5, 10, 30 and 45 min, 1, 2, 4, 6, 12, and 24 hours

Intervention/hour (Mean)
Staccato Loxapine 0.625 mg.143
Staccato Loxapine 1.25 mg.111
Staccato Loxapine 2.5 mg.108
Staccato Loxapine 5 mg.115
Staccato Loxapine 10 mg.122

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Tmax

Tmax = time from inhalation to to maximum observed loxapine concentration (NCT00444028)
Timeframe: predose, 0.5, 1, 2, 3, 5, 10, 30 and 45 min, 1, 2, 4, 6, 12, and 24 hours

Interventionminutes (Mean)
Staccato Loxapine 0.625 mg12.6
Staccato Loxapine 1.25 mg2.15
Staccato Loxapine 2.5 mg2.87
Staccato Loxapine 5 mg2.13
Staccato Loxapine 10 mg5.25

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Pain-free at 2 Hours

Pain-free (Pain-IHS) at the 2 hour time point (NCT00489476)
Timeframe: Baseline and 2 h post-dose

InterventionParticipants (Count of Participants)
Staccato Placebo3
1.25 mg Staccato Loxapine12
2.5 mg Staccato Loxapine13
5 mg Staccato Loxapine9

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Pain-relief Response (Pain Severity of NONE or MILD) at 2 Hours

"The primary efficacy endpoint was Pain-relief response as defined by the International Headache Society (Pain-IHS) as a pain severity of NONE or MILD.~Intent to treat (ITT) with last observation carried forward (LOCF)" (NCT00489476)
Timeframe: Baseline and 2 h post-dose

Interventionparticipants (Number)
Staccato Placebo20
1.25 mg Staccato Loxapine29
2.5 mg Staccato Loxapine34
5 mg Staccato Loxapine33

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Responders, Sustained Freedom From Pain

The percentages of patients with sustained freedom from pain (pain-free at 2 hours after dosing with no rescue medication and no recurrence of headache from 2 to 24 hours) (NCT00489476)
Timeframe: Baseline through 24 h post-dose

InterventionParticipants (Count of Participants)
Staccato Placebo3
1.25 mg Staccato Loxapine9
2.5 mg Staccato Loxapine11
5 mg Staccato Loxapine7

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Numbers and % of Subjects With QTcI Change > 30 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 30 ms at any of the outcome measure time points (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

InterventionParticipants (Count of Participants)
Placebo0
Inhaled Prochlorperazine 5 mg1
Inhaled Prochlorperazine 10 mg0

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Maximum Effect of Inhaled Prochlorperazine on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo

Time-matched differences in QTcI values between the maximum of the mean difference from baseline of the QTcI interval after time-matched placebo subtraction for treatment at 11 post-inhalation times. (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

Interventionmilliseconds (Least Squares Mean)
Placebo+Inhaled Prochlorperazine 5 mg Crossover Subjects5.493
Placebo+Inhaled Prochlorperazine 10 mg Crossover Subjects5.229

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Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)

A thorough QT/QTc study may be considered to have demonstrated assay sensitivity if 1 or more of the lower 95% CI values exceeds 5 msec (NCT00543062)
Timeframe: 1, 1.5, 2, 2.5, 3, 5 hours

Interventionmilliseconds (Least Squares Mean)
Placebo+Oral Moxifloxacin 400 mg Crossover Subjects9.595

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Numbers and % of Subjects With QTcI > 450 ms

Numbers and Percents of Subjects with QTcI exceeding 450 ms (NCT00543062)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
Placebo3
Inhaled Prochlorperazine 5 mg4
Inhaled Prochlorperazine 10 mg6

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Numbers and % of Subjects With QTcI > 480 ms

Numbers and Percents of Subjects with QTcI exceeding 480 ms at any of the outcome measure time points (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

InterventionParticipants (Count of Participants)
Placebo0
Inhaled Prochlorperazine 5 mg0
Inhaled Prochlorperazine 10 mg1

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Numbers and % of Subjects With QTcI Change > 60 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 60 ms at any of the outcome measure time points (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

InterventionParticipants (Count of Participants)
Placebo0
Inhaled Prochlorperazine 5 mg0
Inhaled Prochlorperazine 10 mg0

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QTcI Versus Prochlorperazine Concentration

QTcI @ median prochlorperazine concentration (3.75 mcg/mL) based on linear and nonlinear regression of QTcI versus time matched serum prochlorperazine concentrations (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

Interventionmilliseconds (Least Squares Mean)
Inhaled Prochlorperazine2.83

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Clinical Global Impression-Improvement (CGI-I) Score

Clinical Global Impression- Improvement (CGI-I) scores ranged from 1 to 7: 0=not assessed (missing), 1=very much improved, 2=much improved, 3=minimally improved, 4=no change, 5=minimally worse, 6=much worse, 7=very much worse. (NCT00628589)
Timeframe: Baseline and 2 hours

Interventionunits on a scale (Mean)
Inhaled Placebo2.8
Inhaled Loxapine 5 mg2.3
Inhaled Loxapine 10 mg2.1

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Change in PANSS-EC From Baseline

The Positive and Negative Syndrome Scale-Excited Component (PANSS-EC) comprises 5 items associated with agitation: poor impulse control, tension, hostility, uncooperativeness, and excitement; each scored 1 (min) to 7 (max). The PANSS-EC, the sum of these 5 subscales, thus ranges from 5 to 35. Individuals were eligible if they had a PANSS-EC of ≥14 (out of 35) and a score ≥4 (out of 7) on at least 1 of the 5 items. (NCT00628589)
Timeframe: Baseline and 2 hours

Interventionunits on a scale (Mean)
Inhaled Placebo-5.5
Inhaled Loxapine 5 mg-8.1
Inhaled Loxapine 10 mg-8.6

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CGI-I Responders

Frequency of response based on the CGI-I (defined as achieving a CGI-I score of 1 or 2 at 2 hours after administration of the inhalation) (NCT00628589)
Timeframe: Baseline and 2 hours

InterventionParticipants (Count of Participants)
Inhaled Placebo41
Inhaled Loxapine 5 mg66
Inhaled Loxapine 10 mg75

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CGI-I Responders

Frequency of response based on the CGI-I (defined as achieving a CGI-I score of 1 or 2 at 2 hours after administration of the inhalation) (NCT00721955)
Timeframe: Baseline and 2 hours

InterventionParticipants (Count of Participants)
Inhaled Placebo29
Inhaled Loxapine 5 mg69
Inhaled Loxapine 10 mg78

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Change in PANSS Excited Component (PEC) Score From Baseline Following Dose #1 of Staccato Loxapine, Compared With Placebo

The Positive and Negative Syndrome Scale-Excited Component (PANSS-EC) comprises 5 items associated with agitation: poor impulse control, tension, hostility, uncooperativeness, and excitement; each scored 1 (min) to 7 (max). The PANSS-EC, the sum of these 5 subscales, thus ranges from 5 to 35. Individuals were eligible if they had a PANSS-EC of ≥14 (out of 35) and a score ≥4 (out of 7) on at least 1 of the 5 items. (NCT00721955)
Timeframe: Baseline and 2 hours

Interventionunits on a scale (Mean)
Inhaled Placebo-4.9
Inhaled Loxapine 5 mg-8.1
Inhaled Loxapine 10 mg-9.0

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Clinical Global Impression-Improvement (CGI-I) Score Following Dose #1 of Staccato Loxapine, Compared With Placebo

Clinical Global Impression- Improvement (CGI-I) scores ranged from 1 to 7: 0=not assessed (missing), 1=very much improved, 2=much improved, 3=minimally improved, 4=no change, 5=minimally worse, 6=much worse, 7=very much worse. (NCT00721955)
Timeframe: Baseline and 2 hours

Interventionunits on a scale (Mean)
Inhaled Placebo3.0
Inhaled Loxapine 5 mg2.1
Inhaled Loxapine 10 mg1.9

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The Largest Treatment Difference (Loxapine - Placebo) in Change in FVC From Baseline by Spirometry

The largest treatment difference (Loxapine - Placebo) across the 17 post-treatment time points (15 min to 32 hr) in FVC Change from Same-Period Baseline (NCT00789360)
Timeframe: 17 post-treatment time points (15 min to 32 hr)

Interventionliters (Least Squares Mean)
Inhaled Loxapine-0.271
Inhaled Staccato-0.149

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The Largest Treatment Difference (Loxapine - Placebo) in Change in FEV1 From Baseline by Spirometry

The largest treatment difference (Loxapine - Placebo) across the 17 post-treatment time points (15 min to 32 hr) in FEV1 Change from Same-Period Baseline, (NCT00789360)
Timeframe: 17 post-treatment time points (15 min to 32 hr)

Interventionliters (Least Squares Mean)
Inhaled Loxapine-0.1042
Inhaled Staccato Placebo-0.1025

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Photophobia Free

Free of Photophobia at 2 Hours Post-treatment (NCT00825500)
Timeframe: 2 hours

InterventionParticipants (Count of Participants)
Inhaled Placebo59
Inhaled Loxapine 1.25 mg47
Inhaled Loxapine 2.5 mg54

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Pain-Relief at 2 Hours Post-treatment

Pain-Relief=pretreatment pain rating of 2 (moderate) or 3 (severe) and a rating of 0 (none) or 1 (mild) at the designated assessment time (NCT00825500)
Timeframe: 2 hours

InterventionParticipants (Count of Participants)
Inhaled Placebo56
Inhaled Loxapine 1.25 mg65
Inhaled Loxapine 2.5 mg66

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Numbers and % of Subjects With QTcI Change > 60 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 60 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg0
Inhaled Placebo0

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Numbers and % of Subjects With QTcI Change > 30 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 30 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg1
Inhaled Placebo1

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Numbers and % of Subjects With QTcI > 480 ms

Numbers and Percents of Subjects with QTcI exceeding 480 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg0
Inhaled Placebo0

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Numbers and % of Subjects With QTcI > 450 ms

Numbers and Percents of Subjects with QTcI exceeding 450 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg1
Inhaled Placebo1

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Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)

A thorough QT/QTc study may be considered to have demonstrated assay sensitivity if 1 or more of the lower 95% CI values exceeds 5 msec ant any of the 9 predetermined time points (NCT00874237)
Timeframe: 1, 1.5, 2, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmseconds (Least Squares Mean)
Oral Moxifloxacin vs Placebo Crossover Subjects8.356

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Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo

Largest of the upper CIs of the time matched differences in QTcI values between the maximum of the mean difference from baseline of the QTcI interval after time matched placebo subtraction for ADASUVE treatment at 12 prespecified post inhalation times (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

Interventionmseconds (Least Squares Mean)
Inhaled Loxapine 10 mg vs Placebo Crossover Subjects5.418

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Cardiac Repolarization Change (QTcI) Versus Loxapine Concentration Relationship Following Treatment With Staccato Loxapine in Healthy Volunteers.

QTcI change at the median loxapine concentration (32.2 mcg/mL) based on nonlinear regression of QTcI versus log of time matched serum loxapine concentrations. This analysis looks for repolarization versus concentration relationship in a positive or negative thorough QT/QTc study result. (NCT00874237)
Timeframe: 24 hours

Interventionmseconds (Least Squares Mean)
Inhaled Loxapine 10 mg4.238

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Subjects With QTcI > 480 ms

Numbers of Subjects with QTcI > 480 ms (or 500 ms) at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo0
ADASUVE 10 mg x 2 Doses0

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Subjects With QTcI Increase > 30 ms From Baseline

Numbers of Subjects with QTcI Increase > 30 ms from Baseline at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo0
ADASUVE 10 mg x 2 Doses1

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Subjects With QTcI Increase > 60 ms From Baseline

Numbers of Subjects with QTcI Increase > 60 ms From Baseline at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo0
ADASUVE 10 mg x 2 Doses0

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Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo

Time-matched differences in QTcI values between the maximum of the mean difference from baseline of the QTcI interval after time-matched placebo subtraction for ADASUVE treatment at 12 post-inhalation times. (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmsec (Least Squares Mean)
ADASUVE-Placebo Crossover Subjects4.04

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Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)

A thorough QT/QTc study may be considered to have demonstrated assay sensitivity if 1 or more of the lower 95% CI values exceeds 5 msec (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmsec (Least Squares Mean)
Moxifloxacin QT Crossover Subjects10.47

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QTc Versus Loxapine Concentration

QTc @ Cmax based on linear and nonlinear regression of QTcI versus time matched serum loxapine concentrations (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmsec (Least Squares Mean)
ADASUVE 10 mg x 2 Doses2.6

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Subjects With QTcI > 450 ms

Numbers of Subjects with QTcI > 450 ms at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo2
ADASUVE 10 mg x 2 Doses2

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Maximum Level of Sedation for Lorazepam 1 mg IM + ADASUVE 10 mg

Determine the maximum level of sedation for Lorazepam 1 mg IM + ADASUVE 10 mg based on the 100 mm Visual Analog Scale (VAS) ranging from (0=sleepy to 100=wide awake) (NCT01877642)
Timeframe: 24 hours

Interventionunits on a scale (Mean)
Open Label Group12.3

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Relative Pharmacodynamic Effect on Cogscreen Pathfinder Response for Combined vs Individual (Lorazepam, Loxapine)

LS Means ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for Cogscreen Pathfinder Response following administration of Lorazepam+Loxapine compared to the same measure following each control drug (Lorazepam, Loxapine) given alone (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam134
Lorazepam+Loxapine / Loxapine133

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Relative Pharmacodynamic Effect on Diastolic Blood Pressure for Combined vs Individual (Lorazepam, Loxapine)

LS Means ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for diastolic blood pressure following administration of Lorazepam+Loxapine compared to the same measure following each control drug (Lorazepam, Loxapine) given alone (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam101.8
Lorazepam+Loxapine / Loxapine100.3

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Relative Pharmacodynamic Effect on Pulse Oximetry for Combined vs Individual (Lorazepam, Loxapine)

LS Means ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for pulse oximetry following administration of Lorazepam+Loxapine compared to the same measure following each control drug (Lorazepam, Loxapine) given alone (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam99.7
Lorazepam+Loxapine / Loxapine100.3

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Relative Pharmacodynamic Effect on Respiration Rate for Combined vs Individual (Lorazepam, Loxapine)

LS Mean ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for respiration rate following administration of Lorazepam+Loxapine compared to the same measure following each control drug given alone (Lorazepam, Loxapine) (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam94.3
Lorazepam+Loxapine / Loxapine97.3

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Relative Pharmacodynamic Effect on Sedation for Combined vs Individual (Lorazepam, Loxapine)

LS Means ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for sedation based on a 100 mm Visual Analog Scale (VAS) ranging from (0=sleepy to 100=wide awake) following administration of Lorazepam+Loxapine compared to the same measure following each control drug given alone (Lorazepam, Loxapine) (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam41.7
Lorazepam+Loxapine / Loxapine95.7

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Relative Pharmacodynamic Effect on Systolic Blood Pressure for Combined vs Individual (Lorazepam, Loxapine)

LS Means ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for systolic blood pressure following administration of Lorazepam+Loxapine compared to the same measure following each control drug (Lorazepam, Loxapine) given alone (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam100
Lorazepam+Loxapine / Loxapine102

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Relative Pharmacodynamic Effect on Heart Rate for Combined vs Individual (Lorazepam, Loxapine)

LS Means ratio (90% CI) of the area under the curve for 0 to 24 hours (AUC 0-24) for heart rate following administration of Lorazepam+Loxapine compared to the same measure following each control drug (Lorazepam, Loxapine) given alone (NCT01877642)
Timeframe: 24 hours

Interventionpercentage of effect on control drug (Geometric Least Squares Mean)
Lorazepam+Loxapine / Lorazepam96.9
Lorazepam+Loxapine / Loxapine99.7

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